氯丙硫蒽异构体对血小板5-羟色胺受体的影响：摄取和刺激位点存在不同5-羟色胺构象的证据。

Effects of chlorprothixene isomers on platelet 5-hydroxytryptamine receptors: evidence for different 5-hydroxytryptamine conformations at uptake and stimulatory sites.

作者信息

Drummond A H, Whigham K A, Prentice C R

出版信息

Eur J Pharmacol. 1976 Jun;37(2):385-8. doi: 10.1016/0014-2999(76)90047-9.

Abstract

The thioxanthene neuroleptic, cis-chlorprothixene, was approximately 200 times more potent than its transisomer as an inhibitor of the aggregation of human blood platelets induced by 5-hydroxytryptamine (5HT). Against the active uptake of 5HT by these cells, however, trans-chlorprothixene was twice as inhibitory as its cisisomer, and this inhibition was found to be competitive. It is suggested that 5HT adopts different conformations for binding to its two platelet receptors.

摘要

噻吨类抗精神病药顺式氯普噻吨作为5-羟色胺（5HT）诱导的人血小板聚集抑制剂，其效力比反式异构体约强200倍。然而，对于这些细胞对5HT的主动摄取，反式氯普噻吨的抑制作用是其顺式异构体的两倍，且这种抑制作用是竞争性的。有人提出，5HT在与它的两种血小板受体结合时采取不同的构象。