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Radiolabeled gold nanoparticles (AuNPs) have been widely used for cancer diagnosis and therapy over recent decades. In this study, we focused on the development and in vitro evaluation of four new Au nanoconjugates radiolabeled with technetium-99m (99m Tc) via thiol-bearing ligands attached to the NP surface. More specifically, AuNPs of two different sizes (2 nm and 20 nm, referred to as Au(2) and Au(20), respectively) were functionalized with two bifunctional thiol ligands (referred to as L1H and L2H). The shape, size, and morphology of both bare and ligand-bearing AuNPs were characterized by transmission electron microscopy (TEM) and dynamic light scattering (DLS) techniques. In vitro cytotoxicity was assessed in 4T1 murine mammary cancer cells. The AuNPs were successfully radiolabeled with99mTc-carbonyls at high radiochemical purity (>95%) and showed excellent in vitro stability in competition studies with cysteine and histidine. Moreover, lipophilicity studies were performed in order to determine the lipophilicity of the radiolabeled con-jugates, while a hemolysis assay was performed to investigate the biocompatibility of the bare and functionalized AuNPs. We have shown that the functionalized AuNPs developed in this study lead to stable radiolabeled nanoconstructs with the potential to be applied in multimodality imaging or for in vivo tracking of drug-carrying AuNPs. © 2021 by the authors. Licensee MDPI, Basel, Switzerland.

Purpose: To evaluate the antitumor efficacy of Ag3Au1Trp1:2NPs in a SCID mouse cancer model, with respect to their effect on tumor growth, on tumor’s metastatic potential and the underlying molecular mechanism. Subjects and Methods: Ag3Au1Trp1:2NPs were radiolabeled with Gallium-68 and the biodistribution was studied in Swiss mice without tumors and in SCID mice bearing tumors. SCID mice received intratumoral Ag3Au1Trp1:2NPs and tumor size was measured using calipers. Lung and liver tissues were extracted and studied microscopically for the detection of any metastatic sites. Changes in the Caspase-3 and TNF-related apoptosis-inducing ligand (TRAIL) were also investigated using real-time PCR and Western blot techniques, respectively. Results: In the 4T1 tumor-bearing SCID mice, Ag3Au1Trp1:2NPs showed quick passive accumulation at tumor sites at 30 mins post-injection. Mice that received the highest dose of NPs (5.6mg/mL) demonstrated a 1.9-fold lower tumor volume compared to that of the control group at 11 days post-injection, while mice that did not receive NPs showed metastatic sites in liver and lung. Extracted tumor tissue of treated mice revealed increased Casp-3 mRNA levels as well as elevated TRAIL protein levels. Conclusion: Based on our results, Ag3Au1Trp1:2NPs express anti-tumor and anti-metastatic effects in vivo. Ag3Au1Trp1:2NPs also reach tumor site via the enhancement and retention effect which results in the apoptotic death of cancerous cells selectively via the extrinsic TRAIL-dependent pathway. © 2020 Katifelis et al.

Superparamagnetic iron oxide nanoparticles with well-integrated multimodality imaging properties have generated increasing research interest in the past decade, especially when it comes to the targeted imaging of tumors. Bevacizumab (BCZM) on the other hand is a well-known and widely applied monoclonal antibody recognizing VEGF-A, which is overexpressed in angiogenesis. The aim of this proof-of-concept study was to develop a dual-modality nanoplatform for in vivo targeted single photon computed emission tomography (SPECT) and magnetic resonance imaging (MRI) of tumor vascularization. Iron oxide nanoparticles (IONPs) have been coated with dimercaptosuccinic acid (DMSA), for consequent functionalization with the monoclonal antibody BCZM radiolabeled with 99mTc, via well-developed surface engineering. The IONPs were characterized based on their size distribution, hydrodynamic diameter and magnetic properties. In vitro cytotoxicity studies showed that our nanoconstruct does not cause toxic effects in normal and cancer cells. Fe3O4-DMSA-SMCC-BCZM-99mTc were successfully prepared at high radiochemical purity ( > 92%) and their stability in human serum and in PBS were demonstrated. In vitro cell binding studies showed the ability of the Fe3O4-DMSA-SMCC-BCZM-99mTc to bind to the VEGF-165 isoform overexpressed on M-165 tumor cells. The ex vivo biodistribution studies in M165 tumor-bearing SCID mice showed high uptake in liver, spleen, kidney and lungs. The Fe3O4-DMSA-SMCC-BCZM-99mTc demonstrated quick tumor accumulation starting at 8.9 ± 1.88%ID/g at 2 h p.i., slightly increasing at 4 h p.i. (16.21 ± 2.56%ID/g) and then decreasing at 24 h p.i. (6.01 ± 1.69%ID/g). The tumor-to-blood ratio reached a maximum at 24 h p.i. (~7), which is also the case for the tumor-to-muscle ratio (~18). Initial pilot imaging studies on an experimental gamma-camera and a clinical MR camera prove our hypothesis and demonstrate the potential of Fe3O4-DMSA-SMCC-BCZM-99mTc for targeted dual-modality imaging. Our findings indicate that Fe3O4-DMSA-SMCC-BCZM-99mTc IONPs could serve as an important diagnostic tool for biomedical imaging as well as a promising candidate for future theranostic applications in cancer. © 2018 Tsoukalas, Psimadas, Kastis, Koutoulidis, Harris, Paravatou-Petsotas, Karageorgou, Furenlid, Moulopoulos, Stamopoulos and Bouziotis.

