title: Investigation of an F-18 oxytocin receptor selective ligand via PET imaging.
abstract: The compound 1-(1-(2-(2-(2-fluoroethoxy)-4-(piperidin-4-yloxy)phenyl)acetyl)piperidin-4-yl)-3,4-dihydroquinolin-2(1H)-one (1) was synthesized and positively evaluated in vitro for high potency and selectivity with human oxytocin receptors. The positron emitting analogue, [F-18]1, was synthesized and investigated in vivo via PET imaging using rat and cynomolgus monkey models. PET imaging studies in female Sprague-Dawley rats suggested [F-18]1 reached the brain and accumulated in various regions of the brain, but washed out too rapidly for adequate quantification and localization. In vivo PET imaging studies in a male cynomolgus monkey suggested [F-18]1 had limited brain penetration while specific uptake of radioactivity significantly accumulated within the vasculature of the cerebral ventricles in areas representative of the choroid plexus.
authors: Department of Radiology and Imaging Sciences, Emory University, Atlanta, GA 30329, United States.
authors: Aaron L
authors: AL
authors: Smith
authors: Sara M
authors: SM
authors: Freeman
authors: Ronald J
authors: RJ
authors: Voll
authors: Larry J
authors: LJ
authors: Young
authors: Mark M
authors: MM
authors: Goodman
mesh_terms: D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging; D002478:Cells, Cultured; D002851:Chromatography, High Pressure Liquid; D005260:Female; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D006801:Humans; D008024:Ligands; D008252:Macaca fascicularis; D008297:Male; D023421:Models, Animal; D049268:Positron-Emission Tomography; D051381:Rats; D017207:Rats, Sprague-Dawley; D018045:Receptors, Oxytocin / Q000737:chemistry*
chemical_list: D005462:Fluorine Radioisotopes; D008024:Ligands; D018045:Receptors, Oxytocin
keywords: Adrenergic receptor; Alpha-1 adrenergic receptor; Cerebral ventricles; Choroid plexus; Fluorine-18; Oxytocin; Oxytocin receptor; PET imaging; Receptor imaging
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