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An elemental function of brain dopamine is to coordinate cognitive and motor resources for successful exploitation of environmental energy sources. Dopamine transmission, goal-directed behavior, and glucose homeostasis are altered in schizophrenia patients prior to and after initiation of pharmacological treatment. Thus, we investigated the relationship between blood glucose levels and brain dopamine signaling in drug-naïve patients with first-episode psychosis.We quantified blood glucose levels and binding of the dopamine D2/3 receptor agonist radioligand (+)-[11C]-PHNO in 15 medication-naïve patients and 27 healthy volunteers employing positron emission tomography.Whole-brain voxel-wise linear model analysis identified two clusters of significant interaction between blood glucose levels and diagnosis on (+)-[11C]-PHNO binding-potential values. We observed positive relationships between blood glucose levels and binding-potential values in healthy volunteers but negative ones in patients with first episode psychosis in a cluster surviving rigorous multiple testing correction located in the in the right ventral tegmental area. Another cluster of homologous behavior, however at a lower level of statistical significance, comprised the ventral striatum and pallidum. Extracellular dopamine levels are a major determinant of (+)-[11C]-PHNO binding in the brain. In line with the concept that increased dopamine signaling occurs when goal-directed behavior is needed for restoring energy supply, our data indicate that in healthy volunteers, extracellular dopamine levels are high when blood glucose levels are low and vice-versa. This relationship is reversed in patients with first-episode psychosis, possibly reflecting an underlying pathogenic alteration that links two seemingly unrelated aspects of the illness: altered dopamine signaling and dysfunctional glucose homeostasis.

