50 results on '"Schou, Magnus"'
Search Results
2. Reactive Palladium–Ligand Complexes for 11C-Carbonylation at Ambient Pressure: A Breakthrough in Carbon-11 Chemistry
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Dahl, Kenneth, primary, Lindberg, Anton, additional, Vasdev, Neil, additional, and Schou, Magnus, additional
- Published
- 2023
- Full Text
- View/download PDF
3. Quantification and reliability of [11C]VC - 002 binding to muscarinic acetylcholine receptors in the human lung — a test-retest PET study in control subjects
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Cselényi, Zsolt, Jucaite, Aurelija, Kristensson, Cecilia, Stenkrona, Per, Ewing, Pär, Varrone, Andrea, Johnström, Peter, Schou, Magnus, Vazquez-Romero, Ana, Moein, Mohammad Mahdi, Bolin, Martin, Siikanen, Jonathan, Grybäck, Pär, Larsson, Bengt, Halldin, Christer, Grime, Ken, Eriksson, Ulf G., and Farde, Lars
- Published
- 2020
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4. Pulmonary PET imaging confirms preferential lung target occupancy of an inhaled bronchodilator
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Schou, Magnus, Ewing, Pär, Cselenyi, Zsolt, Fridén, Markus, Takano, Akihiro, Halldin, Christer, and Farde, Lars
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- 2019
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5. A PET study in healthy subjects of brain exposure of 11C-labelled osimertinib – A drug intended for treatment of brain metastases in non-small cell lung cancer
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Varrone, Andrea, Varnäs, Katarina, Jucaite, Aurelija, Cselényi, Zsolt, Johnström, Peter, Schou, Magnus, Vazquez-Romero, Ana, Moein, Mohammad M, Halldin, Christer, Brown, Andrew P, Vishwanathan, Karthick, and Farde, Lars
- Published
- 2020
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6. Brain exposure of osimertinib in patients with epidermal growth factor receptor mutation non‐small cell lung cancer and brain metastases: A positron emission tomography and magnetic resonance imaging study
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Ekman, Simon, primary, Cselényi, Zsolt, additional, Varrone, Andrea, additional, Jucaite, Aurelija, additional, Martin, Heather, additional, Schou, Magnus, additional, Johnström, Peter, additional, Laus, Gianluca, additional, Lewensohn, Rolf, additional, Brown, Andrew P., additional, van der Aart, Jasper, additional, Vishwanathan, Karthick, additional, and Farde, Lars, additional
- Published
- 2023
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7. Potential for imaging the high-affinity state of the 5-HT1B receptor: a comparison of three PET radioligands with differing intrinsic activity
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Lindberg, Anton, Arakawa, Ryosuke, Nogami, Tsuyoshi, Nag, Sangram, Schou, Magnus, Elmore, Charles S., Farde, Lars, Pike, Victor W., and Halldin, Christer
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- 2019
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8. Proof of lung muscarinic receptor occupancy by tiotropium: Translational Positron Emission Tomography studies in non-human primates and humans
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Cselényi, Zsolt, primary, Jucaite, Aurelija, additional, Ewing, Pär, additional, Stenkrona, Per, additional, Kristensson, Cecilia, additional, Johnström, Peter, additional, Schou, Magnus, additional, Bolin, Martin, additional, Halldin, Christer, additional, Larsson, Bengt, additional, Grime, Ken, additional, Eriksson, Ulf G, additional, and Farde, Lars, additional
- Published
- 2023
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- View/download PDF
9. The development of a GPR44 targeting radioligand [11C]AZ12204657 for in vivo assessment of beta cell mass
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Jahan, Mahabuba, Johnström, Peter, Selvaraju, Ram K., Svedberg, Marie, Winzell, Maria Sörhede, Bernström, Jenny, Kingston, Lee, Schou, Magnus, Jia, Zhisheng, Skrtic, Stanko, Johansson, Lars, Korsgren, Olle, Farde, Lars, Halldin, Christer, and Eriksson, Olof
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- 2018
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10. Isotopic Radiolabeling of Crizotinib with Fluorine-18 for In Vivo Pet Imaging
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Sardana, Malvika, primary, Breuil, Louise, additional, Goutal, Sébastien, additional, Goislard, Maud, additional, Kondrashov, Mikhail, additional, Marchal, Etienne, additional, Besson, Florent L., additional, Dugave, Christophe, additional, Wrigley, Gail, additional, Jonson, Anna C., additional, Kuhnast, Bertrand, additional, Schou, Magnus, additional, Tournier, Nicolas, additional, Elmore, Charles S., additional, and Caillé, Fabien, additional
- Published
- 2022
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11. DDDR-01. AZD9574 IS A NOVEL, BRAIN PENETRANT PARP-1 SELECTIVE INHIBITOR WITH ACTIVITY IN AN INTRACRANIAL XENOGRAFT MODEL OF TRIPLE NEGATIVE BREAST CARCINOMA WITH HOMOLOGOUS RECOMBINATION REPAIR DEFICIENCY
- Author
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Jamal, Kunzah, primary, Staniszewska, Anna, additional, Gordon, Jacob, additional, Pilger, Domenic, additional, Illuzzi, Giuditta, additional, Wilson, Joanne, additional, Smith, Aaron, additional, Gosselin, Eric, additional, McWilliams, Lisa, additional, Wen, Shenghua, additional, McGrath, Frank, additional, Dowdell, Gregory, additional, Kabbabe, Dominic, additional, Griffin, Matthew, additional, Davies, Barry, additional, Hamerlik, Petra, additional, Schou, Magnus, additional, Pike, Andy, additional, and Johannes, Jeffrey, additional
- Published
- 2022
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12. Reactive Palladium–Ligand Complexes for 11 C-Carbonylation at Ambient Pressure: A Breakthrough in Carbon-11 Chemistry.
- Author
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Dahl, Kenneth, Lindberg, Anton, Vasdev, Neil, and Schou, Magnus
- Subjects
CARBONYLATION ,POSITRON emission tomography ,DRUG discovery ,CURRENT good manufacturing practices ,COLLEGE laboratories ,CARBONYL group - Abstract
The Pd–Xantphos-mediated
11 C-carbonylation protocol (also known as the "Xantphos- method"), due to its simplistic and convenient nature, has facilitated researchers in meeting a longstanding need for preparing11 C-carbonyl-labeled radiopharmaceuticals at ambient pressure for positron emission tomography (PET) imaging and drug discovery. This development could be viewed as a breakthrough in carbon-11 chemistry, as evidenced by the rapid global adoption of the method by the pharmaceutical industry and academic laboratories worldwide. The method has been fully automated for the good manufacturing practice (GMP)-compliant production of novel radiopharmaceuticals for human use, and it has been adapted for "in-loop" reactions and microwave technology; an impressive number of11 C-labeled compounds (>100) have been synthesized. Given the simplicity and efficiency of the method, as well as the abundance of carbonyl groups in bioactive drug molecules, we expect that this methodology will be even more widely adopted in future PET radiopharmaceutical research and drug development. [ABSTRACT FROM AUTHOR]- Published
- 2023
- Full Text
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13. 18th European Symposium on Radiopharmacy and Radiopharmaceuticals: Salzburg, Austria. 7-10 April 2016
- Author
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Radchenko, V., Engle, J. W., Roy, C., Griswold, J., Nortier, M. F., Birnbaum, E. R., Brugh, M., Mirzadeh, S., John, K. D., Fassbender, M. E., Zhai, Chuangyan, Franssen, Gerben M., Petrik, Milos, Laverman, Peter, Decristoforo, Clemens, Samia, Ait-Mohand, Véronique, Dumulon-Perreault, Brigitte, Guérin, Summer, D., Kroess, A., Rangger, C., Haas, H., Laverman, P., Gerben, F., von Guggenberg, E., Decristoforo, C., Bolzati, Cristina, Salvarese, Nicola, Refosco, Fiorenzo, Meléndez-Alafort, Laura, Carpanese, Debora, Rosato, Antonio, Saviano, Michele, Del Gatto, Annarita, Comegna, Daniela, Zaccaro, Laura, Billaud, Emilie, Ahamed, Muneer, Cleeren, Frederik, Shahbazali, Elnaz, Noël, Tim, Hessel, Volker, Verbruggen, Alfons, Bormans, Guy, Cleeren, F., Lecina, J., Koole, M., Verbruggen, A., Bormans, G., Lugatoa, B., Stucchia, S., Turollaa, E. A., Giulianoa, L., Toddea, S., Ferraboschib, P., Klok, R. P., Mooijer, M. P. J., Hendrikse, N. H., Windhorst, A. D., Collet, C., Petry, N., Chrétien, F., Karcher, G., Pellegrini-Moïse, N., Lamandé-Langle, S., Pfaff, Sarah, Philippe, Cecile, Mitterhauser, Markus, Hacker, Marcus, Wadsak, Wolfgang, Guérard, François, Lee, Yong-Sok, Gouard, Sébastien, Baidoo, Kwamena, Alliot, Cyrille, Chérel, Michel, Brechbiel, Martin W., Gestin, Jean-François, Lam, K., Chan, C., Reilly, R. M., Paillas, Salomé, Marshall, John, Pouget, Jean-Pierre, Sosabowski, Jane, Briard, Emmanuelle, Auberson, Yves P., Reilly, John, Healy, Mark, Sykes, David, Paulus, Andreas, Lichtenbelt, Wouter van Marken, Mottaghy, Felix, Bauwens, Matthias, Baranski, Ann-Christin, Schäfer, Martin, Bauder-Wüst, Ulrike, Haberkorn, Uwe, Eder, Matthias, Kopka, Klaus, Chaussard, M., Hosten, B., Vignal, N., Tsoupko-Sitnikov, V., Hernio, N., Hontonnou, F., Merlet, P., Poyet, J. L., Sarda-Mantel, L., Rizzo-Padoin, N., Cardinale, J., Schäfer, M., Benešová, M., Bauder-Wüst, U., Seibert, O., Giesel, F., Haberkorn, U., Eder, M., Kopka, K., Nematallah, Mansour, Michel, Paquette, Samia, Ait-Mohand, Véronique, Dumulon-Perreault, Roger, Lecomte, Brigitte, Guérin, Fernandez-Maza, L., Rivera-Marrero, S., Capote, A. Prats, Parrado-Gallego, A., Fernandez-Gomez, I., Balcerzyk, M., Sablon-Carrazana, M., Perera-Pintado, A., Merceron-Martinez, D., Acosta-Medina, E., Rodriguez-Tanty, C., Attili, Bala, Ahamed, Muneer, Bormans, Guy, Philippe, C., Zeilinger, M., Scherer, T., Fürnsinn, C., Dumanic, M., Wadsak, W., Hacker, M., Mitterhauser, M., Janssen, B., Vugts, D. J., Molenaar, G.T. T., Funke, U., Kruijer, P. S., Dollé, F., Bormans, G., Lammertsma, A. A., Windhorst, A. D., Vermeulen, Koen, Ahamed, Muneer, Schnekenburger, Michael, Froeyen, Mathy, Olberg, Dag Erlend, Diederich, Marc, Bormansa, Guy, Raaphorst, R. M., Luurtsema, G., Lammertsma, A. A., Elsinga, P. H., Windhorst, A D., Rotteveel, Lonneke, Funke, Uta, ten Dijke, Peter, Bogaard, Harm Jan, Lammertsma, Adriaan A., Windhorst, Albert D., Song, Lei, Able, Sarah, Falzone, Nadia, Kersemans, Veerle, Vallis, Katherine, Carta, Davide, Salvarese, Nicola, Sihver, Wiebke, Gao, Feng, Pietzsch, Hans Jürgen, Biondi, Barbara, Ruzza, Paolo, Refosco, Fiorenzo, Bolzati, Cristina, Haubner, Roland, Finkensted, Armin, Stegmair, Armin, Rangger, Christine, Decristoforo, Clemens, Zoller, Heinz, Virgolini, Irene J., Pooters, Ivo, Lotz, Maartje, Wierts, Roel, Mottaghy, Felix, Bauwens, Matthias, Forsback, Sarita, Jörgen, Bergman, Riikka, Kivelä, Karageorgou, M., Radović, M., Tsoukalas, C., Antic, B., Gazouli, M., Paravatou-Petsotas, M., Xanthopouls, S., Calamiotou, M., Stamopoulos, D., Vranješ-Durić, S., Bouziotis, P., Lunev, A. S., Larenkov, A. A., Petrosova, K. A., Klementyeva, O. E., Kodina, G. E., Kvernenes, O. H., Adamsen, T. C. H., Martin, René, Weidlich, Sebastian, Zerges, Anna-Maria, Gameiro, Cristiana, Lazarova, Neva, Müllera, Marco, Luurtsema, Gert, de