Premium
[ 11 C]β‐CIT‐FE, a radioligand for quantitation of the dopamine transporter in the living brain using positron emission tomography
Author(s) -
Halldin Christer,
Farde Lars,
Lundkvist Camilla,
Ginovart Nathalie,
Nakashima Yoshifumi,
Karlsson Per,
Swahn CarlGunnar
Publication year - 1996
Publication title -
synapse
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.809
H-Index - 106
eISSN - 1098-2396
pISSN - 0887-4476
DOI - 10.1002/(sici)1098-2396(199604)22:4<386::aid-syn10>3.0.co;2-w
Subject(s) - radioligand , positron emission tomography , dopamine transporter , brain positron emission tomography , dopamine , nuclear medicine , transporter , medicine , chemistry , neuroscience , psychology , preclinical imaging , receptor , biology , biochemistry , dopaminergic , microbiology and biotechnology , in vivo , gene
Abstract The cocaine analogue β‐CIT‐FE (N‐(2‐fluoroethyl)‐2β‐carbomethoxy‐3β‐(4‐iodophenyl)nortropane) was labeled with 11 C for positron emission tomography (PET) studies of the dopamine transporter. After intravenous administration to a cynomolgus monkey, [ 11 C]β‐CIT‐FE accumulated in the striatum with a striatum‐to‐cerebellum ratio of about 9 after 60 min. Pseudoequilibrium of specific [ 11 C]β‐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 β‐CIT or the dopamine transporter inhibitor GBR 12909, indicating that striatal radioactivity following injection of [ 11 C]β‐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. [ 11 C]β‐CIT‐FE has potential as a useful PET radioligand for quantitation of the dopamine transporter in the primate brain in vivo. © 1996 Wiley‐Liss, Inc.