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Bioorg Med Chem Lett. 2013 Oct 1;23(19):5415-20. doi: 10.1016/j.bmcl.2013.07.045. Epub 2013 Jul 30.

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

Author information

1
Department of Radiology and Imaging Sciences, Emory University, Atlanta, GA 30329, United States.

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.

KEYWORDS:

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

PMID:
23978650
PMCID:
PMC3955700
DOI:
10.1016/j.bmcl.2013.07.045
[Indexed for MEDLINE]
Free PMC Article
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