用正电子发射断层扫描（PET）成像5-羟色胺（1A）受体：WAY-100635及其类似物。

Imaging the 5-HT(1A) receptors with PET: WAY-100635 and analogues.

作者信息

Houle S, DaSilva J N, Wilson A A

机构信息

Vivian M Rakoff PET Centre, Centre for Addiction and Mental Health, Toronto, Canada.

出版信息

Nucl Med Biol. 2000 Jul;27(5):463-6. doi: 10.1016/s0969-8051(00)00112-8.

DOI:10.1016/s0969-8051(00)00112-8

PMID:10962251

Abstract

This paper summarizes our work on WAY-100635 and analogues, labeled either with carbon-11 or fluorine-18, as potential radioligands for the 5-hydroxytryptamine(1A) (5-HT(1A)) neuroreceptors. Other facets of our work include: (1) human studies with [O-methyl-(11)C]WAY-100634, the major radioactive metabolite of [O-methyl-(11)C]WAY-100635, and with [(11)C]CPC 222; (2) use of a human liver metabolism model to screen in vitro potential metabolic problems in humans; (3) modification of the "dry method" to prepare [carbonyl-(11)C]WAY-100635; and (4) validation studies in humans with [carbonyl-(11)C]WAY-100635.

摘要

本文总结了我们在WAY-100635及其类似物方面的工作，这些类似物用碳-11或氟-18标记，作为5-羟色胺（1A）（5-HT（1A））神经受体的潜在放射性配体。我们工作的其他方面包括：（1）使用[O-甲基-（11）C]WAY-100634（[O-甲基-（11）C]WAY-100635的主要放射性代谢物）和[（11）C]CPC 222进行人体研究；（2）使用人体肝脏代谢模型在体外筛选人体潜在的代谢问题；（3）改进“干法”以制备[羰基-（11）C]WAY-100635；以及（4）用[羰基-（11）C]WAY-100635在人体进行验证研究。