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PAF antagonistic activity of some thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepines.
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1987
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Molecular PharmacologyMedicinal ChemistryPharmaceutical ChemistryRabbit PrpPharmacological StudyMedicinePaf-induced Platelet AggregationPharmacological AgentFused TriazoloPharmacotherapyHeterocycle ChemistryPharmacologyPaf Antagonistic ActivityDrug Discovery
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.