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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.

DOI:10.1016/0014-2999(76)90047-9
PMID:954816
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。

相似文献

1
Effects of chlorprothixene isomers on platelet 5-hydroxytryptamine receptors: evidence for different 5-hydroxytryptamine conformations at uptake and stimulatory sites.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。
Eur J Pharmacol. 1976 Jun;37(2):385-8. doi: 10.1016/0014-2999(76)90047-9.
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The actions of flupenthixol upon 5-hydroxytryptamine-induced aggregation and the uptake of 5-hydroxytryptamine and dopamine by human blood platelets.三氟噻吨对5-羟色胺诱导的人血小板聚集以及5-羟色胺和多巴胺摄取的作用。
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Effects of ketanserin and mepyramine on platelet aggregation and on the uptake of 5-hydroxytryptamine into platelets.酮色林和吡苄明对血小板聚集及5-羟色胺摄取入血小板的影响。
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Human platelet 5HT receptors: characterisation and functional association.人类血小板5-羟色胺受体:特性与功能关联
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Urapidil inhibits 5-hydroxytryptamine induced platelet aggregation and 14C-5-hydroxytryptamine uptake in platelets.乌拉地尔抑制5-羟色胺诱导的血小板聚集以及血小板对14C-5-羟色胺的摄取。
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Effect of oral contraceptives on platelet noradrenaline and5-hydroxytryptamine receptors and aggregation.口服避孕药对血小板去甲肾上腺素、5-羟色胺受体及聚集的影响。
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Interaction of lisuride with monoamine receptors on human blood platelets.利苏瑞ide与人血小板单胺受体的相互作用。
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Verapamil inhibition of 5-hydroxytryptamine (5HT) uptake in rat platelets.维拉帕米对大鼠血小板摄取5-羟色胺(5HT)的抑制作用。
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Alpha-adrenoceptor-mediated actions of optical isomers and desoxy analogs of catecholimidazoline and norepinephrine in human platelets: in vitro.儿茶酚咪唑啉和去甲肾上腺素的光学异构体及脱氧类似物在人血小板中α-肾上腺素能受体介导的作用:体外研究
Biochem Pharmacol. 1986 Nov 15;35(22):4095-102. doi: 10.1016/0006-2952(86)90034-1.

引用本文的文献

1
Shape change of blood platelets--a model for cerebral 5-hydroxytryptamine receptors?血小板的形态变化——一种脑 5-羟色胺受体的模型?
Br J Pharmacol. 1979 Apr;65(4):601-8. doi: 10.1111/j.1476-5381.1979.tb07870.x.