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

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

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

Jpn J Pharmacol. 1987 Aug;44(4):387-91.

PubMed ID

2890779 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Drugs

Etizolam

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Etizolam	Platelet-activating factor receptor	Protein	Humans	Unknown	Antagonist	Details