使用正电子发射断层扫描（PET）通过[11C]DASB测量内源性血清素的潜力：结合研究

Potential of [11C]DASB for measuring endogenous serotonin with PET: binding studies.

作者信息

Lundquist Pinelopi, Wilking Helena, Höglund A Urban, Sandell Johan, Bergström Mats, Hartvig Per, Långström Bengt

机构信息

Division of Pharmacokinetics and Drug Therapy, Department of Pharmaceutical Biosciences, Uppsala University, SE-751 24 Uppsala, Sweden.

出版信息

Nucl Med Biol. 2005 Feb;32(2):129-36. doi: 10.1016/j.nucmedbio.2004.12.001.

DOI:10.1016/j.nucmedbio.2004.12.001

PMID:15721758

Abstract

The serotonin transporter radioligand [11C]-3-amino-4-(2-dimethylaminomethylphenylsulfanyl)-benzonitrile, or [11C]DASB, was examined in order to assess its potential for measuring fluctuations in endogenous serotonin concentrations with positron emission tomography. Binding characteristics of [11C]DASB and the propensity for serotonin to displace the tracer were explored in rat brain homogenates. Experiments showed that serotonin displaced [11C]DASB in vitro. Ex vivo experiments performed after tranylcypromine injection (3 or 15 mg/kg) showed a dose-dependent trend in radioactivity uptake and suggested that serotonin may compete with [11C]DASB for transporter binding.

摘要

为了评估其利用正电子发射断层扫描测量内源性血清素浓度波动的潜力，对血清素转运体放射性配体[11C]-3-氨基-4-(2-二甲基氨基甲基苯硫基)-苯甲腈，即[11C]DASB进行了研究。在大鼠脑匀浆中探究了[11C]DASB的结合特性以及血清素置换该示踪剂的倾向。实验表明，血清素在体外可置换[11C]DASB。在注射反苯环丙胺（3或15mg/kg）后进行的离体实验显示出放射性摄取的剂量依赖性趋势，并表明血清素可能与[11C]DASB竞争转运体结合。