Table of contentsA1 68Ga-PSMA PET/CT in staging and restaging of Prostate Cancer Patients: comparative study with 18F-Choline PET/CTW Langsteger, A Rezaee, W Loidl, HS Geinitz, F Fitz, M Steinmair, G Broinger, L Pallwien-Prettner, M BeheshtiA2 F18 Choline PET - CT: an accurate diagnostic tool for the detection of parathyroid adenoma?L Imamovic, M Beheshti, G Rendl, D Hackl, O Tsybrovsky, M Steinmair, K Emmanuel, F Moinfar, C Pirich, W LangstegerA3 [18F]Fluoro-DOPA-PET/CT in the primary diagnosis of medullary thyroid carcinomaA Bytyqi, G Karanikas, M Mayerhöfer, O Koperek, B Niederle, M HartenbachA4 Variations of clinical PET/MR operations: An international survey on the clinical utilization of PET/MRIT Beyer, K Herrmann, J CzerninA5 Standard Dixon-based attenuation correction in combined PET/MRI: Reproducibility and the possibility of Lean body mass estimationI Rausch, P Rust, MD DiFranco, M Lassen, A Stadlbauer, ME Mayerhöfer, M Hartenbach, M Hacker, T BeyerA6 High resolution digital FDG PET/MRI imaging for assessment of ACL graft viabilityK Binzel, R Magnussen, W Wei, MU Knopp, DC Flanigan, C Kaeding, MV KnoppA7 Using pre-existing hematotoxicity as predictor for severe side effects and number of treatment cycles of Xofigo therapyA Leisser, M Nejabat, M Hartenbach, G Kramer, M Krainer, M Hacker, A HaugA8 QDOSE - comprehensive software solution for internal dose assessmentWencke Lehnert, Karl Schmidt, Sharok Kimiaei, Marcus Bronzel, Andreas KlugeA9 Clinical impact of Time-of-Flight on next-generation digital PET imaging of Yttrium-90 radioactivity following liver radioembolizationCL Wright, K Binzel, J Zhang, Evan Wuthrick, Piotr Maniawski, MV KnoppA10 Snakes in patients! Lessons learned from programming active contours for automated organ segmentationM Blaickner, E Rados, A Huber, M Dulovits, H Kulkarni, S Wiessalla, C Schuchardt, RP Baum, B Knäusl, D GeorgA11 Influence of a genetic polymorphism on brain uptake of the dual ABCB1/ABCG2 substrate [11C]tariquidarM Bauer, B Wulkersdorfer, W Wadsak, C Philippe, H Haslacher, M Zeitlinger, O LangerA12 Outcome prediction of temporal lobe epilepsy surgery from P-glycoprotein activity. Pooled analysis of (R)-[11C]-verapamil PET data from two European centresM Bauer, M Feldmann, R Karch, W Wadsak, M Zeitlinger, MJ Koepp, M-C Asselin, E Pataraia, O LangerA13 In-vitro and in-vivo characterization of [18F]FE@SNAP and derivatives for the visualization of the melanin concentrating hormone receptor 1M Zeilinger, C Philippe, M Dumanic, F Pichler, J Pilz, M Hacker, W Wadsak, M MitterhauserA14 Reducing time in quality control leads to higher specific radioactivity of short-lived radiotracersL Nics, B Steiner, M Hacker, M Mitterhauser, W WadsakA15 In vitro 11C-erlotinib binding experiments in cancer cell lines with epidermal growth factor receptor mutationsA Traxl, Thomas Wanek, Kushtrim Kryeziu, Severin Mairinger, Johann Stanek, Walter Berger, Claudia Kuntner, Oliver LangerA16 7-[11C]methyl-6-bromopurine, a PET tracer to measure brain Mrp1 function: radiosynthesis and first PET evaluation in miceS Mairinger, T Wanek, A Traxl, M Krohn, J Stanek, T Filip, M Sauberer, C Kuntner, J Pahnke, O LangerA17 18F labeled azidoglucose derivatives as "click" agents for pretargeted PET imagingD Svatunek, C Denk, M Wilkovitsch, T Wanek, T Filip, C Kuntner-Hannes, J Fröhlich, H MikulaA18 Bioorthogonal tools for PET imaging: development of radiolabeled 1,2,4,5-TetrazinesC Denk, D Svatunek, T Wanek, S Mairinger, J Stanek, T Filip, J Fröhlich, H Mikula, C Kuntner-HannesA19 Preclinical evaluation of [18F]FE@SUPPY- a new PET-tracer for oncologyT Balber, J Singer, J Fazekas, C Rami-Mark, N Berroterán-Infante, E Jensen-Jarolim, W Wadsak, M Hacker, H