[¹⁸F]MK-9470, a positron emission tomography (PET) tracer for in vivo human PET brain imaging of the cannabinoid-1 receptor

• Published in: Proceedings of the National Academy of Sciences - PNAS Vol. 104; no. 23; pp. 9800 - 9805
• Main Authors: Burns, H. Donald, Van Laere, Koen, Sanabria-Bohórquez, Sandra, Hamill, Terence G, Bormans, Guy, Eng, Wai-si, Gibson, Ray, Ryan, Christine, Connolly, Brett, Patel, Shil, Krause, Stephen, Vanko, Amy, Van Hecken, Anne, Dupont, Patrick, De Lepeleire, Inge, Rothenberg, Paul, Stoch, S. Aubrey, Cote, Josee, Hagmann, William K, Jewell, James P, Lin, Linus S, Liu, Ping, Goulet, Mark T, Gottesdiener, Keith, Wagner, John A, de Hoon, Jan, Mortelmans, Luc, Fong, Tung M, Hargreaves, Richard J
• Format: Journal Article
• Language: English
• Published: United States National Academy of Sciences 05.06.2007; National Acad Sciences
• Subjects: Agonists; Amides - metabolism; Animals; Autoradiography; Biological Sciences; Boluses; Brain; Brain - anatomy & histology; Brain - metabolism; Brain research; cannabinoids; Cerebellum; cerebral cortex; clinical trials; Dosage; drugs; Emissions; Fluorine Radioisotopes; hippocampus; Humans; image analysis; Image Processing, Computer-Assisted; Imaging; in vivo studies; inhibitory concentration 50; Macaca mulatta; Male; males; Molecular Structure; Monkeys; Monkeys & apes; Neuroimaging; Neurology; Pharmacology; Placebos; Positron emission tomography; Positron-Emission Tomography - methods; Pyridines - metabolism; Radioactive Tracers; Receptor, Cannabinoid, CB1 - metabolism; Receptor, Cannabinoid, CB1 - ultrastructure; Receptors; Tomography

[¹⁸F]MK-9470 is a selective, high-affinity, inverse agonist (human IC₅₀, 0.7 nM) for the cannabinoid CB1 receptor (CB1R) that has been developed for use in human brain imaging. Autoradiographic studies in rhesus monkey brain showed that [¹⁸F]MK-9470 binding is aligned with the reported distribution...