Synthesis of [2-{(4-chlorophenyl) (4-[125I]iodophenyl)} methoxyethyl]-1-piperidine-3-carboxylic acid, [125I]CIPCA: A potential radiotracer for GABA uptake sites

✍ Scribed by Marcian E. Van Dort; David L. Gildersleeve; Donald M. Wieland

• Publisher: John Wiley and Sons
• Year: 1995
• Tongue: French
• Weight: 491 KB
• Volume: 36
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.2580361008

✦ Synopsis

Abstract

The synthesis of racemic [2‐{(4‐Chlorophenyl) (4‐iodophenyl)} methoxyethyl]‐1‐piperidine‐3‐carboxylic acid, (CIPCA) and its radioiodinated analog [^125ß^I]CIPCA is described. CIPCA was synthesized from 4‐iodobenzoyl chloride in five steps in 16% overall yield. Ammonium sulfate catalyzed solid‐state isotopic exchange of CIPCA with Na^125^I provided [^125^I]CIPCA in 34% isolated radiochemical yield at a specific activity of 118 Ci/mmol. [^125^ICIPCA] demonstrated moderate brain extraction and good in vivo radiostability in preliminary biodistribution studies conducted in CD‐1 mice. [^125^I]CIPCA is a potentially useful radiotracer for study of the GABA uptake system.