Viernstein, M MitterhauserA20 Investigation of Small [18F]-Fluoroalkylazides for Rapid Radiolabeling and In Vivo Click ChemistryC Denk, D Svatunek, B Sohr, H Mikula, J Fröhlich, T Wanek, C Kuntner-Hannes, T FilipA21 Microfluidic 68Ga-radiolabeling of PSMA-HBED-CC using a flow-through reactorS Pfaff, C Philippe, M Mitterhauser, M Hartenbach, M Hacker, W WadsakA22 Influence of 24-nor-ursodeoxycholic acid on hepatic disposition of [18F]ciprofloxacin measured with positron emission tomographyT Wanek, E Halilbasic, M Visentin, S Mairinger, B Stieger, C Kuntner, M Trauner, O LangerA23 Automated 18F-flumazenil production using chemically resistant disposable cassettesP Lam, M Aistleitner, R Eichinger, C ArtnerA24 Similarities and differences in the synthesis and quality control of 177Lu-DOTA-TATE, 177Lu -HA-DOTA-TATE and 177Lu-DOTA-PSMA (PSMA-617)H Eidherr, C Vraka, A Haug, M Mitterhauser, L Nics, M Hartenbach, M Hacker, W WadsakA25 68Ga- and 177Lu-labelling of PSMA-617H Kvaternik, R Müller, D Hausberger, C Zink, RM AignerA26 Radiolabelling of liposomes with 67Ga and biodistribution studies after administration by an aerosol inhalation systemU Cossío, M Asensio, A Montes, S Akhtar, Y te Welscher, R van Nostrum, V Gómez-Vallejo, J LlopA27 Fully automated quantification of DaTscan SPECT: Integration of age and gender differencesF VandeVyver, T Barclay, N Lippens, M TrochA28 Lesion-to-background ratio in co-registered 18F-FET PET/MR imaging - is it a valuable tool to differentiate between low grade and high grade brain tumor?L Hehenwarter, B Egger, J Holzmannhofer, M Rodrigues-Radischat, C PirichA29 [11C]-methionine PET in gliomas - a retrospective data analysis of 166 patientsN Pötsch, I Rausch, D Wilhelm, M Weber, J Furtner, G Karanikas, A Wöhrer, M Mitterhauser, M Hacker, T Traub-WeidingerA30 18F-Fluorocholine versus 18F-Fluorodeoxyglucose for PET/CT imaging in patients with relapsed or progressive multiple myeloma: a pilot studyT Cassou-Mounat, S Balogova, V Nataf, M Calzada, V Huchet, K Kerrou, J-Y Devaux, M Mohty, L Garderet, J-N TalbotA31 Prognostic benefit of additional SPECT/CT in sentinel lymph node mapping of breast cancer patientsS Stanzel, G Pregartner, T Schwarz, V Bjelic-Radisic, B Liegl-Atzwanger, R AignerA32 Evaluation of diagnostic value of TOF-18F-FDG PET/CT in patients with suspected pancreatic cancerS Stanzel, F Quehenberger, RM AignerA33 New quantification method for diagnosis of primary hyperpatahyroidism lesions and differential diagnosis vs thyropid nodular disease in dynamic scintigraphyA Koljević Marković, Milica Janković, V Miler Jerković, M Paskaš, G Pupić, R Džodić, D PopovićA34 A rare case of diffuse pancreatic involvement in patient with merkel cell carcinoma detected by 18F-FDGMC Fornito, D FamiliariA35 TSH-stimulated 18F-FDG PET/CT in the diagnosis of recurrent/metastatic radioiodine-negative differentiated thyroid carcinomas in patients with various thyroglobuline levelsP Koranda, H Polzerová, I Metelková, L Henzlová, R Formánek, E Buriánková, M KamínekA36 Breast Dose from lactation following I131 treatmentWH Thomson, C LewisA37 A new concept for performing SeHCAT studies with the gamma cameraWH Thomson, J O'Brien, G James, A NotghiA38 Whole body F-18-FDG-PET and tuberculosis: sensitivity compared to x-ray-CTH Huber, I Stelzmüller, R Wunn, M Mandl, F Fellner, B Lamprecht, M GabrielA39 Emerging role 18F-FDG PET-CT in the diagnosis and follow-up of the infection in heartware ventricular assist system (HVAD)MC Fornito, G LeonardiA40 Validation of Poisson resampling softwareWH Thomson, J O'Brien, G JamesA41 Protection of PET nuclear medicine personnel: problems in satisfying dose limit requirementsJ Hudzietzová, J Sabol, M Fülöp.

