Abstract
The effects of a series of lactamimides on [ 3 H]d-cis- diltiazem binding to rat brain membranes, on [ 3H]nitrendipine binding to cardiac membranes, and on calcium-induced contractions in depolarized guinea pig taenia and ileum preparations were examined. Several of the lactamimides examined displaced [ 3 H]d-cis- diltiazem binding and antagonized, in a competitive fashion, calcium-induced contractions. Over the series of lactamimides, there was a highly significant, positive linear correlation ( r = 0.87, P < 0.001) between their potency to displace [ 3 H]d-cis- diltiazem and their potency to antagonize calcium-induced contractions in the depolarized taenia and ileum preparations. Of the lactamimides examined, MDL 16,582A [ N-(2,2-diphenylpentyl)azacyclotridecan-2-imine · hydrochloride] had potency equivalent to d- cis-diltiazem with p A 2 values of 7.27 and 7.38, respectively, against calcium-induced contractions in the guinea pig ileum. These lactamimides are a novel chemical class displaying diltiazem-like calcium antagonist properties.
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