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2-Ethynylbenzenealkanamines. A new class of calcium entry blockers

…, HR Almond, MD Brannan, RJ Carmosin…

文献索引:Carson; Almond; Brannan; Carmosin; Flaim; Gill; Gleason; Keely; Ludovici; Pitis; Rebarchak; Villani Journal of Medicinal Chemistry, 1988 , vol. 31, # 3 p. 630 - 636

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被引用次数: 26

摘要

A series of 2-(aryi-or alkylethyny1) benzenealkanamines were synthesized. They exhibit antihypertensive activity in spontaneously hypertensive rats and coronary vasodilator activity with minimal negative inotropic activity in the" Langendorff" guinea pig heart in vitro. They have been shown to exert their activity by inhibition of Ca2+ influx across cell membranes. Optimal activity is found among the N-(arylethyl)-5-methoxy-a-methyl-2-(phen-ylethyny1) ...