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 [F]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 Cu-NOTA-pertuzumab F(ab') 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 [F]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 [Ga]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 O-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 [F]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, С.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 F-labeled PEtOx in comparison to Zr-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 mTc(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 [F]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 [ABSTRACT FROM AUTHOR]

This report explores the potential of novel 6-aryloxy-2-aminopyrimidine-benzonitrile scaffolds as promising anti-infective agents in the face of the increasing threat of infectious diseases. Starting from 2-amino-4,6-dichloropyrimidine, a series of 24 compounds inspired from the antiviral drugs dapivirine, etravirine, and rilpivirine were designed and synthesized via a two-step reaction sequence in good yields. Biological testing of synthetic analogs revealed potent inhibition against both viral and tuberculosis targets. Notably, compounds 5p (2,4-dimethyl substitution; IC 50  = 44 ± 4.9 µM; selectivity index [SI] = 20) and 5 s (3-thiophenphenyl; IC 50  = 6 ± 1 µM; SI = 120) showed significant antiviral activity against pandemic influenza virus A/Puerto Rico/8/34 (H1N1) with positive toxicity profiles and also exhibited good IC 50 values (5p, IC 50  = 10 ± 2 µM; SI = 9 and 5 s, IC 50  = 16 ± 2 µM; SI = 60) against the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) (Wuhan strain) compared with favipiravir. In addition, analogs 5a, 5r, 5t, and 5u showed good antitubercular activity against Mycobacterium tuberculosis H37Rv strain and compounds 3, 5f, 5n, and 5q showed moderate antibacterial activity against gram+ve and gram-ve bacterial strains, suggesting that this scaffold has a broad spectrum of therapeutic effects., (© 2024 Deutsche Pharmazeutische Gesellschaft.)

Purpose: Positron emission tomography (PET) provides precise molecular information on physiological processes, but its low temporal resolution is a major obstacle. Consequently, we characterized the metabolic response of the human brain to working memory performance using an optimized functional PET (fPET) framework at a temporal resolution of 3 s. Methods: Thirty-five healthy volunteers underwent fPET with [18F]FDG bolus plus constant infusion, 19 of those at a hybrid PET/MRI scanner. During the scan, an n-back working memory paradigm was completed. fPET data were reconstructed to 3 s temporal resolution and processed with a novel sliding window filter to increase signal to noise ratio. BOLD fMRI signals were acquired at 2 s. Results: Consistent with simulated kinetic modeling, we observed a constant increase in the [18F]FDG signal during task execution, followed by a rapid return to baseline after stimulation ceased. These task-specific changes were robustly observed in brain regions involved in working memory processing. The simultaneous acquisition of BOLD fMRI revealed that the temporal coupling between hemodynamic and metabolic signals in the primary motor cortex was related to individual behavioral performance during working memory. Furthermore, task-induced BOLD deactivations in the posteromedial default mode network were accompanied by distinct temporal patterns in glucose metabolism, which were dependent on the metabolic demands of the corresponding task-positive networks. Conclusions: In sum, the proposed approach enables the advancement from parallel to truly synchronized investigation of metabolic and hemodynamic responses during cognitive processing. This allows to capture unique information in the temporal domain, which is not accessible to conventional PET imaging. [ABSTRACT FROM AUTHOR]

Positron emission tomography (PET) is a powerful diagnostic tool that holds incredible potential for clinicians to track a wide variety of biological processes using specialized radiotracers. Currently, however, a single radiotracer accounts for over 95% of procedures, largely due to the cost of radiotracer synthesis. Microfluidic platforms provide a solution to this problem by enabling a dose-on-demand pipeline in which a single benchtop platform would synthesize a wide array of radiotracers. In this review, we will explore the field of microfluidic production of radiotracers from early research to current development. Furthermore, the benefits and drawbacks of different microfluidic reactor designs will be analyzed. Lastly, we will discuss the various engineering considerations that must be addressed to create a fully developed, commercially effective platform that can usher the field from research and development to commercialization. [ABSTRACT FROM AUTHOR]

Fluorine‐18 (18F) is the most favorable positron emitter for radiolabeling Positron Emission Tomography (PET) probes. However, conventional 18F labeling through covalent C−F bond formation is challenging, involving multiple steps and stringent conditions unsuitable for sensitive biomolecular probes whose integrity may be altered. Over the past decade, an elegant new approach has been developed involving the coordination of an aluminum fluoride {Al18F} species in aqueous media at a late‐stage of the synthetic process. The objective of this study was to implement this method and to optimize radiolabeling efficiency using a Design of Experiments (DoE). To assess the impact of various experimental parameters on {Al18F} incorporation, a pentadentate chelating agent NODA‐MP‐C4 was prepared as a model compound. This model carried a thiourea function present in the final conjugates resulting from the grafting of the chelating agent onto the probe. The formation of the radioactive complex Al18F‐NODA‐MP‐C4 was studied to achieve the highest radiochemical conversion. A complementary "cold" series study using the natural isotope 19F was also conducted to guide the radiochemical operating conditions. Ultimately, Al18F‐NODA‐MP‐C4 was obtained with a reproducible and satisfactory radiochemical conversion of 79±3.5 % (n=5). [ABSTRACT FROM AUTHOR]