Aim: The aim of this study was to develop a dual-modality positron emission tomography/magnetic resonance (PET/MR) imaging probe by radiolabeling gadolinium-containing AGuIX derivatives with the positron-emitter Gallium-68 (68Ga). Materials & methods: AGuIX@NODAGA nanoparticles were labeled with 68Ga at high efficiency. Tumor accumulation in an appropriate disease model was assessed by ex vivo biodistribution and in vivo PET/MR imaging. Results: 68Ga-AGuIX@NODAGA was proven to passively accumulate in U87MG human glioblastoma tumor xenografts. Metabolite assessment in serum, urine and tumor samples showed that 68Ga-AGuIX@NODAGA remains unmetabolized up to at least 60 min postinjection. Conclusion: This study demonstrates that 68Ga-AGuIX@NODAGA can be used as a dual-modality PET/MR imaging agent with passive accumulation in the diseased area, thus showing great potential for PET/MR image-guided radiation therapy. © 2017 Olivier Tillement.

The aim of this study was to develop a dual-modality PET/MR imaging probe by radiolabeling iron oxide magnetic nanoparticles (IONPs), surface functionalized with water soluble stabilizer 2,3-dicarboxypropane-1,1-diphosphonic acid (DPD), with the positron emitter Gallium-68. Magnetite nanoparticles (Fe3O4 MNPs) were synthesized via coprecipitation method and were stabilized with DPD. The Fe3O4-DPD MNPs were characterized based on their structure, morphology, size, surface charge, and magnetic properties. In vitro cytotoxicity studies showed reduced toxicity in normal cells, compared to cancer cells. Fe3O4-DPD MNPs were successfully labeled with Gallium-68 at high radiochemical purity (>91%) and their stability in human serum and in PBS was demonstrated, along with their further characterization on size and magnetic properties. The ex vivo biodistribution studies in normal Swiss mice showed high uptake in the liver followed by spleen. The acquired PET images were in accordance with the ex vivo biodistribution results. Our findings indicate that Ga68-Fe3O4-DPD MNPs could serve as an important diagnostic tool for biomedical imaging. © 2017 Maria-Argyro Karageorgou et al.

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

The synthesis and characterization of three neutral tricarbonyl fac-M(CO)3(NNO) (M = Re, 99mTc) complexes based on the picolylamine N,N-diacetic acid (PADA) ligand is reported. One of the two carboxylate groups of the PADA ligand is efficiently and conveniently derivatized with an amine nucleophile through the use of the PADA anhydride. In this work, aniline, benzylamine and pyrrolidine were used as model amine nucleophites. The rhenium complexes were synthesized using the [NEt 4]2[Re(CO)3Br3] precursor and fully characterized by elemental analysis, spectroscopic methods, and X-ray crystallography. The analogous technetium-99m complexes were also prepared quantitatively using the (99mTc(CO)3(H2O) 3]+ precursor. The reaction scheme presented for the synthesis of the fac-M(CO)3(NNO) (M = Re, 99mTc) complexes can be applied to the development of target-specific radiopharmaceuticals because, in principle, any bioactive pharmacophore bearing an amine group can be used in the place of the model amine nucleophiles. © 2008 American Chemical Society.

The novel tetradentate N3O bifunctional agent 3-hydroxy-4-[2-(2′-pyridinecarboxamido)acetylamino]benzoic acid (1), reacts with [Bu4N][ReOCl4] of [Bu4N][ 99gTcOCl4] in EtOH resulting in neutral and stable oxorhenium 2 or oxotechnetium-99 g 3 complexes. Both complexes were characterized by elemental analysis, IR, 1H and 13C NMR spectroscopy. X-ray analysis of 2 showed that the rhenium atom is pentacoordinate presenting a distorted square-pyramidal coordination geometry. The analogous oxotechnetium-99m complex 4 was also prepared quantitatively by the reaction of ligand 1 with Na99mTcO4 in isotonic saline using tin chloride as reducing agent. Its identity was established by chromatographic comparison to the oxorhenium 2 and oxotechnetium 3 complexes. © Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003.

