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 |
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Authors: | David Alagille Andrei O. Koren Greg Kudej Julie Staley Kelly Cosgrove John Seibyl Gilles D. Tamagnan |
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Affiliation: | 1. Molecular Neuroimaging, 60 Temple St, Suite 8A, New Haven, CT 06510, USA;2. Yale University School of Medicine, Psychiatry and Diagnostic Radiology, New Haven, CT 06511, USA |
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Abstract: | The dopamine D4 receptor subtype has drawn considerable attention due to its potential implication in schizophrenia and erectile dysfunction. 6‐[123I]Iodo‐2‐[[4‐(2‐methoxyphenyl)piperazin‐1‐yl]methyl]imidazo[1,2‐a]pyridine [123I]‐1, a potent and selective new dopamine D4 agonist, was synthesized by classical iododestannylation using sodium [123I]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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Keywords: | dopamine D4 SPECT schizophrenia erectile dysfunction |
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