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6‐[ 123 I]Iodo‐2‐[[4‐(2‐methoxyphenyl) piperazin‐1‐yl]methyl]imidazo[1,2‐ a ]pyridine as potential SPECT agent for imaging dopamine D 4 receptor: synthesis and in vivo evaluation in a nonhuman primate
Author(s) -
Alagille David,
Koren Andrei O.,
Kudej Greg,
Staley Julie,
Cosgrove Kelly,
Seibyl John,
Tamagnan Gilles D.
Publication year - 2008
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1500
Subject(s) - chemistry , chloramine t , radioligand , methyl iodide , agonist , dopamine , pyridine , radiosynthesis , in vivo , dopamine agonist , stereochemistry , medicinal chemistry , radiochemistry , in vitro , receptor , medicine , biochemistry , organic chemistry , microbiology and biotechnology , biology
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.