[11C]β-CIT-FE, a radioligand for quantitation of the dopamine transporter in the living brain using positron emission tomography

✍ Scribed by Christer Halldin; Lars Farde; Camilla Lundkvist; Nathalie Ginovart; Yoshifumi Nakashima; Per Karlsson; Carl-Gunnar Swahn

• Publisher: John Wiley and Sons
• Year: 1996
• Tongue: English
• Weight: 431 KB
• Volume: 22
• Category: Article
• ISSN: 0887-4476
• DOI: 10.1002/(sici)1098-2396(199604)22:4<386::aid-syn10>3.0.co;2-w

✦ Synopsis

The cocaine analogue P-CIT-FE (N-(2-fluoroethyl)-2~-carbomethoxy-3~-(4-iodopheny1)nortropane) was labeled with ' lC for positron emission tomography (PET) studies of the dopamine transporter. After intravenous administration to a cynomolgus monkey, ["CIP-CIT-FE accumulated in the striatum with a striatum-to-cerebellum ratio of about 9 after 60 min. Pseudoequilibrium of specific ["Clp-CIT-FE binding in the striatum was obtained within 30-50 min. The radioactivity ratios of the thalamus to the cerebellum and the neocortex to the cerebellum were about 2 and 1.5, respectively. In displacement and pretreatment experiments, radioactivity in the striatum but not in the cerebellum was reduced after injection of P-CIT or the dopamine transporter inhibitor GBR 12909, indicating that striatal radioactivity following injection of ["CIP-CIT-FE represents reversible binding to dopamine transporter sites. After displacement or pretreatment with cocaine there was a marked effect not only in the striatum but also in the thalamus and neocortex. [WIP-CIT-FE has potential as a useful PET radioligand for quantitation of the dopamine transporter in the primate brain in vivo.