Investigation of an F-18 oxytocin receptor selective ligand via PET imaging

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:23

Article

Smith, Aaron L.^1,2  Freeman, Sara M.²  Voll, Ronald J.¹  Young, Larry J.²  Goodman, Mark M.¹ 

[1] Emory Univ, Dept Radiol & Imaging Sci, Atlanta, GA 30329 USA

[2] Yerkes Natl Primate Res Ctr, Dept Psychiat & Behav Sci, Ctr Translat Social Neurosci, Atlanta, GA 30322 USA

关键词: Oxytocin;    Oxytocin receptor;    Receptor imaging;    Fluorine-18;    PET imaging;    Cerebral ventricles;    Choroid plexus;    Alpha-1 adrenergic receptor;    Adrenergic receptor;   

DOI  :  10.1016/j.bmcl.2013.07.045

来源: Elsevier

【 摘 要 】

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. (C) 2013 Published by Elsevier Ltd.

【 授权许可】

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