假定的前列环素受体拮抗剂（FCE - 22176）对人血小板和NCB - 20细胞是一种完全激动剂。

The putative prostacyclin receptor antagonist (FCE-22176) is a full agonist on human platelets and NCB-20 cells.

作者信息

Wilkins A J, MacDermot J

出版信息

Eur J Pharmacol. 1986 Aug 7;127(1-2):117-9. doi: 10.1016/0014-2999(86)90211-6.

Abstract

The action of FCE-22176 on prostacyclin receptors of human platelets and the NCB-20 cell line have been examined. FCE-22176 is a full agonist in both systems, mediating activation of adenylate cyclase. The concentration required for half-maximum enzyme activation was 174 nM in platelet membranes and 193 nM in homogenates of NCB-20 cells. The binding of [3H]iloprost to human platelet or NCB-20 cell membranes was inhibited by FCE-22176, and Ki values of 400 and 280 nM were obtained.

摘要

已对FCE - 22176作用于人类血小板和NCB - 20细胞系前列环素受体的情况进行了研究。FCE - 22176在这两个系统中均为完全激动剂，可介导腺苷酸环化酶的激活。在血小板膜中，酶激活达到半最大值所需的浓度为174 nM，在NCB - 20细胞匀浆中为193 nM。FCE - 22176抑制了[3H]伊洛前列素与人类血小板或NCB - 20细胞膜的结合，获得的Ki值分别为400 nM和280 nM。