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 | Zendy

Alagille David | Zendy; Koren Andrei O. | Zendy; Kudej Greg | Zendy; Staley Julie | Zendy; Cosgrove Kelly | Zendy; Seibyl John | Zendy; Tamagnan Gilles D. | Zendy

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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

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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