This study examines how two popular drug‐likeness concepts used in early development, Lipinski Rule of Five (Ro5) and Veber's Rules, possibly affected drug profiles of FDA approved drugs since 1997. Our findings suggest that when all criteria are applied, relevant compounds may be excluded, addressing the harmfulness of blindly employing these rules. Of all oral drugs in the period used for this analysis, around 66 % conform to the RO5 and 85 % to Veber's Rules. Molecular Weight and calculated LogP showed low consistent values over time, apart from being the two least followed rules, challenging their relevance. On the other hand, hydrogen bond related rules and the number of rotatable bonds are amongst the most followed criteria and show exceptional consistency over time. Furthermore, our analysis indicates that topological polar surface area and total count of hydrogen bonds cannot be used as interchangeable parameters, contrary to the original proposal. This research enhances the comprehension of drug profiles that were FDA approved in the post‐Lipinski period. Medicinal chemists could utilize these heuristics as a limited guide to direct their exploration of the oral bioavailability chemical space, but they must also steer the wheel to break these rules and explore different regions when necessary. [ABSTRACT FROM AUTHOR]

The increasing exposure to nanoplastics (NPs) raises significant concerns for human health, primarily due to their potential bioaccumulative properties. While NPs have recently been detected in human blood, their interactions with specific immune cell subtypes and their impact on immune regulation remain unclear. In this proof-of-concept study, model palladium-doped polystyrene NPs (PS-Pd NPs) are utilized to enable single-cell mass cytometry (CyTOF) detection. The size-dependent impact of carboxylate polystyrene NPs (50-200 nm) is investigated across 15 primary immune cell subpopulations using CyTOF. By taking advantage of Pd-doping for detecting PS-Pd NPs, this work evaluates their impact on human immune-cells at the single-cell level following blood exposure. This work traces PS-Pd NPs in 37 primary immune-cell subpopulations from human blood, quantifying the palladium atom count per cell by CyTOF while simultaneously assessing the impact of PS-Pd NPs on cell viability, functionality, and uptake. These results demonstrate that NPs can interact with, interfere with, and translocate into several immune cell subpopulations after exposure. In vivo distribution experiments in mice further confirmed their accumulation in immune cells within the liver, blood, and spleen, particularly in monocytes, macrophages, and dendritic cells. These findings provide valuable insights into the impact of NPs on human health., (© 2024 The Author(s). Advanced Materials published by Wiley‐VCH GmbH.)