Vries, Michèl, Ghyoot, Michel, van der Woude, Gina, Zijlma, Rolf, Dierckx, Rudi, Boersma, Hendrikus H., Elsinga, Philip H., Lambrecht, Fatma Yurt, Er, Ozge, Ince, Mine, Avci, Cıgır Biray, Gunduz, Cumhur, Sarı, Fatma Aslihan, Ocakoglu, Kasim, Er, Ozge, Ersoz, Onur Alp, Lambrecht, Fatma Yurt, Ince, Mine, Kayabasi, Cagla, Gunduz, Cumhur, Kniess, Torsten, Meister, Sebastian, Fischer, Steffen, Steinbach, Jörg, Ashfaq, Rabia, Iqbal, Saeed, ullah Khan, Irfan, Iglesias-Jerez, R., Martín-Banderas, L., Perera-Pintado, A., Borrego-Dorado, I., Farinha-Antunes, Ines, Kwizera, Chantal, Lacivita, Enza, Lucente, Ermelinda, Niso, Mauro, De Giorgio, Paola, Perrone, Roberto, Colabufo, Nicola A., Elsinga, Philip H., Leopoldo, Marcello, Vaulina, V. V., Fedorova, O. S., Orlovskaja, V. V., Chen, С. L., Li, G. Y., Meng, F. C., Liu, R. S., Wang, H. E., Krasikova, R. N., Meléndez-Alafort, Laura, Abozeid, Mohamed, Ferro-Flores, Guillermina, Negri, Anna, Bello, Michele, Uzunov, Nikolay, Paiusco, Martha, Esposito, Juan, Rosato, Antonio, Meléndez-Alafort, Laura, Bolzati, Cristina, Ferro-Flores, Guillermina, Salvarese, Nicola, Carpanese, Debora, Abozeid, Mohamed, Rosato, Antonio, Uzunov, Nikolay, Palmieri, L., Verbrugghen, T., Glassner, M., Hoogenboom, R., Staelens, S., Wyffels, L., Orlovskaja, V. V., Kuznetsova, O. F., Fedorova, O. S., Maleev, V. I., Belokon, Yu. N., Geolchanyan, A., Saghyan, A. S., Mu, L., Schibli, R., Ametamey, S. M., Krasikova, R. N., Revunov, Evgeny, Malmquist, Jonas, Johnström, Peter, Van Valkenburgh, Juno, Steele, Dalton, Halldin, Christer, Schou, Magnus, Osati, Samira, Paquette, Michel, Beaudoin, Simon, Ali, Hasrat, Guerin, Brigitte, Leyton, Jeffrey V., van Lier, Johan E., Di Iorio, V, Iori, M., Donati, C., Lanzetta, V., Capponi, P. C., Rubagotti, S., Dreger, T., Kunkel, F., Asti, M., Zhai, Chuangyan, Rangger, Christine, Summer, Dominik, Haas, Hubertus, Decristoforo, Clemens, Kijprayoon, Suphansa, Ruangma, Ananya, Ngokpol, Suthatip, Tuamputsha, Samart, Filp, Ulrike, Pees, Anna, Taddei, Carlotta, Pekošak, Aleksandra, Gee, Antony D., Poot, Alex J., Windhorst, Albert D., Gunay, Mine Silindir, Ozer, A. Yekta, Erdogan, Suna, Baysal, Ipek, Guilloteau, Denis, Chalon, Sylvie, Galli, Filippo, Artico, Marco, Taurone, Samanta, Bianchi, Enrica, Weintraub, Bruce D., Skudlinski, Mariusz, Signore, Alberto, Lepareur, Nicolas, Noiret, Nicolas, Hindré, François, Lacœuille, Franck, Benoist, Eric, Garin, Etienne, Trejo-Ballado, F., Zamora-Romo, E., Manrique-Arias, J. C., Gama-Romero, H M, Contreras-Castañon, G., Tecuapetla-Chantes, R. G., Avila-Rodriguez, M. A., Kvaternik, H., Hausberger, D., Zink, C., Rumpf, B., Aigner, R. M., Kvaternik, H., Hausberger, D., Rumpf, B., Aigner, R. M., Janković, Drina, Lakić, Mladen, Savić, Aleksandar, Ristić, Slavica, Nikolić, Nadežda, Vukadinović, Aleksandar, Sabo, Tibor J., Vranješ-Đurić, Sanja, Vranješ-Đurić, S., Radović, M., Janković, D., Nikolić, N., Goya, G. F., Calatayud, P., Spasojević, V., Antić, B., Goblet, David, Gameiro, Cristiana, Lazarova, Neva, Gameiro, Cristiana, Oxley, Ian, Abrunhosa, Antero, Kramer, Vasko, Vosjan, Maria, Spaans, Arnold, Vats, Kusum, Satpati, Drishty, Sarma, Haladhar D., Banerjee, Sharmila, Wojdowska, W., Pawlak, D. W., Parus, L. J., Garnuszek, P., Mikołajczak, R., Pijarowska-Kruszyna, J., Jaron, A., Kachniarz, A., Malkowski, B., Garnuszek, P., Mikolajczak, R., Ilem-Ozdemir, Derya, Caglayan-Orumlu, Oya, Asikoglu, Makbule, Ilem-Ozdemir, Derya, Caglayan-Orumlu, Oya, Asikoglu, Makbule, Eveliina, Arponen, Semi, Helin, Timo, Saarinen, Simo, Vauhkala, Esa, Kokkomäki, Pertti, Lehikoinen, De Simone, Mariarosaria, Pascali, Giancarlo, Carzoli, Ludovica, Quaglierini, Mauro, Telleschi, Mauro, Salvadori, Piero A., Lam, Phoebe, Aistleitner, Martina, Eichinger, Reinhard, Artner, Christoph, Nakka, Surendra, MC, Hemantha Kumara, Al-Qahtani, Mohammed, Al-Qahtani, Mohammed, Al-Malki, Yousif, Mambilima, N., Rubow, S. M., Berroterán-Infante, N., Hacker, M., Mitterhauser, M., Wadsak, W., Funke, Uta, Cleeren, Frederik, Lecina, Joan, Gallardo, Rodrigo, Verbruggen, Alfons M., Bormans, Guy, Ramos-Membrive, Rocío, Brotons, Ana, Quincoces, Gemma, Inchaurraga, Laura, de Redín, Inés Luis, Morán, Verónica, García-García, Berta, Irache, Juan Manuel, Peñuelas, Iván, Trabelsi, M., Cooper, M. S., Abella, Alejandra, Fuente, Teodomiro, Montellano, Antonio Jesús, Martínez, Teresa, Rabadan, Ruben, Meseguer-Olmo, Luis, Lehtiniemi, P., Yim, C., Mikkola, K., Nuutila, P., Solin, O., von Guggenberg, E., Rangger, C., Mair, C., Balogh, L., Pöstényi, Z., Pawlak, D., Mikołajczak, R., Socan, A., Peitl, P. Kolenc, Krošelj, M., Rangger, C., Decristoforo, C., Collet, C., Remy, S., Didier, R., Vergote, T., Karcher, G., Véran, N., Pawlak, D., Maurin, M., Garnuszek, P., Karczmarczyk, U., Mikołajczak, R., Fredericia, Pil, Severin, Gregory, Groesser, Torsten, Köster, Ulli, Jensen, Mikael, Leonte, R., Puicea, F. D., Raicu, A., Min, E. A., Serban, R., Manda, G., Niculae, D., Zerna, Marion, Schieferstein, Hanno, Müller, Andre, Berndt, Mathias, Yim, Cheng-Bin, Mikkola, Kirsi, Nuutila, Pirjo, Solin, Olof, Seifert, D., Ráliš, J., Lebeda, O., Selivanova, Svetlana V., Senta, Helena, Lavallée, Éric, Caouette, Lyne, Turcotte, Éric, Lecomte, Roger, Kochovska, Marina Zdraveska, Ivanovska, Emilija Janjevik, Jokic, Vesna Spasic, Ackova, Darinka Gjorgieva, Smilkov, Katarina, Makreski, Petre, Stafilov, Trajče, Janevik-Ivanovska, Emilija, Alemu, Aschalew, Muchira, Joel Munene, Wanjeh, David Mwanza, Janevik-Ivanovska, Emilija, Janevik-Ivanovska, Emilija, Zdravev, Zoran, Bhonsle, Uday, Alberto, Osso Júnior João, Duatti, Adriano, Angelovska, Bistra, Stojanovska, Zdenka, Sarafinovska, Zorica Arsova, Bosnakovski, Darko, Gorgieva-Ackova, Darinka, Smilkov, Katarina, Drakalska, Elena, Venkatesh, Meera, Gulaboski, Rubin, Colin, Didier J., Inkster, James A. H., Germain, Stéphane, Seimbille, Yann, Atiq-ur-Rehman, and Cayero-Otero
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- 2016
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14. Abstract 6302: Structure-based and property-based drug design of AZD9574, a CNS penetrant PARP1 selective inhibitor and trapper
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Ghosh, Avipsa, primary, Hande, Sudhir M., additional, Balazs, Amber, additional, Barratt, Derek, additional, Cosulich, Sabina, additional, Davies, Barry, additional, Degorce, Sébastien, additional, Embrey, Kevin, additional, Gill, Sonja, additional, Gunnarsson, Anders, additional, Illuzzi, Giuditta, additional, Johnström, Peter, additional, Lane, Jordan, additional, Larner, Carrie, additional, Lawrence, Rachel, additional, Leo, Elisabetta, additional, Madin, Andrew, additional, Martin, Elizabeth, additional, McWilliams, Lisa, additional, O’Connor, Lenka, additional, O’Connor, Mark, additional, Orme, Jonathan, additional, Pachl, Fiona, additional, Packer, Martin, additional, Pike, Andy, additional, Rawlins, Philip, additional, Schimpl, Marianne, additional, Schou, Magnus, additional, Staniszewska, Anna, additional, Yang, Wenzhan, additional, Yates, James, additional, Zhang, Andrew, additional, Zheng, XiaoLa, additional, Fawell, Stephen, additional, Hamerlik, Petra, additional, and Johannes, Jeffrey, additional
- Published
- 2022
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15. Abstract 5977: Discovery and preclinical validation of [11C]AZ3391: A first in class blood-brain barrier permeable, subtype selective PARP-1 PET radioligand
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Johnström, Peter, primary, Johannes, Jeffrey, additional, Pike, Andy, additional, Cselényi, Zsolt, additional, and Schou, Magnus, additional
- Published
- 2022
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16. Abstract 5076: Evaluation of the CNS penetration of a next generation PARP inhibitor, AZD9574, in cynomolgus monkey using positron emission tomography
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Pike, Andy, primary, Balazs, Amber, additional, Cselényi, Zsolt, additional, Degorce, Sébastien L., additional, Ghosh, Avipsa, additional, Hande, Sudhir M., additional, Johannes, Jeffrey, additional, Johnström, Peter, additional, Packer, Martin J., additional, Schou, Magnus, additional, and Zheng, XiaoLan, additional
- Published
- 2022
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17. Identification of positron emission tomography (PET) tracer candidates by prediction of the target-bound fraction in the brain
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Fridén, Markus, Wennerberg, Marie, Antonsson, Madeleine, Sandberg-Ställ, Maria, Farde, Lars, and Schou, Magnus
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- 2014
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18. Identification of PET radiometabolites by cytochrome P450, UHPLC/Q-ToF-MS and fast radio-LC: applied to the PET radioligands [11C]flumazenil, [18F]FE-PE2I, and [11C]PBR28
- Author
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Amini, Nahid, Nakao, Ryuji, Schou, Magnus, and Halldin, Christer
- Published
- 2013
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19. Multiple Applications of a Novel Biarsenical Imaging Probe in Fluorescence and PET Imaging of Melanoma
- Author
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Kondrashov, Mikhail, Svensson, Samuel, Strom, Peter, Westermark, Andreas, Jacobson-Ingemyr, Hanna, Takano, Akihiro, Tari, Lenke, Toth, Miklos, Cai, Minying, Hruby, Victor J., Schou, Magnus, Kondrashov, Mikhail, Svensson, Samuel, Strom, Peter, Westermark, Andreas, Jacobson-Ingemyr, Hanna, Takano, Akihiro, Tari, Lenke, Toth, Miklos, Cai, Minying, Hruby, Victor J., and Schou, Magnus
- Abstract
A new fluorescent biarsenical peptide labeling probe was synthesized and labeled with the radioactive isotopes C-11 and F-18. The utility of this probe was demonstrated by installing each of these isotopes into a melanocortin 1 receptor (MC1R) binding peptide, which targets melanoma tumors. Its applicability was further showcased by subsequent in vitro imaging in cells as well as in vivo imaging in melanoma xenograft mice by fluorescence and positron emission tomography., Funding Agencies|Knut och Alice Wallenbergs FoundationKnut & Alice Wallenberg Foundation [2018.0066]; NIHUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) - USA [GM108040]
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- 2021
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20. Additional file 1 of Quantification and reliability of [11C]VC - 002 binding to muscarinic acetylcholine receptors in the human lung — a test-retest PET study in control subjects
- Author
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Cselényi, Zsolt, Jucaite, Aurelija, Kristensson, Cecilia, Stenkrona, Per, Ewing, Pär, Varrone, Andrea, Johnström, Peter, Schou, Magnus, Vazquez-Romero, Ana, Moein, Mohammad Mahdi, Bolin, Martin, Siikanen, Jonathan, Grybäck, Pär, Larsson, Bengt, Halldin, Christer, Grime, Ken, Eriksson, Ulf G., and Farde, Lars
- Abstract
Additional file 1. Supplemental Material 1
- Published
- 2020
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21. Synthesis and Preclinical Evaluation of 6-[18F]Fluorine-α-methyl-l-tryptophan, a Novel PET Tracer for Measuring Tryptophan Uptake.
