Studies directed toward ascertaining the active conformation of 1, 4-dihydropyridine calcium entry blockers

G Rovnyak, N Andersen, J Gougoutas…

Index: Rovnyak; Andersen; Gougoutas; Hedberg; Kimball; Malley; Moreland; Porubcan; Pudzianowski Journal of Medicinal Chemistry, 1988 , vol. 31, # 5 p. 936 - 944

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Citation Number: 53

Abstract

A series of unsymmetrically substituted 4-phenyl-1, 4-dihydropyridine calcium entry blockers were investigated for their ability to relax potassium-contracted rabbit aortic smooth muscle and to competitively displace [3H] nitrendipine from its specific binding sites on guinea pig myocardial membranes in order to delineate the pharmacologically active conformer with respect to the position of the aromatic substituent (synperiplanar or antiperiplanar). The ...