评估[(11)C]麦角乙脲作为非人类灵长类动物 5HTR 的 PET 示踪剂。
Evaluation of [(11)C]metergoline as a PET radiotracer for 5HTR in nonhuman primates.
机构信息
Medical Department, Brookhaven National Laboratory, Upton, NY 11973, United States.
出版信息
Bioorg Med Chem. 2010 Nov 15;18(22):7739-45. doi: 10.1016/j.bmc.2010.04.039. Epub 2010 Apr 20.
Abstract
Metergoline, a serotonin receptor antagonist, was labeled with carbon-11 in order to evaluate its pharmacokinetics and distribution in non-human primates using positron emission tomography. [(11)C]Metergoline had moderate brain uptake and exhibited heterogeneous specific binding, which was blocked by pretreatment with metergoline and altanserin throughout the cortex. Non-specific binding and insensitivity to changes in synaptic serotonin limit its potential as a PET radiotracer. However, the characterization of [(11)C]metergoline pharmacokinetics and binding in the brain and peripheral organs using PET improves our understanding of metergoline drug pharmacology.
摘要
美替拉酮，一种 5-羟色胺受体拮抗剂，被放射性碳-11 标记，以便使用正电子发射断层扫描评估其在非人类灵长类动物中的药代动力学和分布。[(11)C]美替拉酮具有中等的脑摄取，并表现出不均匀的特异性结合，这种结合可被美替拉酮和阿坦色林预处理在整个皮质中阻断。非特异性结合和对突触 5-羟色胺变化的不敏感性限制了其作为正电子发射断层扫描放射性示踪剂的潜力。然而，使用正电子发射断层扫描对 [(11)C]美替拉酮在大脑和外周器官中的药代动力学和结合进行特征描述，提高了我们对美替拉酮药物药理学的理解。
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