Me. Vandort et al., SYNTHESIS OF ODOPHENYL))METHOXYETHYL]-1-PIPERIDINE-3-CARBOXYLIC ACID,[I-125] CIPCA - A POTENTIAL RADIOTRACER FOR GABA UPTAKE SITES, Journal of labelled compounds & radiopharmaceuticals, 36(10), 1995, pp. 961-971
Citations number
20
Categorie Soggetti
Chemistry Analytical","Pharmacology & Pharmacy","Biochemical Research Methods
The synthesis of racemic [2-{(4-Chlorophenyl)(4-iodophenyl)} methoxyet
hyl]-1-piperidine-3-carboxylic acid, (CIPCA) and its radioiodinated an
alog [I-125]CIPCA is described. CIPCA was synthesized from 4-iodobenzo
yl chloride in five steps in 16% overall yield. Ammonium sulfate catal
yzed solid-state isotopic exchange of CIPCA with (NaI)-I-125 provided
[I-125]CIPCA in 34% isolated radiochemical yield at a specific activit
y of 118 Ci/mmol. [I-125]CIPCA demonstrated moderate brain extraction
and good in vivo radiostability in preliminary biodistribution studies
conducted in CD-1 mice. [I-125]CIPCA is a potentially useful radiotra
cer for study of the GABA uptake system.