Calcium-and calmodulin-antagonism of elnadipine derivatives: comparative SAR

…, W Voigt, K Schoenafinger, E Schraven

Index: Mannhold; Jablonka; Voigt; Schonafinger; Schraven European Journal of Medicinal Chemistry, 1992 , vol. 27, # 3 p. 229 - 235

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Citation Number: 184

Abstract

Abstract The Ca 2+-antagonistic properties of elnadipine derivatives have been quantified by means of binding experiments in bovine cerebral cortex membranes using 3 H- nitrendipine. Competition experiments have shown a 308-fold concentration range of K i- values (2.9× 10− 10 to 8.9× 10− 8) for elnadipine derivatives and a eudismic ratio for elnadipine and its (+)-enantiomer of 448. Calmodulin (CaM)-antagonistic properties have ...