[11C]β-CIT, a cocaine analogue. Preparation, autoradiography and preliminary PET investigations
1993; Elsevier BV; Volume: 20; Issue: 3 Linguagem: Inglês
10.1016/0969-8051(93)90045-v
ISSN1872-9614
AutoresLars Müller, Christer Halldin, Lars Farde, Per Karlsson, Håkan Hall, Carl-Gunnar Swahn, John L. Neumeyer, Yigong Gao, Milius Richard,
Tópico(s)Parkinson's Disease Mechanisms and Treatments
Resumoβ-CIT (2β-carbomethoxy-3β-(4-iodophenyl)tropane) is a cocaine analogue with a high affinity for the dopamine transporter. [11C]β-CIT was prepared by N-methylation of nor-β-CIT with [11C]methyl iodide. The total radiochemical yield of [11C]β-CIT was 40–50% with an overall synthesis time of 35–40 min. The radiochemical purity was >99% and the specific radioactivity at the time of injection was about 1000 Ci/mmol (37 GBq/μ mol). Autoradiographic examination of [11C]β-CIT binding in human brains post-mortem demonstrated a high level of specific binding in the striatum. PET examination of [11C]β-CIT in a Cynomolgus monkey showed a marked accumulation of radioactivity in the striatum. The ratio of radioactivity in the striatum-to-cerebellum approached 5 after 87 min. In a displacement experiment, radioactivity in the striatum but not in the cerebellum, was markedly reduced after injection of unlabelled cocaine. [11C]β-CIT has a potential as ligand for PET examination of cocaine effects in man.
Referência(s)