- Author
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Krasikova, Raisa, Kondrashov, Mikhail, Avagliano, Camilla, Petukhov, Mikhail, Vazquez-Romero, Ana, Revunov, Evgeny, Johnström, Peter, Tari, Lenke, Tóth, Miklós, Häggkvist, Jenny, Erhardt, Sophie, Cervenka, Simon, Schou, Magnus, Krasikova, Raisa, Kondrashov, Mikhail, Avagliano, Camilla, Petukhov, Mikhail, Vazquez-Romero, Ana, Revunov, Evgeny, Johnström, Peter, Tari, Lenke, Tóth, Miklós, Häggkvist, Jenny, Erhardt, Sophie, Cervenka, Simon, and Schou, Magnus
- Abstract
The positron emission tomography (PET) radioligand α-[11C]methyl-l-tryptophan ([11C]AMT) has been used to assess tryptophan metabolism in cancer, epilepsy, migraine, and autism. Despite its extensive application, the utility of this tracer is currently hampered by the short half-life of the radionuclide used for its labeling (11C, t1/2 = 20.4 min). We herein report the design, synthesis, radiolabeling, and initial in vivo evaluation of a fluorine-18 (18F, t 1/2 = 109.7 min) labeled analogue that is fluorinated in the 6-position of the aromatic ring ([18F]6-F-AMTr). In a head-to-head comparison between [18F]6-F-AMTr and [11C]AMT in mice using PET, peak brain radioactivity, regional brain distribution, and kinetic profiles were similar between the two tracers. [18F]6-F-AMTr was however not a substrate for IDO1 or TPH as determined in in vitro enzymatic assays. The brain uptake of the tracer is thus more likely related to LAT1 transport over the blood-brain barrier than metabolism along the serotonin or kynurenine pathways.
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- 2020
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22. Synthesis, Biodistribution, and Radiation Dosimetry of a Novel mGluR5 Radioligand : F-18-AZD9272
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Nag, Sangram, Varnäs, Katarina, Arakawa, Ryosuke, Jahan, Mahabuba, Schou, Magnus, Farde, Lars, Halldin, Christer, Nag, Sangram, Varnäs, Katarina, Arakawa, Ryosuke, Jahan, Mahabuba, Schou, Magnus, Farde, Lars, and Halldin, Christer
- Abstract
The metabotropic glutamate receptor subtype mGluR5 has been proposed as a potential drug target for CNS disorders such as anxiety, depression, Parkinson's disease, and epilepsy. The AstraZeneca compound AZD9272 has previously been labeled with carbon-11 and used as a PET radioligand for mGluR5 receptor binding. The molecular structure of AZD9272 allows one to label the molecule with fluorine-18 without altering the structure. The aim of this study was to develop a fluorine-18 analogue of AZD9272 and to examine its binding distribution in the nonhuman primate brain in vivo as well as to obtain whole body radiation dosimetry. F-18-AZD9272 was successfully synthesized from a nitro precursor. The radioligand was stable, with a radiochemical purity of >99% at 2 h after formulation in a sterile phosphate buffered solution (pH = 7.4). After injection of F-18-AZD9272 in two cynomolgus monkeys, the maximum whole brain radioactivity concentration was 4.9-6.7% of the injected dose (n = 2) and PET images showed a pattern of regional radioactivity consistent with that previously obtained for C-11-AZD9272. The percentage of parent radioligand in plasma was 59 and 64% (n = 2) at 120 min after injection of F-18-AZD9272, consistent with high metabolic stability. Two whole body PET scans were performed in nonhuman primates for a total of 231 min after injection of F-18-AZD9272. Highest uptakes were seen in liver and small intestine, followed by brain and kidney. The estimated effective dose was around 0.017 mSv/MBq. F-18-AZD9272 shows suitable properties as a PET radioligand for in vivo imaging of binding in the primate brain. F-18-labeled AZD9272 offers advantages over C-11-AZD9272 in terms of higher image resolution, combined with a longer half-life. Moreover, based on the distribution and the estimated radiation burden, imaging of F-18-AZD9272 could be used as an improved tool for quantitative assessment and characterization of AZD9272 binding sites in the human brain by using
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- 2020
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23. Preclinical Comparison of the Blood–brain barrier Permeability of Osimertinib with Other EGFR TKIs
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Colclough, Nicola, primary, Chen, Kan, additional, Johnström, Peter, additional, Strittmatter, Nicole, additional, Yan, Yumei, additional, Wrigley, Gail L., additional, Schou, Magnus, additional, Goodwin, Richard, additional, Varnäs, Katarina, additional, Adua, Sally J., additional, Zhao, Minghui, additional, Nguyen, Don X., additional, Maglennon, Gareth, additional, Barton, Peter, additional, Atkinson, James, additional, Zhang, Lin, additional, Janefeldt, Annika, additional, Wilson, Joanne, additional, Smith, Aaron, additional, Takano, Akihiro, additional, Arakawa, Ryosuke, additional, Kondrashov, Mikhail, additional, Malmquist, Jonas, additional, Revunov, Evgeny, additional, Vazquez-Romero, Ana, additional, Moein, Mohammad Mahdi, additional, Windhorst, Albert D., additional, Karp, Natasha A., additional, Finlay, M. Raymond V., additional, Ward, Richard A., additional, Yates, James W.T., additional, Smith, Paul D., additional, Farde, Lars, additional, Cheng, Zack, additional, and Cross, Darren A.E., additional
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- 2021
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24. Brain exposure of the ATM inhibitor AZD1390 in humans—a positron emission tomography study
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Jucaite, Aurelija, primary, Stenkrona, Per, additional, Cselényi, Zsolt, additional, De Vita, Serena, additional, Buil-Bruna, Nuria, additional, Varnäs, Katarina, additional, Savage, Alicia, additional, Varrone, Andrea, additional, Johnström, Peter, additional, Schou, Magnus, additional, Davison, Chris, additional, Sykes, Andy, additional, Pilla Reddy, Venkatesh, additional, Hoch, Matthias, additional, Vazquez-Romero, Ana, additional, Moein, Mohammad Mahdi, additional, Halldin, Christer, additional, Merchant, Melinda S, additional, Pass, Martin, additional, and Farde, Lars, additional
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- 2020
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25. Rapid and efficient synthesis of ¹¹C-labeled benzimidazolones using [¹¹C]carbon dioxide
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Horkka, Kaisa, Dahl, Kenneth, Bergare, Jonas, Elmore, Charles S., Halldin, Christer, and Schou, Magnus
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positron emission tomography ,benzimidazolones ,carbon dioxide ,radiochemistry ,isotopic labeling - Abstract
[11C]Carbon dioxide is an attractive synthon for the labeling of positron emission tomography (PET) tracers for subsequent use in biomedical research and drug development. In this study, [11C]CO2was used for direct11C‐labeling of a set of cyclic aromatic ureas starting from their correspondingortho‐phenylenediamines, BEMP (2‐tert‐butylimino‐2‐diethylamino‐1,3‐dimethylperhydro‐1,3,2‐diazaphosphorine) as fixation base, and Mitsunobu reagents (DBAD,nBu3P) for the intramolecular cyclization. The procedure is rapid (6 minutes total synthesis time), mild (proceeds at room temperature) and provided a set of11C‐benzimidazolones in good to excellent radiochemical yields. As a final testament to the utility of this method, the beta‐adrenoceptor PET ligand [11C]CGP12177, was successfully prepared using the optimized conditions.
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- 2019
26. Additional file 1: of Pulmonary PET imaging confirms preferential lung target occupancy of an inhaled bronchodilator
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Schou, Magnus, Ewing, Pär, Cselenyi, Zsolt, Fridén, Markus, Takano, Akihiro, Halldin, Christer, and Farde, Lars
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Figure S1. Time-course for radioactivity in plasma following intravenous injection of [11C]VC-002. Average radioactivity concentrations across all NHPs examined at baseline (n = 9) and after pre-treatment via intravenous infusion (n = 4) or inhalation (n = 5) of ipratropium. Figure S2. The fraction of radioactivity corresponding to parent radioligand in plasma following intravenous injection of [11C]VC-002. Average radioactivity concentrations across all NHPs examined at baseline (n = 9) and after pre-treatment via intravenous infusion (n = 4) or inhalation of ipratropium (n = 5). Figure S3. The relationship between receptor occupancy in the lungs and pituitary at given plasma concentrations. Note the shift towards higher occupancy in pituitary gland after intravenous administration. Figure S5. PET images from each experimental session. Figure S6. Time-course for radioactivity in venous and arterial blood following intravenous injection of [11C]VC-002. (DOCX 1861 kb)
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- 2019
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27. Visible-Light-Enabled Aminocarbonylation of Unactivated Alkyl Iodides with Stoichiometric Carbon Monoxide for Application on Late-Stage Carbon Isotope Labeling
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Sardana, Malvika, primary, Bergman, Joakim, additional, Ericsson, Cecilia, additional, Kingston, Lee P., additional, Schou, Magnus, additional, Dugave, Christophe, additional, Audisio, Davide, additional, and Elmore, Charles S., additional
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- 2019
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28. A PET study in healthy subjects of brain exposure of 11C-labelled osimertinib – A drug intended for treatment of brain metastases in non-small cell lung cancer
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Varrone, Andrea, primary, Varnäs, Katarina, additional, Jucaite, Aurelija, additional, Cselényi, Zsolt, additional, Johnström, Peter, additional, Schou, Magnus, additional, Vazquez-Romero, Ana, additional, Moein, Mohammad M, additional, Halldin, Christer, additional, Brown, Andrew P, additional, Vishwanathan, Karthick, additional, and Farde, Lars, additional
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- 2019
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29. Brain exposure of the ATM inhibitor AZD1390 in humans—a positron emission tomography study.
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Jucaite, Aurelija, Stenkrona, Per, Cselényi, Zsolt, Vita, Serena De, Buil-Bruna, Nuria, Varnäs, Katarina, Savage, Alicia, Varrone, Andrea, Johnström, Peter, Schou, Magnus, Davison, Chris, Sykes, Andy, Reddy, Venkatesh Pilla, Hoch, Matthias, Vazquez-Romero, Ana, Moein, Mohammad Mahdi, Halldin, Christer, Merchant, Melinda S, Pass, Martin, and Farde, Lars
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- 2021
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30. [18F]fluoro-benziodoxole : a no-carrier-added electrophilic fluorinating reagent. Rapid, simple radiosynthesis, purification and application for fluorine-18 labelling
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Gonzalez, Miguel A. Cortes, Nordeman, Patrik, Gomez, Antonio Bermejo, Meyer, Denise N., Antoni, Gunnar, Schou, Magnus, Szabo, Kalman J., Gonzalez, Miguel A. Cortes, Nordeman, Patrik, Gomez, Antonio Bermejo, Meyer, Denise N., Antoni, Gunnar, Schou, Magnus, and Szabo, Kalman J.
- Abstract
Operationally simple radiosynthesis and purification of [F-18]fluoro-benziodoxole was developed starting from a cyclotron produced [F-18]F- precursor, [F-18]TBAF, and tosyl-benziodoxole. The synthetic utility of [F-18]fluoro-benziodoxole was demonstrated by electrophilic fluorocyclization of o-styrilamides proceeding with high RCC (typically 50-90%) and high molar activity (up to 396 GBq mol(-1)).