This research presents the development of positron emission tomography (PET) radiotracers for detecting Mycobacterium tuberculosis (MTB) for the diagnosis and monitoring of tuberculosis. Two phage display-derived peptides with proven selective binding to MTB were identified for development into PET radiopharmaceuticals: H8 (linear peptide) and PH1 (cyclic peptide). We sought to functionalize H8/PH1 with NODASA, a bifunctional chelator that allows complexation of PET-compatible radiometals such as gallium-68. Herein, we report on the chelator functionalization, optimized radiosynthesis, and assessment of the radiopharmaceutical properties of [ 68 Ga]Ga-NODASA-H8 and [ 68 Ga]Ga-NODASA-PH1. Robust radiolabeling was achieved using the established routine method, indicating consistent production of a radiochemically pure product (RCP ≥ 99.6%). For respective [ 68 Ga]Ga-NODASA-H8 and [ 68 Ga]Ga-NODASA-PH1, relatively high levels of decay-corrected radiochemical yield (91.2% ± 2.3%, 86.7% ± 4.0%) and apparent molar activity (A m , 3.9 ± 0.8 and 34.0 ± 5.3 GBq/μmol) were reliably achieved within 42 min, suitable for imaging purposes. Notably, [ 68 Ga]Ga-NODASA-PH1 remained stable in blood plasma for up to 2 h, while [ 68 Ga]Ga-NODASA-H8 degraded within 30 min. For both 68 Ga peptides, minimal whole-blood cell binding and plasma protein binding were observed, indicating a favorable pharmaceutical behavior. [ 68 Ga]Ga-NODASA-PH1 is a promising candidate for further in vitro/in vivo evaluation as a tuberculosis-specific infection imaging agent., (© 2024 The Author(s). Journal of Labelled Compounds and Radiopharmaceuticals published by John Wiley & Sons Ltd.)

A set of 211 At-astatoarenes were synthesized from corresponding trimethylgermyl arenes with an average radiochemical conversion (RCC) of ca. 50 % for electron-rich and approx. 70 % in case of electron-deficient arenes. Both electron rich and electron poor substrates were successfully radiolabeled at room temperature (RT) using relatively low precursor amounts (0.15 μmol/0.02 mL solvent (7.5 mM)). Ready access to ortho-, para- and meta- astatinated arenes was achievable. Optimized reaction conditions were successfully applied to label a poly (ADP-ribose) polymerase (PARP) inhibitor with a RCC of approx. 50 %. We believe that trimethylgermyl derivatives are a viable addition to the astatination precursor toolbox and facilitate astatination of arenes. The developed labeling method should easily be applicable for productions under good manufacturing practice (GMP)., (© 2024 The Authors. ChemPlusChem published by Wiley-VCH GmbH.)

The human microbiome significantly influences drug metabolism through the gut-liver axis, leading to modified drug responses and potential toxicity. Due to the complex nature of the human gut environment, the understanding of microbiome-driven impacts on these processes is limited. To address this, a multiorgan-on-a-chip (MOoC) platform that combines the human microbial-crosstalk (HuMiX) gut-on-chip (GoC) and the Dynamic42 liver-on-chip (LoC), mimicking the bidirectional interconnection between the gut and liver known as the gut-liver axis, is introduced. This platform supports the viability and functionality of intestinal and liver cells. In a proof-of-concept study, the metabolism of irinotecan, a widely used colorectal cancer drug, is imitated within the MOoC. Utilizing liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS), irinotecan metabolites are tracked, confirming the platform's ability to represent drug metabolism along the gut-liver axis. Further, using the authors' gut-liver platform, it is shown that the colorectal cancer-associated gut bacterium, Escherichia coli, modifies irinotecan metabolism through the transformation of its inactive metabolite SN-38G into its toxic metabolite SN-38. This platform serves as a robust tool for investigating the intricate interplay between gut microbes and pharmaceuticals, offering a representative alternative to animal models and providing novel drug development strategies., (© 2024 The Authors. Advanced Healthcare Materials published by Wiley‐VCH GmbH.)

Radioimmunoconjugates (RICs) composed of tumor-targeting monoclonal antibodies and radionuclides have been developed for diagnostic and therapeutic application. A new radiolabeling method using microfluidic devices is expected to facilitate simpler and more rapid synthesis of RICs. In the microfluidic method, microfluidic chips can promote the reaction between reactants by mixing them efficiently, and pumping systems enable automated synthesis. In this study, we synthesized RICs by the pre-labeling method, in which the radiometal is coordinated to the chelator and then the radiolabeled chelator is incorporated into the antibodies, using microfluidic devices for the first time. As a result of examining the reaction parameters including the material of mixing units, reaction temperature, and flow rate, RICs with radiochemical purity (RCP) exceeding 90% were obtained. These high-purity RICs were successfully synthesized without any purification simply by pumping three solutions of a chelating agent, radiometal, and antibody into microfluidic devices. Under the same conditions, the RCP of RICs labeled by conventional methods was below 50%. These findings indicate the utility of microfluidic devices for automatic and rapid synthesis of high-quality RICs., (© 2024 John Wiley & Sons Ltd.)

