2-Ethynylbenzenealkanamines. A new class of calcium entry blockers

Article abstract of DOI:10.1021/jm00398a023

A series of 2-(aryl- or alkylethynyl)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-α-methyl-2-(phenylethynyl)benzeneethanamines and -propanamines.