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- 2018
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31. Increased Brain Exposure of an Alpha-Synuclein Fibrillization Modulator by Utilization of an Activated Ester Prodrug Strategy
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Cairns, Andrew G., Vazquez-Romero, Ana, Mahdi-Moein, Mohammad, Ådén, Jörgen, Elmore, Charles S., Takano, Akihiro, Arakawa, Ryosuke, Varrone, Andrea, Almqvist, Fredrik, Schou, Magnus, Cairns, Andrew G., Vazquez-Romero, Ana, Mahdi-Moein, Mohammad, Ådén, Jörgen, Elmore, Charles S., Takano, Akihiro, Arakawa, Ryosuke, Varrone, Andrea, Almqvist, Fredrik, and Schou, Magnus
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Previous work in our laboratories has identified a series of peptidomimetic 2-pyridone molecules as modulators of alpha-synuclein (α-syn) fibrillization in vitro. As a first step toward developing molecules from this scaffold as positron emission tomography imaging agents, we were interested in evaluating their blood-brain barrier permeability in nonhuman primates (NHP) in vivo. For this purpose, 2-pyridone 12 was prepared and found to accelerate α-syn fibrillization in vitro. Acid 12, and its acetoxymethyl ester analogue 14, were then radiolabeled with 11C (t1/2 = 20.4 min) at high radiochemical purity (>99%) and high specific radioactivity (>37 GBq/μmol). Following intravenous injection of each compound in NHP, a 4-fold higher radioactivity in brain was observed for [11C]14 compared to [11C]12 (0.8 vs 0.2 SUV, respectively). [11C]14 was rapidly eliminated from plasma, with [11C]12 as the major metabolic product observed by radio-HPLC. The presented prodrug approach paves the way for future development of 2-pyridones as imaging biomarkers for in vivo imaging of α-synuclein deposits in brain.
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- 2018
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32. [F-18]fluoro-benziodoxole : a no-carrier-added electrophilic fluorinating reagent. Rapid, simple radiosynthesis, purification and application for fluorine-18 labelling
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Cortés González, Miguel A., Nordeman, Patrik, Bermejo Gómez, Antonio, Meyer, Denise N., Antoni, Gunnar, Schou, Magnus, Szabó, Kálmán J., Cortés González, Miguel A., Nordeman, Patrik, Bermejo Gómez, Antonio, Meyer, Denise N., Antoni, Gunnar, Schou, Magnus, and Szabó, Kálmán J.
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Operationally simple radiosynthesis and purification of [F-18]fluoro-benziodoxole was developed starting from a cyclotron produced [F-18]F- precursor, [F-18]TBAF, and tosyl-benziodoxole. The synthetic utility of [F-18]fluoro-benziodoxole was demonstrated by electrophilic fluorocyclization of o-styrilamides proceeding with high RCC (typically 50-90%) and high molar activity (up to 396 GBq mol(-1)).
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- 2018
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33. A PET study in healthy subjects of brain exposure of 11 C-labelled osimertinib – A drug intended for treatment of brain metastases in non-small cell lung cancer.
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Varrone, Andrea, Varnäs, Katarina, Jucaite, Aurelija, Cselényi, Zsolt, Johnström, Peter, Schou, Magnus, Vazquez-Romero, Ana, Moein, Mohammad M, Halldin, Christer, Brown, Andrew P, Vishwanathan, Karthick, and Farde, Lars
- Abstract
Osimertinib is a tyrosine kinase inhibitor (TKI) of the mutated epidermal growth factor receptor (EGFRm) with observed efficacy in patients with brain metastases. Brain exposure and drug distribution in tumor regions are important criteria for evaluation and confirmation of CNS efficacy. The aim of this PET study was therefore to determine brain distribution and exposure of
11 C-labelled osimertinib administered intravenously in subjects with an intact blood–brain barrier. Eight male healthy subjects (age 52 ± 8 years) underwent one PET measurement with11 C-osimertinib. The pharmacokinetic parameters Cmax (brain) (standardized uptake value), Tmax (brain) and AUC0–90 min brain/blood ratio were calculated. The outcome measure for11 C-osimertinib brain exposure was the total distribution volume (VT ).11 C-osimertinib distributed rapidly to the brain, with higher uptake in grey than in white matter. Mean Cmax , Tmax and AUC0–90 min brain/blood ratio were 1.5 (range 1–1.8), 13 min (range 5–30 min), and 3.8 (range 3.3–4.1). Whole brain and white matter VT were 14 mL×cm−3 (range 11–18) and 7 mL×cm−3 (range 5–12). This study in healthy volunteers shows that11 C-osimertinib penetrates the intact blood–brain barrier. The approach used further illustrates the role of molecular imaging in facilitating the development of novel drugs for the treatment of malignancies affecting the brain. [ABSTRACT FROM AUTHOR]- Published
- 2020
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34. Abstract CT013: Osimertinib displays high brain exposure in healthy subjects with intact blood-brain barrier: a microdose positron emission tomography (PET) study with 11C-labelled osimertinib
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Vishwanathan, Karthick, primary, Varrone, Andrea, additional, Varnas, Katarina, additional, Jucaite, Aurelija, additional, Cselenyi, Zsolt, additional, Johnstrom, Peter, additional, Schou, Magnus, additional, Vasquez-Romero, Ana, additional, Moein, Mohammed Mahdi, additional, Halldin, Christer, additional, Brown, Andrew P., additional, and Farde, Lars, additional
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- 2018
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35. Synthesis of trifluoromethyl moieties by late-stage copper (I) mediated nucleophilic fluorination
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Bermejo Gómez, Antonio, Cortés González, Miguel A., Lübcke, Marvin, Johansson, Magnus J., Schou, Magnus, Szabó, Kálmán J., Bermejo Gómez, Antonio, Cortés González, Miguel A., Lübcke, Marvin, Johansson, Magnus J., Schou, Magnus, and Szabó, Kálmán J.
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The nucleophilic fluorination of bromodifluoromethyl derivatives mediated by the complex (PPh3)(3)CuF is described. Under the reaction conditions, different trifluoroacetates, trifluorolcetones, trifluoroarenes and trifluoroacetamides were obtained in good yields.
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- 2017
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36. 18Th European Symposium On Radiopharmacy And Radiopharmaceuticals
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Radchenko, V., Engle, J. W., Roy, C., Griswold, J., Nortier, M. F., Birnbaum, E. R., Brugh, M., Mirzadeh, S., John, K. D., Fassbender, M. E., Zhai, Chuangyan, Franssen, Gerben M., Petrik, Milos, Laverman, Peter, Decristoforo, Clemens, Samia, Ait-Mohand, Véronique, Dumulon-Perreault, Brigitte, Guérin, Summer, D., Kroess, A., Rangger, C., Haas, H., Laverman, P., Gerben, F., von Guggenberg, E., Decristoforo, C., Bolzati, Cristina, Salvarese, Nicola, Refosco, Fiorenzo, Meléndez-Alafort, Laura, Carpanese, Debora, Rosato, Antonio, Saviano, Michele, Del Gatto, Annarita, Comegna, Daniela, Zaccaro, Laura, Billaud, Emilie, Ahamed, Muneer, Cleeren, Frederik, Shahbazali, Elnaz, Noël, Tim, Hessel, Volker, Verbruggen, Alfons, Bormans, Guy, Cleeren, F., Lecina, J., Koole, M., Verbruggen, A., Bormans, G., Lugatoa, B., Stucchia, S., Turollaa, E. A., Giulianoa, L., Toddea, S., Ferraboschib, P., Klok, R. P., Mooijer, M. P. J., Hendrikse, N. H., Windhorst, A. D., Collet, C., Petry, N., Chrétien, F., Karcher, G., Pellegrini-Moïse, N., Lamandé-Langle, S., Pfaff, Sarah, Philippe, Cecile, Mitterhauser, Markus, Hacker, Marcus, Wadsak, Wolfgang, Guérard, François, Lee, Yong-Sok, Gouard, Sébastien, Baidoo, Kwamena, Alliot, Cyrille, Chérel, Michel, Brechbiel, Martin W., Gestin, Jean-François, Lam, K., Chan, C., Reilly, R. M., Paillas, Salomé, Marshall, John, Pouget, Jean-Pierre, Sosabowski, Jane, Briard, Emmanuelle, Auberson, Yves P., Reilly, John, Healy, Mark, Sykes, David, Paulus, Andreas, Lichtenbelt, Wouter van Marken, Mottaghy, Felix, Bauwens, Matthias, Baranski, Ann-Christin, Schäfer, Martin, Bauder-Wüst, Ulrike, Haberkorn, Uwe, Eder, Matthias, Kopka, Klaus, Chaussard, M., Hosten, B., Vignal, N., Tsoupko-Sitnikov, V., Hernio, N., Hontonnou, F., Merlet, P., Poyet, J. L., Sarda-Mantel, L., Rizzo-Padoin, N., Cardinale, J., Schäfer, M., Benešová, M., Bauder-Wüst, U., Seibert, O., Giesel, F., Haberkorn, U., Eder, M., Kopka, K., Nematallah, Mansour, Michel, Paquette, Roger, Lecomte, Fernandez-Maza, L., Rivera-Marrero, S., Capote, A. Prats, Parrado-Gallego, A., Fernandez-Gomez, I., Balcerzyk, M., Sablon-Carrazana, M., Perera-Pintado, A., Merceron-Martinez, D., Acosta-Medina, E., Rodriguez-Tanty, C., Attili, Bala, Philippe, C., Zeilinger, M., Scherer, T., Fürnsinn, C., Dumanic, M., Wadsak, W., Hacker, M., Mitterhauser, M., Janssen, B., Vugts, D. J., Molenaar, G.T. T., Funke, U., Kruijer, P. S., Dollé, F., Lammertsma, A. A., Vermeulen, Koen, Schnekenburger, Michael, Froeyen, Mathy, Olberg, Dag Erlend, Diederich, Marc, Bormansa, Guy, Raaphorst, R. M., Luurtsema, G., Elsinga, P. H., Windhorst, A D., Rotteveel, Lonneke, Funke, Uta, ten Dijke, Peter, Bogaard, Harm Jan, Lammertsma, Adriaan A., Windhorst, Albert D., Song, Lei, Able, Sarah, Falzone, Nadia, Kersemans, Veerle, Vallis, Katherine, Carta, Davide, Sihver, Wiebke, Gao, Feng, Pietzsch, Hans Jürgen, Biondi, Barbara, Ruzza, Paolo, Haubner, Roland, Finkensted, Armin, Stegmair, Armin, Rangger, Christine, Zoller, Heinz, Virgolini, Irene J., Pooters, Ivo, Lotz, Maartje, Wierts, Roel, Forsback, Sarita, Jörgen, Bergman, Riikka, Kivelä, Karageorgou, M., Radović, M., Tsoukalas, C., Antic, B., Gazouli, M., Paravatou-Petsotas, M., Xanthopouls, S., Calamiotou, M., Stamopoulos, D., Vranješ-Durić, S., Bouziotis, P., Lunev, A. S., Larenkov, A. A., Petrosova, K. A., Klementyeva, O. E., Kodina, G. E., Kvernenes, O. H., Adamsen, T. C. H., Martin, René, Weidlich, Sebastian, Zerges, Anna-Maria, Gameiro, Cristiana, Lazarova, Neva, Müllera, Marco, Luurtsema, Gert, de Vries, Michèl, Ghyoot, Michel, van der Woude, Gina, Zijlma, Rolf, Dierckx, Rudi, Boersma, Hendrikus H., Elsinga, Philip H., Lambrecht, Fatma Yurt, Er, Ozge, Ince, Mine, Avci, Cıgır Biray, Gunduz, Cumhur, Sarı, Fatma Aslihan, Ocakoglu, Kasim, Ersoz, Onur Alp, Kayabasi, Cagla, Kniess, Torsten, Meister, Sebastian, Fischer, Steffen, Steinbach, Jörg, Ashfaq, Rabia, Iqbal, Saeed, ullah Khan, Irfan, Iglesias-Jerez, R., Martín-Banderas, L., Borrego-Dorado, I., Farinha-Antunes, Ines, Kwizera, Chantal, Lacivita, Enza, Lucente, Ermelinda, Niso, Mauro, De