Thirteen commercial Tasmanian essential oils were evaluated for their antimicrobial activity against 14 human pathogens and cosmetic contaminants including Enterococcus hirae, Kocuria rhizophila, Staphylococcus epidermidis, Propionibacterium acnes, Staphylococcus aureus, Escherichia coli, Klebsiella aerogenes, Klebsiella pneumoniae, Pluralibacter gergoviae, Pseudomonas fluorescens, Burkholderia cepacia, Pseudomonas putida, Aspergillus brasiliensis, and Aspergillus fumigatus. The antimicrobial activities of various essential oils were evaluated using the AlamarBlue Cell Viability Assay, covering a testing concentration range from 3.125 to 800 µg/mL. Essential oils were deemed active if their minimum inhibitory concentration (MIC) value was less than or equal to 800 µg/mL. The essential oils of Rosemary (Rosmarinus officinalis ct. α-pinene), Parsley Herb (Petroselinum crispum), and Bitter Fennels (Foeniculum vulgare) demonstrated significant growth inhibitory effects on one microorganism (P. fluorescens) within an MIC value of ≤ 800 µg/mL. Big Badja Gum (Eucalyptus badjensis), Blue Gum (Eucalyptus globulus), Peppermint (Mentha piperita), and Lavender (Lavandula angustifolia) essential oils inhibited the growth of two different microorganisms. Southern Rosalina (Melaleuca ericifolia), Parsley Seed (Petroselinum crispum), Smoky Tea Tree (Leptospermum glaucescens), and Kunzea (Kunzea ambigua) essential oils exhibited an MIC value of less than or equal to 800 µg/mL against 4, 5, 6, and 8 microorganisms respectively. Notably, Coastal Tea Tree (Leptospermum laevigatum) essential oil displayed the most profound antimicrobial activity, inhibiting 11 out of 15 microbial strains within an MIC range of 50–800 µg/mL. The results of the gas chromatography analysis showed that the coastal tea tree essential oil was composed primarily of monoterpenes, with smaller amounts of sesquiterpenes and their oxygenated derivatives. 35 Compounds were identified, representing 95.50% of the compounds in the coastal tea tree essential oil. The main constituents of this essential oil were α-pinene (34.83%), followed by α- and β-eudesmols (10.21% total), and limonene (9.56%). [ABSTRACT FROM AUTHOR]

Positron emission tomography (PET) is a powerful imaging tool for drug discovery, clinical diagnosis, and monitoring of disease progression. Fluorine‐18 is the most common radionuclide used for PET, but advances in radiotracer development have been limited by the historical lack of methodologies and precursors amenable to radiolabeling with fluorine‐18. Radiolabeling of electron‐rich (hetero)aromatic rings remains a long‐standing challenge in the production of PET radiopharmaceuticals. In this personal account, we discuss the history of spirocyclic iodonium ylide precursors, from inception to applications in clinical research, for the incorporation of fluorine‐18 into complex non‐activated (hetero)aromatic rings. [ABSTRACT FROM AUTHOR]

Multimodal classification research has been gaining popularity with new datasets in domains such as satellite imagery, biometrics, and medicine. Prior research has shown the benefits of combining data from multiple sources compared to traditional unimodal data that has led to the development of many novel multimodal architectures. However, the lack of consistent terminologies and architectural descriptions makes it difficult to compare different solutions. We address these challenges by proposing a new taxonomy for describing multimodal classification models based on trends found in recent publications. Examples of how this taxonomy could be applied to existing models are presented as well as a checklist to aid in the clear and complete presentation of future models. Many of the most difficult aspects of unimodal classification have not yet been fully addressed for multimodal datasets, including big data, class imbalance, and instance-level difficulty.We also provide a discussion of these challenges and future directions of research. [ABSTRACT FROM AUTHOR]

