✦ LIBER ✦

6-[123I]Iodo-2-[[4-(2-methoxyphenyl) piperazin-1-yl]methyl]imidazo[1,2-a]pyridine as potential SPECT agent for imaging dopamine D4 receptor: synthesis and in vivo evaluation in a nonhuman primate

✍ Scribed by David Alagille; Andrei O. Koren; Greg Kudej; Julie Staley; Kelly Cosgrove; John Seibyl; Gilles D. Tamagnan

Publisher: John Wiley and Sons
Year: 2008
Tongue: French
Weight: 129 KB
Volume: 51
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.1500

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✦ Synopsis

Abstract

The dopamine D~4~ receptor subtype has drawn considerable attention due to its potential implication in schizophrenia and erectile dysfunction. 6‐[^123^I]Iodo‐2‐[[4‐(2‐methoxyphenyl)piperazin‐1‐yl]methyl]imidazo[1,2‐a]pyridine [^123^I]‐1, a potent and selective new dopamine D~4~ agonist, was synthesized by classical iododestannylation using sodium [^123^I]iodide and chloramine‐T. Radiolabeling yield varied from 34 to 38% with a radiochemical purity exceeding 99%. Despite a good in vitro profile, in vivo evaluation of this radioligand in baboon showed no brain uptake after i.v. injection. Copyright © 2008 John Wiley & Sons, Ltd.

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