艾司唑仑对血小板活化因子（PAF）的拮抗活性。对血小板聚集和PAF受体结合的体外作用。

An antagonistic activity of etizolam on platelet-activating factor (PAF). In vitro effects on platelet aggregation and PAF receptor binding.

作者信息

Mikashima H, Takehara S, Muramoto Y, Khomaru T, Terasawa M, Tahara T, Maruyama Y

机构信息

Research Laboratories, Yoshitomi Pharmaceutical Industries, Ltd., Fukuoka, Japan.

出版信息

Jpn J Pharmacol. 1987 Aug;44(4):387-91. doi: 10.1254/jjp.44.387.

DOI:10.1254/jjp.44.387

PMID:2890779

Abstract

The antagonistic effect of etizolam, an anti-anxiety drug, on platelet-activating factor (PAF) was investigated in rabbit platelets in vitro. Etizolam inhibited PAF-induced aggregation in a dose-dependent manner, with an IC50 of 3.8 microM, about one tenth that of triazolam (IC50 = 30 microM). At 300 microM, it inhibited both ADP and arachidonic acid-induced aggregation only slightly, while the other anti-anxiety drugs tested had no effect on PAF-induced aggregation even at this concentration. Etizolam and triazolam inhibited the specific binding of 3H-PAF to PAF receptor sites on washed rabbit platelets with IC50 values of 22 nM and 320 nM, respectively. Diazepam and estazolam were inactive even at 1 microM. These results indicate that etizolam is a specific antagonist of PAF.

摘要

在体外对兔血小板研究了抗焦虑药物艾司唑仑对血小板活化因子（PAF）的拮抗作用。艾司唑仑以剂量依赖性方式抑制PAF诱导的聚集，IC50为3.8微摩尔，约为三唑仑（IC50 = 30微摩尔）的十分之一。在300微摩尔时，它仅轻微抑制ADP和花生四烯酸诱导的聚集，而测试的其他抗焦虑药物即使在此浓度下对PAF诱导的聚集也无作用。艾司唑仑和三唑仑抑制3H-PAF与洗涤过的兔血小板上PAF受体位点的特异性结合，IC50值分别为22纳摩尔和320纳摩尔。地西泮和艾司唑仑即使在1微摩尔时也无活性。这些结果表明艾司唑仑是PAF的特异性拮抗剂。