Background: Adrenal masses are commonly encountered in clinical practice, many of whom are incidental. Identifying malignancy, and excess hormone production is essential for appropriate management. Biochemical workup and imaging tests (dedicated adrenal CT and/or MRI) are used to determine the likelihood of excessive hormone function and malignancy, respectively. However, imaging cannot provide information about function and biochemical workup cannot localize the source. Furthermore, in primary aldosteronism, adrenal vein sampling, the gold standard for lateralization, has important limitations such as the technical expertise required, the elevated costs, and potential complications. Over the last decades, there has been a renewed interest in alternative noninvasive imaging techniques that provide information about adrenal function without the need for invasive procedures. In this review, we will evaluate the evidence and the potential role of 11 C-metomidate as a promising positron emission tomography (PET) tracer in clinical practice., Methods: A review of the English literature for articles describing the use of the tracer 11 C-metomidate in adrenal disorders., Results: A total of 12 studies were included in the systematic review, which altogether addressed the use of 11 C-metomidate in adrenal masses and the application of this tracer in primary aldosteronism., Conclusions: 11 C-metomidate, a selective inhibitor of 11-β-hydroxylase, demonstrated a high specificity for adrenocortical tissue. In addition, 11 C-metomidate is correlated with this enzyme activity making it a potentially useful PET tracer for the identification primary aldosteronism, in addition to detection of adrenocortical masses.

Positron emission tomography (PET) is becoming increasingly important in nuclear medicine and drug discovery. To date, the development of many potential PET tracers is hampered by the lack of suitable synthetic pathways for their preparation. This is particularly true for the highly desired radiolabeling of compounds bearing [ 18 F]CF 3 -groups. For instance, S(O) n CF 3 -groups (n=0, 1, 2) serve as structural motif in a range of biologically active compounds, but their radiosynthesis remains largely unprecedented (for n=1, 2). Herein, we describe general methods for the radiosynthesis of 18 F-labeled aryl trifluoromethyl sulfones, -sulfoxides, and -sulfides. All three methods are operationally straightforward, start from widely available precursors, i.e., sulfonyl fluorides and thiophenols, and make use of the recently established [ 18 F]Ruppert-Prakash reagent. Further, the syntheses display good functional group tolerance as demonstrated by the 18 F-labeling of more than 40 compounds. The applicability of the new method is demonstrated by the radiolabeling of three bioactive molecules, optionally to be used as PET tracers. In a broader context, this work presents a substantial expansion of the chemical space of radiofluorinated structural motifs to be used for the development of new PET tracers., (© 2024 The Authors. Angewandte Chemie International Edition published by Wiley-VCH GmbH.)

α,β-aromatic lactams are highly abundant in biologically active molecules, yet so far they cannot be radiolabeled with short-lived (t 1/2 =20.3 min), β + -decaying carbon-11, which has prevented their application as positron emission tomography tracers. Herein, we developed, optimized, and applied a widely applicable, one-pot, quick, robust and automatable radiolabeling method for α,β-aromatic lactams starting from [ 11 C]CO 2 using the reagent POCl 3 ⋅AlCl 3 . This method proceeds via intramolecular Friedel-Crafts acylation of in situ formed [ 11 C]isocyanates and shows a broad substrate scope for the formation of five- and six-membered rings. We implemented our developed labeling method for the radiosynthesis of the potential PARP1 PET tracer [carbonyl- 11 C]DPQ in a clinical radiotracer production facility following the standards of the European Pharmacopoeia., (© 2024 The Authors. Chemistry - A European Journal published by Wiley-VCH GmbH.)