A series of (TcO)-Tc-99m[SN(R)S][S] complexes carrying the 1-(2-methoxyphenyl)piperazine moiety on the tridentate ligand [SN(R)S] was synthesized. For structural characterization and for in vitro binding assays the analogous oxorhenium complexes were prepared. As demonstrated by appropriate competition binding tests in rat hippocampal preparations, all oxorhenium analogues showed affinity for the 5-HT1A receptor binding sites with IC50 values at the nanomolar range (IC50 = 5.8-103 nM). All (TcO)-Tc-99m[SN(R)S]/[S] complexes showed significant brain uptake in rats at 2 min p.i. (0.24-1.31% ID). However, a clear correlation between distribution of radioactivity in the brain and distribution of 5-HT1A receptors could not be established. (C) 2002 Elsevier Science Inc. All rights reserved.

Theoretically, the reaction of the tridentate aminedithiol ligand EtN(CH2CH2SH)2, L1H2, and the monodentate thiol 4-ClC6H4SH, L2H, with the ReVOCl3(PPh3)2 may lead to the formation of the following complexes: (i) neutral mixed ligand complexes ReOL1L2 (the syn isomer, complex 1 and the anti isomer, complex 2, (ii) binuclear complex of the tridentate ligand, (MO)2(L1)3, complex 3, and (iii) anionic complex of the monothiol [MO(L2)4]-, complex 4. When a mixture of L1H2/L2H, 1/1 ratio, is applied, the major product of the reaction is the syn isomer 1. A small amount of the anti isomer 2 is also isolated (yield < 2 %) while none of the complexes 3 and 4 form during the reaction under the above conditions. The oxorhenium complexes 3 and 4 have been synthesized by the reaction of L1H2 or L2H with the precursor ReOCl3(PPh3)2. The crystal structure of 1, 3, and 4 is determined by X-ray crystallography. The corresponding Tc-99m complexes have been prepared by exchange reaction using Tc-99m glucoheptonate as precursor. Similarly the major reaction product is the syn isomer, complex 1´, while none of the other complexes form during the reaction at tracer level. The above studies demonstrate that simultaneous action of a tridentate SNS ligand and a monodentate thiol in equimolar quantities on ReVOCl3(PPh3)2 or Tc-99m glucoheptonate leads to a single rhenium or technetium-99m species, the syn MOL1L2.

Our work over the past few years has been focused on the design and evaluation of novel chelating systems suitable for oxorhenium and/or oxotechnetium that may lead to useful radioagents. Several 99mTc mixed ligand complexes carrying the SNS/S or the SNN/S donor atom set have shown promising biological properties for future application. The in vivo stability and thereby biological properties of these complexes is greatly dependent on the electronic and lipophilic character of the monothiol. We report here on the comparative resistance to cysteine substitution of two parallel series of 99mTcO{[Et2NCH2CH2N(CH2CH2S)2](p-RPhS)} and 99mTcO-[(Et2NCH2CH2NCH2CH2S) (p-RPhS)] complexes wherein the phenyl monothiolate coligand is substituted in the p-position by R: -NH2 (electron donating group), -H and NO2 (electron withdrawing group). The electronic influence on cysteine substitution rate can thus be investigated. All above complexes are prepared at tracer level using glucoheptonate as transfer ligand and are purified by organic extraction and HPLC. Their structure has been previously resolved by comparison with authentic samples. The 99mTc complexes are stable in solution in the absence of thiol for long periods of time. Competition experiments with cysteine are performed in aqueous medium at pH 7.4 and using two different cysteine concentrations, 10 mM and 1 mM, by incubation at 37°C. Aliquots of the incubate withdrawn at 0, 15, 30, 60, 120 min and 24 h time intervals are subjected to HPLC analysis. A RP C18 column is eluted by TEAP buffer pH 7.4/EtOH gradient system, whereby all radioactive ingredients are well separated. All complexes are attacked by cysteine under the above conditions forming mixtures of intermediates, that with time lead to total loss of the original 99mTc compounds. Relative resistance to cysteine substitution is directly proportional to monothiol nucleophilicity in both series of complexes: -NH2 > -H> -NO2. Since the free thiol content - mainly cysteine and its derivatives - varries in vivo, mixed ligand systems as the above can be used for directing and trapping 99mTc in tissues of choice by finely monitoring stability via the monothiol.