文章基本信息

标题：Antagonism of the Human Thromboxane A2 Receptor by an Anti-asthmatic Agent AA-2414
本地全文：下载
作者：Tomofumi KUROKAWA ; Tatsumi MATSUMOTO ; Yasuko ASHIDA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1994
卷号：17
期号：3
页码：383-385
DOI：10.1248/bpb.17.383
出版社：The Pharmaceutical Society of Japan
摘要：The human thromboxane A₂ receptor (TXA₂-R)-coding gene was introduced into Chinese hamster ovary cells and a cell line (TCHO-25) stably expressing TXA₂-R, at a level of 3×10⁵/cell, was obtained. An anti-asthmatic agent AA-2414 [(±)-7-(3, 5, 6-trimethyl-1, 4-benzoquinon-2-yl)-7-phenylheptanoic acid] competitively inhibited the specific binding of a TXA₂ mimic ([³H] U-46619) to the TCHO-25 cells, with an IC₅₀ of 6.0×10^-8M, indicating that the drug is an antagonist of human TXA₂-R. The TCHO-25 cells offer a tool for the screening and characterization of human TXA₂-R antagonists.
关键词：thromboxane A2 receptor antagonist;anti-asthmatic agent;AA-2414;(±)-7-(3, 5, 6-trimethyl-1, 4-benzoquinon-2-yl)-7-phenylheptanoic acid