PAF ANTAGONISTIC ACTIVITY OF SOME THIENO [3, 2-f] [1, 2, 4] TRIAZOLO [4, 3-a] [1, 4] DIAZEPINES

Tetsuya Tahara; Hiroshi Mikashima; Michio Terasawa; Yutaka Maruyama

doi:10.1248/cpb.35.2119

Tetsuya Tahara, Hiroshi Mikashima, Michio Terasawa, Yutaka Maruyama

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Keywords: thieno [3, 2-f] [1, 2, 4] triazolo [4, 3-a] [1, 4] diazepine, PAF antagonistic activity, anti-platelet aggregation, anti-bronchoconstriction, etizolam

JOURNAL FREE ACCESS

1987 Volume 35 Issue 5 Pages 2119-2121

DOI https://doi.org/10.1248/cpb.35.2119

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Abstract

Some thieno [3, 2-f] [1, 2, 4] triazolo [4, 3-a] [1, 4] diazepines were antagonistic to PAF-induced platelet aggregation in rabbit PRP and bronchoconstriction in guinea pigs. A study of structure-activity relationships demonstrates that the fused triazolo ring with a lower alkyl group is crucial for the activity. Among these compounds, etizolam was the most potent and specific antagonist of PAF.

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