Giorgio, Paola, Perrone, Roberto, Colabufo, Nicola A., Leopoldo, Marcello, Vaulina, V. V., Fedorova, O. S., Orlovskaja, V. V., Chen, С. L., Li, G. Y., Meng, F. C., Liu, R. S., Wang, H. E., Krasikova, R. N., Abozeid, Mohamed, Ferro-Flores, Guillermina, Negri, Anna, Bello, Michele, Uzunov, Nikolay, Paiusco, Martha, Esposito, Juan, Palmieri, L., Verbrugghen, T., Glassner, M., Hoogenboom, R., Staelens, S., Wyffels, L., Kuznetsova, O. F., Maleev, V. I., Belokon, Yu. N., Geolchanyan, A., Saghyan, A. S., Mu, L., Schibli, R., Ametamey, S. M., Revunov, Evgeny, Malmquist, Jonas, Johnström, Peter, Van Valkenburgh, Juno, Steele, Dalton, Halldin, Christer, Schou, Magnus, Osati, Samira, Paquette, Michel, Beaudoin, Simon, Ali, Hasrat, Guerin, Brigitte, Leyton, Jeffrey V., van Lier, Johan E., Di Iorio, V, Iori, M., Donati, C., Lanzetta, V., Capponi, P. C., Rubagotti, S., Dreger, T., Kunkel, F., Asti, M., Summer, Dominik, Haas, Hubertus, Kijprayoon, Suphansa, Ruangma, Ananya, Ngokpol, Suthatip, Tuamputsha, Samart, Filp, Ulrike, Pees, Anna, Taddei, Carlotta, Pekošak, Aleksandra, Gee, Antony D., Poot, Alex J., Gunay, Mine Silindir, Ozer, A. Yekta, Erdogan, Suna, Baysal, Ipek, Guilloteau, Denis, Chalon, Sylvie, Galli, Filippo, Artico, Marco, Taurone, Samanta, Bianchi, Enrica, Weintraub, Bruce D., Skudlinski, Mariusz, Signore, Alberto, Lepareur, Nicolas, Noiret, Nicolas, Hindré, François, Lacœuille, Franck, Benoist, Eric, Garin, Etienne, Trejo-Ballado, F., Zamora-Romo, E., Manrique-Arias, J. C., Gama-Romero, H M, Contreras-Castañon, G., Tecuapetla-Chantes, R. G., Avila-Rodriguez, M. A., Kvaternik, H., Hausberger, D., Zink, C., Rumpf, B., Aigner, R. M., Janković, Drina, Lakić, Mladen, Savić, Aleksandar, Ristić, Slavica, Nikolić, Nadežda, Vukadinović, Aleksandar, Sabo, Tibor J., Vranješ-Đurić, Sanja, Vranješ-Đurić, S., Janković, D., Nikolić, N., Goya, G. F., Calatayud, P., Spasojević, V., Antić, B., Goblet, David, Oxley, Ian, Abrunhosa, Antero, Kramer, Vasko, Vosjan, Maria, Spaans, Arnold, Vats, Kusum, Satpati, Drishty, Sarma, Haladhar D., Banerjee, Sharmila, Wojdowska, W., Pawlak, D. W., Parus, L. J., Garnuszek, P., Mikołajczak, R., Pijarowska-Kruszyna, J., Jaron, A., Kachniarz, A., Malkowski, B., Mikolajczak, R., Ilem-Ozdemir, Derya, Caglayan-Orumlu, Oya, Asikoglu, Makbule, Eveliina, Arponen, Semi, Helin, Timo, Saarinen, Simo, Vauhkala, Esa, Kokkomäki, Pertti, Lehikoinen, De Simone, Mariarosaria, Pascali, Giancarlo, Carzoli, Ludovica, Quaglierini, Mauro, Telleschi, Mauro, Salvadori, Piero A., Lam, Phoebe, Aistleitner, Martina, Eichinger, Reinhard, Artner, Christoph, Nakka, Surendra, MC, Hemantha Kumara, Al-Qahtani, Mohammed, Al-Malki, Yousif, Mambilima, N., Rubow, S. M., Berroterán-Infante, N., Lecina, Joan, Gallardo, Rodrigo, Verbruggen, Alfons M., Ramos-Membrive, Rocío, Brotons, Ana, Quincoces, Gemma, Inchaurraga, Laura, de Redín, Inés Luis, Morán, Verónica, García-García, Berta, Irache, Juan Manuel, Peñuelas, Iván, Trabelsi, M., Cooper, M. S., Abella, Alejandra, Fuente, Teodomiro, Montellano, Antonio Jesús, Martínez, Teresa, Rabadan, Ruben, Meseguer-Olmo, Luis, Lehtiniemi, P., Yim, C., Mikkola, K., Nuutila, P., Solin, O., Mair, C., Balogh, L., Pöstényi, Z., Pawlak, D., Socan, A., Peitl, P. Kolenc, Krošelj, M., Remy, S., Didier, R., Vergote, T., Véran, N., Maurin, M., Karczmarczyk, U., Fredericia, Pil, Severin, Gregory, Groesser, Torsten, Köster, Ulli, Jensen, Mikael, Leonte, R., Puicea, F. D., Raicu, A., Min, E. A., Serban, R., Manda, G., Niculae, D., Zerna, Marion, Schieferstein, Hanno, Müller, Andre, Berndt, Mathias, Yim, Cheng-Bin, Mikkola, Kirsi, Nuutila, Pirjo, Solin, Olof, Seifert, D., Ráliš, J., Lebeda, O., Selivanova, Svetlana V., Senta, Helena, Lavallée, Éric, Caouette, Lyne, Turcotte, Éric, Lecomte, Roger, Kochovska, Marina Zdraveska, Ivanovska, Emilija Janjevik, Jokic, Vesna Spasic, Ackova, Darinka Gjorgieva, Smilkov, Katarina, Makreski, Petre, Stafilov, Trajče, Janevik-Ivanovska, Emilija, Alemu, Aschalew, Muchira, Joel Munene, Wanjeh, David Mwanza, Zdravev, Zoran, Bhonsle, Uday, Alberto, Osso Júnior João, Duatti, Adriano, Angelovska, Bistra, Stojanovska, Zdenka, Sarafinovska, Zorica Arsova, Bosnakovski, Darko, Gorgieva-Ackova, Darinka, Drakalska, Elena, Venkatesh, Meera, Gulaboski, Rubin, Colin, Didier J., Inkster, James A. H., Germain, Stéphane, Seimbille, Yann, and Radyofarmasi
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Meeting Abstracts - Abstract
OP03 Selective extraction of medically-related radionuclides from proton-irradiated thorium targets, V. Radchenko, J.W. Engle, C. Roy, J. Griswold, M.F. Nortier, E.R. Birnbaum, M. Brugh, S. Mirzadeh, K. D. John, M.E. Fassbender, OP04 Comparison of [68Ga]FSC(succ-RGD)3 and [68Ga]NODAGA-RGD for PET imaging of αvβ3 integrin expression, Chuangyan Zhai, Gerben M. Franssen, Milos Petrik, Peter Laverman, Clemens Decristoforo, OP05 A new NPY-Y1R targeting peptide for breast cancer PET imaging, Ait-Mohand Samia, Dumulon-Perreault Véronique, Guérin Brigitte, OP06 The influence of multivalency on CCK 2 receptor targeting, D. Summer, A. Kroess, C. Rangger, H. Haas, P. Laverman, F. Gerben, E. von Guggenberg, C.Decristoforo, OP07 SPECT Imaging of αvβ3 Expression by [99mTc(N)PNP43]- Bifunctional Chimeric RGD Peptide not Cross-Reacting with αvβ5, Cristina Bolzati, Nicola Salvarese, Fiorenzo Refosco, Laura Meléndez-Alafort, Debora Carpanese, Antonio Rosato, Michele Saviano, Annarita Del Gatto, Daniela Comegna, Laura Zaccaro, OP09 New dienophiles for the inverse-electron-demand Diels-Alder reaction and for pretargeted PET imaging, Emilie Billaud, Muneer Ahamed, Frederik Cleeren, Elnaz Shahbazali, Tim Noël, Volker Hessel, Alfons Verbruggen and Guy Bormans, OP10 New complexing agent for Al18F-labelling of heat-sensitive biomolecules: Synthesis and preclinical evaluation of Al18F-RESCA1-HAS, Cleeren F, Lecina J, Koole M, Verbruggen A and Bormans G, OP11 A novel versatile precursor efficient for F-18 radiolabelling via click-chemistry, B. Lugatoa, S. Stucchia, E.A. Turollaa, L. Giulianoa, S.Toddea, P. Ferraboschib, OP12 A general applicable method to quantify unidentified UV impurities in radiopharmaceuticals, R.P. Klok, M.P.J. Mooijer, N.H. Hendrikse, A.D. Windhorst, OP13 Development of [18F]Fluoro-C-glycosides to radiolabel peptides, Collet C., Petry N., Chrétien F., Karcher G., Pellegrini-Moïse N., Lamandé-Langle S., OP14 A Microfluidic Approach for the 68Ga-labeling of PSMAHBED-CC and NODAGA-RGD, Sarah Pfaff, Cecile Philippe, Markus Mitterhauser, Marcus Hacker, Wolfgang Wadsak, OP16 Surprising reactivity of astatine in the nucleophilic substitution of aryliodonium salts: application to the radiolabeling of antibodies, François Guérard, Yong-Sok Lee, Sébastien Gouard, Kwamena Baidoo, Cyrille Alliot, Michel Chérel, Martin W. Brechbiel, Jean-François Gestin, OP17 64Cu-NOTA-pertuzumab F(ab')2 fragments, a second-generation probe for PET imaging of the response of HER2-positive breast cancer to trastuzumab (Herceptin), Lam K, Chan C, Reilly RM, OP18 Development of radiohalogenated analogues of a avb6-specific peptide for high LET particle emitter targeted radionuclide therapy of cancer, Salomé Paillas, John Marshall, Jean-Pierre Pouget, Jane Sosabowski, OP19 Ligand Specific Efficiency (LSE) as a guide in tracer optimization, Emmanuelle Briard, Yves P. Auberson, John Reilly, Mark Healy, David Sykes, OP23 The radiosynthesis of an 18F-labeled triglyceride, developed to visualize and quantify brown adipose tissue activity, Andreas Paulus, Wouter van Marken Lichtenbelt,Felix Mottaghy, Matthias Bauwens, OP24 Influence of the fluorescent dye on the tumor targeting properties of dual-labeled HBED-CC based PSMA inhibitors, Baranski, Ann-Christin, Schäfer, Martin, Bauder-Wüst, Ulrike, Haberkorn, Uwe, Eder, Matthias, Kopka, Klaus, OP25 [18F]MEL050 as a melanin PET tracer : fully automated radiosynthesis and evaluation for the detection of pigmented melanoma in mice pulmonary metastases, Chaussard M, Hosten B, Vignal N, Tsoupko-Sitnikov V, Hernio N, Hontonnou F, Merlet P, Poyet JL, Sarda-Mantel L, Rizzo-Padoin N, OP26 Design and Preclinical Evaluation of Novel Radiofluorinated PSMA Targeting Ligands Based on PSMA-617, J. Cardinale, M. Schäfer, M. Benešová, U. Bauder-Wüst, O. Seibert, F. Giesel, U. Haberkorn, M. Eder, K. Kopka, OP27 A novel radiolabeled peptide for PET imaging of prostate cancer: 64Cu-DOTHA2-PEG-RM26, Mansour Nematallah, Paquette Michel, Ait-Mohand Samia, Dumulon-Perreault Véronique, Lecomte Roger, Guérin Brigitte, OP29 Biodistribution of [18F]Amylovis®, a new radiotracer PET imaging of β-amyloid plaques, Fernandez-Maza L, Rivera-Marrero S, Prats Capote A, Parrado-Gallego A, Fernandez-Gomez I, Balcerzyk M, Sablon-Carrazana M, Perera-Pintado A, Merceron-Martinez D, Acosta-Medina E, Rodriguez-Tanty C, OP30 Synthesis and preclinical evaluation of [11C]-BA1 PET tracer for the imaging of CSF-1R, Bala Attili, Muneer Ahamed, Guy Bormans, OP31 In vivo imaging of the MCHR1 in the ventricular system via [18F]FE@SNAP, C. Philippe, M. Zeilinger, T. Scherer, C. Fürnsinn, M. Dumanic, W. Wadsak, M. Hacker, M. Mitterhauser, OP32 Synthesis of the first carbon-11 labelled P2Y12 receptor antagonist for imaging the anti-inflammatory phenotype of activated microglia, B. Janssen, D.J. Vugts, G.T. Molenaar, U. Funke, P.S. Kruijer, F. Dollé, G. Bormans, A.A. Lammertsma, A.D. Windhorst, OP33 Radiosynthesis of a selective HDAC6 inhibitor [11C]KB631 and in vitro and ex vivo evaluation, Koen Vermeulen, Muneer Ahamed, Michael Schnekenburger, Mathy Froeyen, Dag Erlend Olberg, Marc Diederich, Guy Bormansa, OP34 Improving metabolic stability of fluorine-18 labelled verapamil analogues, Raaphorst RM, Luurtsema G, Lammertsma AA, Elsinga PH, Windhorst AD, OP36 Development of a novel PET tracer for the activin receptor-like kinase 5, Lonneke Rotteveel, Uta Funke, Peter ten Dijke, Harm Jan Bogaard, Adriaan A. Lammertsma, Albert D. Windhorst, OP37 SPECT imaging and biodistribution studies of 111In-EGF-Au-PEG nanoparticles in vivo, Lei Song, Sarah Able, Nadia Falzone, Veerle Kersemans, Katherine Vallis, OP38 Melanoma targeting with [99mTc(N)(PNP3)]-labeled NAPamide derivatives: preliminary pharmacological studies, Davide Carta, Nicola Salvarese, Wiebke Sihver, Feng Gao, Hans Jürgen Pietzsch, Barbara Biondi, Paolo Ruzza, Fiorenzo Refosco, Cristina Bolzati, OP39 [68Ga]NODAGA-RGD: cGMP synthesis and data from a phase I clinical study, Roland Haubner, Armin Finkensted, Armin Stegmair, Christine Rangger, Clemens Decristoforo, Heinz Zoller, Irene J. Virgolin, OP44 Implementation of a GMP-grade radiopharmacy facility in Maastricht, Ivo Pooters, Maartje Lotz, Roel Wierts, Felix Mottaghy, Matthias Bauwens, OP45 Setting