An Antagonistic Activity of Etizolam on Platelet-Activating Factor (PAF) In Vitro Effects on Platelet Aggregation and PAF Receptor Binding

[摘要] References(13)Cited-By(9)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 μM, about one tenth that of triazolam (IC50=30 μM). At 300 μM, 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 μM. These results indicate that etizolam is a specific antagonist of PAF.

[学科分类] 药理学