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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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Smith AL,Freeman SM,Voll RJ,Young LJ,Goodman MM

doi

10.1016/j.bmcl.2013.07.045

subject

Has Abstract

pub_date

2013-10-01 00:00:00

pages

5415-20

issue

19

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)00890-1

journal_volume

23

pub_type

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