up a GMP production of a new radiopharmaceutical, Forsback, Sarita, Bergman Jörgen, Kivelä Riikka, OP48 In vitro and in vivo evaluation of 68-gallium labeled Fe3O4-DPD nanoparticles as potential PET/MRI imaging agents, M. Karageorgou, M. Radović, C. Tsoukalas, B. Antic, M. Gazouli, M. Paravatou-Petsotas, S. Xanthopouls, M. Calamiotou, D. Stamopoulos, S. Vranješ-Durić, P. Bouziotis, OP49 Fast PET imaging of inflammation using 68Ga-citrate with Fe-containing salts of hydroxy acids, A. S. Lunev, A. A. Larenkov, K.A. Petrosova, O. E. Klementyeva, G. E. Kodina, PP01 Installation and validation of 11C-methionine synthesis, Kvernenes, O.H., Adamsen, T.C.H., PP02 Fully automated synthesis of 68Ga-labelled peptides using the IBA Synthera® and Synthera® Extension modules, René Martin, Sebastian Weidlich, Anna-Maria Zerges, Cristiana Gameiro, Neva Lazarova, Marco Müllera, PP03 GMP compliant production of 15O-labeled water using IBA 18 MeV proton cyclotron, Gert Luurtsema, Michèl de Vries, Michel Ghyoot, Gina van der Woude, Rolf Zijlma, Rudi Dierckx, Hendrikus H. Boersma, Philip H. Elsinga, PP04 In vitro Nuclear Imaging Potential of New Subphthalocyanine and Zinc Phthalocyanine, Fatma Yurt Lambrecht, Ozge Er, Mine Ince, Cıgır Biray Avci, Cumhur Gunduz, Fatma Aslihan Sarı, PP05 Synthesis, Photodynamic Therapy Efficacy and Nuclear Imaging Potential of Zinc Phthalocyanines, Kasim Ocakoglu, Ozge Er, Onur Alp Ersoz, Fatma Yurt Lambrecht, Mine Ince, Cagla Kayabasi, Cumhur Gunduz, PP06 Radio-U(H)PLC – the Search on the Optimal Flow Cell for the γ-Detector, Torsten Kniess, Sebastian Meister, Steffen Fischer, Jörg Steinbach, PP07 Radiolabeling, characterization & biodistribution study of cysteine and its derivatives with Tc99m, Rabia Ashfaq, Saeed Iqbal, Atiq-ur-Rehman, Irfan ullah Khan, PP08 Radiolabelling of poly (lactic-co.glycolic acid) (PLGA) nanoparticles with 99mTC, R Iglesias-Jerez, Cayero-Otero, L. Martín-Banderas, A. Perera-Pintado, I. Borrego-Dorado, PP09 Development of [18F]PD-410 as a non-peptidic PET radiotracer for gastrin releasing peptide receptors, Ines Farinha-Antunes, Chantal Kwizera, Enza Lacivita, Ermelinda Lucente, Mauro Niso, Paola De Giorgio, Roberto Perrone, Nicola A. Colabufo, Philip H. Elsinga, Marcello Leopoldo, PP10 An improved nucleophilic synthesis of 2-(3,4-dimethoxyphenyl)-6-(2-[18F]fluoroethoxy) benzothiazole ([18F]FEDMBT), potential diagnostic agent for breast cancer imaging by PET, V.V. Vaulina, O.S. Fedorova, V.V. Orlovskaja, ?�.L. Chen, G.Y. Li, F.C. Meng, R.S. Liu, H.E. Wang, R.N. Krasikova, PP11 Internal radiation dose assessment of radiopharmaceuticals prepared with accelerator-produced 99mTc, Laura Meléndez-Alafort, Mohamed Abozeid, Guillermina Ferro-Flores, Anna Negri, Michele Bello, Nikolay Uzunov, Martha Paiusco, Juan Esposito, Antonio Rosato, PP12 A specialized five-compartmental model software for pharmacokinetic parameters calculation, Laura Meléndez-Alafort, Cristina Bolzati, Guillermina Ferro-Flores, Nicola Salvarese, Debora Carpanese, Mohamed Abozeid, Antonio Rosato, Nikolay Uzunov, PP13 Molecular imaging of the pharmacokinetic behavior of low molecular weight 18F-labeled PEtOx in comparison to 89Zr-labeled PEtOx, Palmieri L, Verbrugghen T, Glassner M, Hoogenboom R, Staelens S, Wyffels L, PP14 Towards nucleophilic synthesis of the α-[18F]fluoropropyl-L-dihydroxyphenylalanine, V. V. Orlovskaja, O. F. Kuznetsova, O. S. Fedorova, V. I. Maleev, Yu. N. Belokon, A. Geolchanyan, A. S. Saghyan, L. Mu, R. Schibli, S. M. Ametamey, R. N. Krasikova, PP15 A convenient one-pot synthesis of [18F]clofarabine, Revunov, Evgeny, Malmquist, Jonas, Johnström, Peter, Van Valkenburgh, Juno, Steele, Dalton, Halldin, Christer, Schou, Magnus, PP16 BODIPY-estradiol conjugates as multi-modality tumor imaging agents, Samira Osati,Michel Paquette,Simon Beaudoin,Hasrat Ali,Brigitte Guerin, Jeffrey V. Leyton, Johan E. van Lier, PP17 Easy and high yielding synthesis of 68Ga-labelled HBED-PSMA and DOTA-PSMA by using a Modular-Lab Eazy automatic synthesizer, Di Iorio V, Iori M, Donati C, Lanzetta V, Capponi PC, Rubagotti S, Dreger T, Kunkel F, Asti M, PP18 Synthesis and evaluation of fusarinine C-based octadentate bifunctional chelators for zirconium-89 labelling, Chuangyan Zhai, Christine Rangger, Dominik Summer, Hubertus Haas, Clemens Decristoforo, PP19 Fully automated production of [18F]NaF using a re-configuring FDG synthesis module., Suphansa Kijprayoon, Ananya Ruangma, Suthatip Ngokpol, Samart Tuamputsha, PP20 Extension of the Carbon-11 Small Labeling Agents Toolbox and Conjugate Addition, Ulrike Filp, Anna Pees, Carlotta Taddei, Aleksandra Pekošak, Antony D. Gee, Alex J. Poot, Albert D. Windhorst, PP21 In vitro studies on BBB penetration of pramipexole encapsulated theranostic liposomes for the therapy of Parkinson’s disease, Mine Silindir Gunay, A. Yekta Ozer, Suna Erdogan, Ipek Baysal, Denis Guilloteau, Sylvie Chalon, PP22 Factors affecting tumor uptake of 99mTc-HYNIC-VEGF165, Filippo Galli, Marco Artico, Samanta Taurone, Enrica Bianchi, Bruce D. Weintraub, Mariusz Skudlinski, Alberto Signore, PP23 Rhenium-188: a suitable radioisotope for targeted radiotherapy, Nicolas Lepareur, Nicolas Noiret, François Hindré, Franck Lacœuille, Eric Benoist, Etienne Garin, PP24 Preparation of a broad palette of 68Ga radiopharmaceuticals for clinical applications, Trejo-Ballado F, Zamora-Romo E, Manrique-Arias JC, Gama-Romero HM, Contreras-Castañon G, Tecuapetla-Chantes RG, Avila-Rodriguez MA, PP25 68Ga-peptide preparation with the use of two 68Ge/68Ga-generators, H. Kvaternik, D. Hausberger, C. Zink, B. Rumpf, R. M. Aigner, PP26 Assay of HEPES in 68Ga-peptides by HPLC, H. Kvaternik, D. Hausberger, B. Rumpf, R. M. Aigner, PP27 Preparation, in vitro and in vivo evaluation of a 99mTc(I)-Diethyl Ester (S,S)-Ethylenediamine- N,N´-DI-2-(3-Cyclohexyl) Propionic acid as a target-specific radiopharmaceutical, Drina Janković, Mladen Lakić, Aleksandar Savić, Slavica Ristić, Nadežda Nikolić, Aleksandar Vukadinović, Tibor J. Sabo, Sanja Vranješ-Đurić, PP28 90Y-labeled magnetite nanoparticles for possible application in cancer therapy, S. Vranješ-Đurić, M. Radović, D. Janković, N. Nikolić, G. F. Goya, P. Calatayud, V. Spasojević, B. Antić, PP29 Simplified automation of the GMP production of 68Ga-labelled peptides, David Goblet, Cristiana Gameiro, Neva Lazarova, PP30 Combining commercial production of multi-products in a GMP environment with Clinical & R&D activities, Cristiana Gameiro, Ian Oxley, Antero Abrunhosa, Vasko Kramer, Maria Vosjan, Arnold Spaans, PP31 99mTc(CO)3-labeling and Comparative In-Vivo Evaluation of Two Clicked cRGDfK Peptide Derivatives, Kusum Vats, Drishty Satpati, Haladhar D Sarma, Sharmila Banerjee, PP32 Application of AnaLig resin for 99mTc separation from molybdenum excess, Wojdowska W., Pawlak D.W., Parus L. J., Garnuszek P., Mikołajczak R., PP33 Constraints for selection of suitable precursor for one-step automated synthesis of [18F]FECNT, the dopamine transporter ligand, Pijarowska-Kruszyna J, Jaron A, Kachniarz A, Malkowski B, Garnuszek P, Mikolajczak R, PP34 Gamma scintigraphy studies with 99mTc- amoxicillin sodium in bacterially infected and sterile inflamed rats, Derya Ilem-Ozdemir, Oya Caglayan-Orumlu, Makbule Asikoglu, PP35 Preparation of 99mTc- Amoxicillin Sodium Lyophilized Kit, Derya Ilem-Ozdemir, Oya Caglayan-Orumlu, Makbule Asikoglu, PP36 Outfits of Tracerlan FXC-PRO for 11C-Labeling, Arponen Eveliina, Helin Semi, Saarinen Timo, Vauhkala Simo, Kokkomäki Esa, Lehikoinen Pertti, PP37 Microfluidic synthesis of ω-[18F]fluoro-1-alkynes, Mariarosaria De Simone, Giancarlo Pascali, Ludovica Carzoli, Mauro Quaglierini, Mauro Telleschi, Piero A. Salvadori, PP38 Automated 18F-flumazenil production using chemically resistant disposable cassettes, Phoebe Lam, Martina Aistleitner, Reinhard Eichinger, Christoph Artner, PP39 The effect of the eluent solutions (TBAHCO3, Kryptand K2.2.2) on the radiochemical yields of 18F-Fluoromethylcholine, Surendra Nakka, Hemantha Kumara MC, Al-Qahtani Mohammed, PP40 [68Ga]Radiolabeling of short peptide that has a PET imaging potentials, Al-Qahtani, Mohammed, Al-Malki, Yousif, PP41 Is validation of radiochemical purity analysis in a public hospital in a developing country possible?, N Mambilima, SM Rubow, PP42 Improved automated radiosynthesis of [18F]FEPPA, N. Berroterán-Infante, M. Hacker, M. Mitterhauser, W. Wadsak, PP43 Synthesis and initial evaluation of Al18F-RESCA1-TATE for somatostatin receptor imaging with PET, Uta Funke, Frederik Cleeren, Joan Lecina, Rodrigo Gallardo, Alfons M. Verbruggen, Guy Bormans, PP44 Radiolabeling and SPECT/CT imaging of different polymer-decorated zein nanoparticles for oral administration, Rocío Ramos-Membrive, Ana Brotons, Gemma Quincoces, Laura Inchaurraga, Inés Luis de Redín, Verónica Morán, Berta García-García, Juan Manuel Irache, Iván Peñuelas, PP45 An analysis of the quality of 68Ga-DOTANOC radiolabelling over a 3 year period, Trabelsi, M., Cooper M.S., PP46 In vivo biodistribution of adult human mesenchymal stem cells I (MSCS-ah) labeled with 99MTC-HMPAO administered via intravenous and intra-articular in animal model. Preliminary results, Alejandra Abella, Teodomiro Fuente, Antonio Jesús Montellano, Teresa Martínez, Ruben Rabadan, Luis Meseguer-Olmo, PP47 Synthesis of [18F]F-exendin-4 with high specific activity, Lehtiniemi P, Yim C, Mikkola K, Nuutila P, Solin O, PP48 Experimental radionuclide therapy with 177Lu-labelled cyclic minigastrin and human dosimetry estimations, von Guggenberg E, Rangger C, Mair C, Balogh L, Pöstényi Z, Pawlak D, Mikołajczak R, PP49 Synthesis of radiopharmaceuticals for cell radiolabelling using anion exchange column, Socan A, Kolenc Peitl P, Krošelj M, Rangger C, Decristoforo C, PP50 [68Ga]peptide production on commercial synthesiser mAIO, Collet C., Remy S., Didier R,Vergote T.,Karcher G., Véran N., PP51 Dry kit formulation for efficient radiolabeling of 68Ga-PSMA, D. Pawlak, M. Maurin, P. Garnuszek, U. Karczmarczyk, R. Mikołajczak, PP52 Development of an experimental method using Cs-131 to evaluate radiobiological effects of internalized Auger-electron emitters, Pil Fredericia, Gregory Severin, Torsten Groesser, Ulli Köster, Mikael Jensen, PP53 Preclinical comparative evaluation of NOTA/NODAGA/DOTA CYCLO-RGD peptides labelled with Ga-68, R. Leonte, F. D. Puicea, A. Raicu, E. A. Min, R. Serban, G. Manda, D. Niculae, PP54 Synthesizer- and Kit-based preparation of prostate cancer imaging agent 68Ga-RM2, Marion Zerna, Hanno Schieferstein, Andre Müller, Mathias Berndt, PP55 Synthesis of pancreatic beta cell-specific [18F]fluoro-exendin-4 via strain-promoted aza-dibenzocyclooctyne/azide cycloaddition, Cheng-Bin Yim, Kirsi Mikkola, Pirjo Nuutila, Olof Solin, PP56 Automated systems for radiopharmacy, D. Seifert, J. Ráliš, O. Lebeda, PP57 Simple, suitable for everyday routine use quality control method to assess radionuclidic purity of cyclotron-produced 99mTc, Svetlana V. Selivanova, Helena Senta, Éric Lavallée, Lyne Caouette, Éric Turcotte, Roger Lecomte, PP58 Effective dose estimation using Monte Carlo simulation for patients undergoing radioiodine therapy, Marina Zdraveska Kochovska, Emilija Janjevik Ivanovska, Vesna Spasic Jokic, PP59 Chemical analysis of the rituximab radioimmunoconjugates in lyophilized formulations intended for oncological applications, Darinka Gjorgieva Ackova, Katarina Smilkov, Petre Makreski, Trajče Stafilov, Emilija Janevik-Ivanovska, PP61 The need and benefits of established radiopharmacy in developing African countries, Aschalew Alemu, Joel Munene Muchira, David Mwanza Wanjeh, Emilija Janevik-Ivanovska, PP62 University Master Program of Radiopharmacy – step forward for Good Radiopharmacy Education, Emilija Janevik-Ivanovska, Zoran Zdravev, Uday Bhonsle, Osso Júnior João Alberto, Adriano Duatti, Bistra Angelovska, Zdenka Stojanovska, Zorica Arsova Sarafinovska, Darko Bosnakovski, Darinka Gorgieva-Ackova, Katarina Smilkov, Elena Drakalska, Meera Venkatesh, Rubin Gulaboski, PP63 Synthesis and preclinical validations of a novel 18F-labelled RGD peptide prepared by ligation of a 2-cyanobenzothiazole with 1,2-aminothiol to image angiogenesis., Didier J. Colin, James A. H. Inkster, Stéphane Germain, Yann Seimbille
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- 2016
37. Abstract 2641: AZD4635 A2A receptor occupancy in cynomolgus monkey using PET and its application to an oncology clinical development program
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Johnström, Peter, primary, Gutierrez, Pablo Morentin, additional, Varnäs, Katarina, additional, Schou, Magnus, additional, Takano, Akihiro, additional, Jones, Lorraine, additional, Mugundu, Ganesh, additional, McCoon, Patricia, additional, Lyne, Paul, additional, Infante, Jeffrey, additional, Falchook, Gerald, additional, Patel, Manish, additional, Karlix, Janet, additional, Merchant, Melinda, additional, Clarke, James, additional, Cross, Alan, additional, Seneca, Nicholas, additional, Farde, Lars, additional, Congreve, Miles, additional, Mason, Jon S., additional, and Marshall, Fiona H., additional
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- 2017
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38. A total synthesis of hydroxylsine in protected form and investigations of the reductive opening of p-methoxybenzylidene acetals
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Gustafsson, Tomas, Schou, Magnus, Almqvist, Fredrik, and Kihlberg, Jan
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Chirality -- Research ,Chemical synthesis -- Observations ,Malic acid -- Research ,Biological sciences ,Chemistry - Abstract
A synthesis of (2S,5R)-5-hydroxylysine is developed based on (R)-malic acid and Williams glycine template as chiral precursors. An equivalent amount of trialkysilyl hydride is formed in the reaction, which leads to additional mechanistic insight into reductive openings of p-methoxybenzylidene acetals with sodium cyanoborohydride as reducing agent.
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- 2004
39. Efficient DBU accelerated synthesis of F-18-labelled trifluoroacetamides
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Bermejo Gómez, Antonio, Cortés González, Miguel A., Lübcke, Marvin, Johansson, Magnus J., Halldin, Christer, Szabó, Kálmán J., Schou, Magnus, Bermejo Gómez, Antonio, Cortés González, Miguel A., Lübcke, Marvin, Johansson, Magnus J., Halldin, Christer, Szabó, Kálmán J., and Schou, Magnus
- Abstract
Nucleophilic F-18-fluorination of bromodifluoromethyl derivatives was performed using [F-18] Bu4NF in the presence of DBU(1,8-diazabicyclo[5.4.0]undec-7-ene). This novel procedure provided a diverse set of [F-18] trifluoroacetamides in good to excellent radiochemical conversions. A mechanism where DBU acts as organomediator in this transformation is proposed.
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- 2016
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40. Large Variation in Brain Exposure of Reference CNS Drugs: a PET Study in Nonhuman Primates
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Schou, Magnus, primary, Varnäs, Katarina, additional, Lundquist, Stefan, additional, Nakao, Ryuji, additional, Amini, Nahid, additional, Takano, Akihiro, additional, Finnema, Sjoerd J., additional, Halldin, Christer, additional, and Farde, Lars, additional
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- 2015
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41. Low background and high contrast PET imaging of amyloid-β with [11C]AZD2995 and [11C]AZD2184 in Alzheimer's disease patients
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Forsberg, Anton, Juréus, Anders, Cselényi, Zsolt, Eriksdotter, Maria, Freund-Levi, Yvonne, Jeppsson, Fredrik, Swahn, Britt-Marie, Sandell, Johan, Julin, Per, Schou, Magnus, Andersson, Jan, Johnström, Peter, Varnäs, Katarina, Halldin, Christer, Farde, Lars, Svensson, Samuel, Forsberg, Anton, Juréus, Anders, Cselényi, Zsolt, Eriksdotter, Maria, Freund-Levi, Yvonne, Jeppsson, Fredrik, Swahn, Britt-Marie, Sandell, Johan, Julin, Per, Schou, Magnus, Andersson, Jan, Johnström, Peter, Varnäs, Katarina, Halldin, Christer, Farde, Lars, and Svensson, Samuel
- Abstract
PURPOSE: The aim of this study was to evaluate AZD2995 side by side with AZD2184 as novel PET radioligands for imaging of amyloid-β in Alzheimer's disease (AD). METHODS: In vitro binding of tritium-labelled AZD2995 and AZD2184 was studied and compared with that of the established amyloid-β PET radioligand PIB. Subsequently, a first-in-human in vivo PET study was performed using [(11)C]AZD2995 and [(11)C]AZD2184 in three healthy control subjects and seven AD patients. RESULTS: AZD2995, AZD2184 and PIB were found to share the same binding site to amyloid-β. [(3)H]AZD2995 had the highest signal-to-background ratio in brain tissue from patients with AD as well as in transgenic mice. However, [(11)C]AZD2184 had superior imaging properties in PET, as shown by larger effect sizes comparing binding potential values in cortical regions of AD patients and healthy controls. Nevertheless, probably due to a lower amount of nonspecific binding, the group separation of the distribution volume ratio values of [(11)C]AZD2995 was greater in areas with lower amyloid-β load, e.g. the hippocampus. CONCLUSION: Both AZD2995 and AZD2184 detect amyloid-β with high affinity and specificity and also display a lower degree of nonspecific binding than that reported for PIB. Overall [(11)C]AZD2184 seems to be an amyloid-β radioligand with higher uptake and better group separation when compared to [(11)C]AZD2995. However, the very low nonspecific binding of [(11)C]AZD2995 makes this radioligand potentially interesting as a tool to study minute levels of amyloid-β. This sensitivity may be important in investigating, for example, early prodromal stages of AD or in the longitudinal study of a disease modifying therapy.
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- 2013
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42. Synthesis and evaluation of new PET radioloigands for imaging central norepinephrine transporters
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Schou, Magnus and Schou, Magnus
- Abstract
The noradrenergic (NE), serotonergic (5-HT) and dopaminergic (DA) neurotransmission systems all have specific proteins responsible for the regulation of synaptic concentrations of neurotransmitter in the central nervous system (CNS) and in the periphery. Several reports have shown that the expression of these proteins, the monoamine transporters, within the CNS, may be altered in patients with certain neurodegenerative or neuropsychiatric disorders. Positron emission tomography (PET) is an imaging technique that enables quantitative studies in high resolution of receptor or transporter proteins inside the living human brain. At the outset of research for this thesis, PET had been used successfully in the mapping of 5-HT and DA transporters, but not NE transporters (NETs). The aim of this thesis was to develop a radioligand suitable for imaging NETs in the human brain in vivo. This project focused on the screening of candidate NET radioligands by emission measurements in cynomolgus monkeys in vivo. Concomitant with these studies, radiometabolite analyses were performed on peripheral monkey plasma. To further characterise radioligands, in vitro autoradiography studies were performed on post mortem human brain tissue. During this screening process, nine of the most potent and selective NET inhibitors reported to date were prepared and labeled with carbon- 11 (t1/2 20.4 min) or fluorine- 18 (t1/2 109.8 min). Some improvements were also made with regards to the labelling of aryl fluoromethyl ethers and sulfides with fluorine-18, with a view to potential application in preparing new candidate NET radioligands. Several candidate radioligands failed in the initial screening process. However, one lead compound was identified, namely (S,S)-[11C]MeNER. The regional distribution of (S,S)-[11C]MeNER in monkey brain was found to be in accord with known densities of NETs and was also shown to be specific to NET in a pre-treatment experiment. However, the binding kinetics of (S,S)
- Published
- 2006
43. Identification of PET radiometabolites by cytochrome P450, UHPLC/Q-ToF-MS and fast radio-LC: applied to the PET radioligands [11C]flumazenil, [18F]FE-PE2I, and [11C]PBR28
- Author
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Amini, Nahid, primary, Nakao, Ryuji, additional, Schou, Magnus, additional, and Halldin, Christer, additional
- Published
- 2012
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44. Clinical Validation of 18F-AZD4694, an Amyloid-β–Specific PET Radioligand
- Author
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Cselényi, Zsolt, primary, Jönhagen, Maria Eriksdotter, additional, Forsberg, Anton, additional, Halldin, Christer, additional, Julin, Per, additional, Schou, Magnus, additional, Johnström, Peter, additional, Varnäs, Katarina, additional, Svensson, Samuel, additional, and Farde, Lars, additional
- Published
- 2012
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- View/download PDF
45. Identification of PET radiometabolites by cytochrome P450, UHPLC/Q-ToF-MS and fast radio-LC: applied to the PET radioligands [C]flumazenil, [F]FE-PE2I, and [C]PBR28.
- Author
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Amini, Nahid, Nakao, Ryuji, Schou, Magnus, and Halldin, Christer
- Subjects
METABOLITES ,RADIOLIGAND assay ,MICROSOMES ,POSITRON emission tomography ,LIQUID chromatography ,HIGH performance liquid chromatography - Abstract
A general method is presented for the identification of radiometabolites in plasma of human and monkey subjects after administration of positron emission tomography (PET) radioligands. The radiometabolites are first produced in vitro, using liver microsomes, subsequently separated using fast radio-liquid chromatography (radio-LC), and individually collected and identified by ultra high-performance liquid chromatography/quadrupole-time of flight-mass spectrometry in MS and MS mode. Fast radio-LC provided superior resolution compared to conventional radio-LC, resulting in separation of a greater number of metabolites. The radiometabolites produced in vivo are then compared to and identified based on the in vitro results. This approach was applied to three PET radioligands, [C]flumazenil, [F]FE-PE2I, and [C]PBR28, resulting in the identification of five, two, and one radiometabolites, respectively. This procedure can easily be adopted to identify the radiometabolites produced in vivo from a variety of PET radioligands. [ABSTRACT FROM AUTHOR]
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- 2013
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46. Clinical Validation of 18F-AZD4694, an Amyloid-β-Specific PET Radioligand.
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Cselényi, Zsolt, Jönhagen, Maria Eriksdotter, Forsberg, Anton, Halldin, Christer, Julin, Per, Schou, Magnus, Johnstrom, Peter, Varnas, Katarina, Svensson, Samuel, and Farde, Lars
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- 2012
- Full Text
- View/download PDF
47. Potential for imaging the high-affinity state of the 5-HT1B receptor: a comparison of three PET radioligands with differing intrinsic activity.
- Author
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Lindberg, Anton, Arakawa, Ryosuke, Nogami, Tsuyoshi, Nag, Sangram, Schou, Magnus, Elmore, Charles S., Farde, Lars, Pike, Victor W., and Halldin, Christer
- Subjects
POSITRON emission tomography ,KRA ,FENFLURAMINE ,BRAIN imaging ,DOPAMINE receptors ,TRANSLOCATOR proteins - Abstract
Background: Over the last decade, a few radioligands have been developed for PET imaging of brain 5-HT
1B receptors. The 5-HT1B receptor is a G-protein-coupled receptor (GPCR) that exists in two different agonist affinity states. An agonist ligand is expected to be more sensitive towards competition from another agonist, such as endogenous 5-HT, than an antagonist ligand. It is of interest to know whether the intrinsic activity of a PET radioligand for the 5-HT1B receptor impacts on its ability to detect changes in endogenous synaptic 5-HT density. Three high-affinity11 C-labeled 5-HT1B PET radioligands with differing intrinsic activity were applied to PET measurements in cynomolgus monkey to evaluate their sensitivity to be displaced within the brain by endogenous 5-HT. For these experiments, fenfluramine was pre-administered at two different doses (1.0 and 5.0 mg/kg, i.v.) to induce synaptic 5-HT release. Results: A dose-dependent response to fenfluramine was detected for all three radioligands. At the highest dose of fenfluramine (5.0 mg/kg, i.v.), reductions in specific binding in the occipital cortex increased with radioligand agonist efficacy, reaching 61% for [11 C]3. The most antagonistic radioligand showed the lowest reduction in specific binding. Conclusions: Three 5-HT1B PET radioligands were identified with differing intrinsic activity that could be used in imaging high- and low-affinity states of 5-HT1B receptors using PET. From this limited study, radioligand sensitivity to endogenous 5-HT appears to depend on agonist efficacy. More extensive studies are required to substantiate this suggestion. [ABSTRACT FROM AUTHOR]- Published
- 2019
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48. The development of a GPR44 targeting radioligand [11C]AZ12204657 for in vivo assessment of beta cell mass.
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Jahan, Mahabuba, Johnström, Peter, Selvaraju, Ram K., Svedberg, Marie, Winzell, Maria Sörhede, Bernström, Jenny, Kingston, Lee, Schou, Magnus, Jia, Zhisheng, Skrtic, Stanko, Johansson, Lars, Korsgren, Olle, Farde, Lars, Halldin, Christer, and Eriksson, Olof
- Subjects
G protein coupled receptors ,MEMBRANE proteins ,PANCREATIC beta cells ,CELL receptors ,RADIOLIGAND assay - Abstract
Background: The G-protein-coupled receptor 44 (GPR44) is a beta cell-restricted target that may serve as a marker for beta cell mass (BCM) given the development of a suitable PET ligand.Methods: The binding characteristics of the selected candidate, AZ12204657, at human GPR44 were determined using in vitro ligand binding assays. AZ12204657 was radiolabeled using
11 C- or3 H-labeled methyl iodide ([11 C/3 H]CH3 I) in one step, and the conversion of [11 C/3 H]CH3 I to the radiolabeled product [11 C/3 H]AZ12204657 was quantitative. The specificity of radioligand binding to GPR44 and the selectivity for beta cells were evaluated by in vitro binding studies on pancreatic sections from human and non-human primates as well as on homogenates from endocrine and exocrine pancreatic compartments.Results: The radiochemical purity of the resulting radioligand [11 C]AZ12204657 was > 98%, with high molar activity (MA), 1351 ± 575 GBq/μmol (n = 18). The radiochemical purity of [3 H]AZ12204657 was > 99% with MA of 2 GBq/μmol. Pancreatic binding of [11 C/3 H]AZ12204657 was co-localized with insulin-positive islets of Langerhans in non-diabetic individuals and individuals with type 2 diabetes (T2D). The binding of [11 C]AZ12204657 to GPR44 was > 10 times higher in islet homogenates compared to exocrine homogenates. In human islets of Langerhans GPR44 was co-expressed with insulin, but not glucagon as assessed by co-staining and confocal microscopy.Conclusion: We radiolabeled [11 C]AZ12204657, a potential PET radioligand for the beta cell-restricted protein GPR44. In vitro evaluation demonstrated that [3 H]AZ12204657 and [11 C]AZ12204657 selectively target pancreatic beta cells. [11 C]AZ12204657 has promising properties as a marker for human BCM. [ABSTRACT FROM AUTHOR]- Published
- 2018
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49. Abstract 15351: Risk Profile, Antithrombotic Treatment and Clinical Outcomes for Patients in Nordic Countries With Atrial Fibrillation - Results From the Garfield-AF Registry
- Author
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Pope, Marita Knudsen, Atar, Dan, Svilaas, Arne, Hole, Torstein, Eivind, Berge, Dalsgaard-Nielsen, Joern, Rosenqvist, Maarten, Schou, Magnus, Crisby, Milita, Raatikainen, Pekka, Airaksinen, Juhani, Illingworth, Laura, Pieper, Karen, Kayani, Gloria, Le Heuzey, Jean-Yves, Steffel, Jan, Stepinska, Janina, Camm, John, Bassand, Jean Pierre, and Kakkar, Ajey Kumar
- Abstract
Aims:To evaluate clinical characteristics, management and outcomes for patients with newly diagnosed non-valvular atrial fibrillation (AF) at risk for stroke in Nordic countries.Methods:We extracted data from the ?Global Anticoagulant Registry in the FIELD of AF?(GARFIELD-AF), comprising baseline characteristics and medical history, antithrombotic treatment, and one-year clinical outcomes for patients with AF in the Nordic countries Sweden, Denmark, Finland and Norway, and Non-Nordic European countries. For clinical outcomes, results were compared to Non-European countries.Results:From 2009 to 2016, 52 014 patients worldwide were enrolled in the study, of which 2 395 from Nordic and 27 546 from Non-Nordic-European countries. Nordic patients were older than Non-Nordic-Europeans (mean age 71.7 vs 70.6). In both groups, almost nine in ten had a CHA2DS2-VASc score ?2. Antithrombotic treatment was prescribed to 90.0% of European patients. The use of oral anticoagulants ? antiplatelets (AP), was higher in Nordic countries in all CHA2DS2-VASc categories, i.e., 0-1 (72.6% vs 60.7%), 2-3 (82.0% vs 72.8%) and ?4 (80.1% vs 75.2%). In Nordic countries, AP monotherapy was more rarely used than in Non-Nordic European countries (10.4% vs 18.2%). All-cause mortality rate was significantly lower in Nordic patients than in Non-Nordic European patients and Non-European patients (event rate per 100 patient years 3.76 vs 4.58 vs 4.09, p-value <0.001), stroke rate was lower (1.17 vs 1.35 vs 1.34, p-value <0.001), while major bleeds occurred significantly more often (1.39 vs 0.90 vs 0.69, p-value <0.001).Conclusion:The use of antithrombotic treatment in patients with AF in Europe is generally quite high. Improvements can be made to the choice of drug, that is less AP, especially in Non-Nordic-European countries. Nordic countries had a significantly lower rate of mortality and stroke, but also significantly more major bleeding than Non-Nordic and Non-European countries.
- Published
- 2019
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50. Integrated Strategy for Use of Positron Emission Tomography in Nonhuman Primates to Confirm Multitarget Occupancy of Novel Psychotropic Drugs: An Example with AZD3676.
- Author
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Varnäs K, Juréus A, Johnström P, Ahlgren C, Schött P, Schou M, Gruber S, Jerning E, Malmborg J, Halldin C, Afzelius L, and Farde L
- Subjects
- Animals, Blood Proteins metabolism, Brain diagnostic imaging, Brain drug effects, Brain metabolism, Brain physiology, Humans, Macaca fascicularis, Memory drug effects, Mice, Receptor, Serotonin, 5-HT1A metabolism, Receptor, Serotonin, 5-HT1B metabolism, Serotonin 5-HT1 Receptor Antagonists metabolism, Serotonin 5-HT1 Receptor Antagonists pharmacology, Benzofurans metabolism, Benzofurans pharmacology, Piperazines metabolism, Piperazines pharmacology, Positron-Emission Tomography, Psychotropic Drugs metabolism, Psychotropic Drugs pharmacology, Quinazolines metabolism, Quinazolines pharmacology
- Abstract
Positron emission tomography (PET) is widely applied in central nervous system (CNS) drug development for assessment of target engagement in vivo. As the majority of PET investigations have addressed drug interaction at a single binding site, findings of multitarget engagement have been less frequently reported and have often been inconsistent with results obtained in vitro. AZD3676 [N,N-dimethyl-7-(4-(2-(pyridin-2-yl)ethyl)piperazin-1-yl) benzofuran-2-carboxamide] is a novel combined serotonin (5-hydroxytryptamine) 5-HT1A and 5-HT1B receptor antagonist that was developed for the treatment of cognitive impairment in Alzheimer's disease. Here, we evaluated the properties of AZD3676 as a CNS drug by combining in vitro and ex vivo radioligand binding techniques, behavioral pharmacology in rodents, and PET imaging in nonhuman primates. Target engagement in the nonhuman primate brain was assessed in PET studies by determination of drug-induced occupancy using receptor-selective radioligands. AZD3676 showed preclinical properties consistent with CNS drug potential, including nanomolar receptor affinity and efficacy in rodent models of learning and memory. In PET studies of the monkey brain, AZD3676 inhibited radioligand binding in a dose-dependent manner with similar affinity at both receptors. The equally high affinity at 5-HT1A and 5-HT1B receptors as determined in vivo was not predicted from corresponding estimates obtained in vitro, suggesting more than 10-fold selectivity for 5-HT1A versus 5-HT1B receptors. These findings support the further integrated use of PET for confirmation of multitarget occupancy of CNS drugs. Importantly, earlier introduction of PET studies in nonhuman primates may reduce future development costs and the requirement for animal experiments in preclinical CNS drug development programs., (Copyright © 2016 by The American Society for Pharmacology and Experimental Therapeutics.)
- Published
- 2016
- Full Text
- View/download PDF
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