Abstract
The effects of d-cis-diltiazem (diltiazem) and verapamil on 1,4-dihydropyridine binding to dog cardiac membranes were studied in competition, saturation and kinetic binding experiments with [ 3H](+)-PN200-110. Diltiazem increased [ 3H](+)-PN200-110 binding with an observed maximal effect at 50 μM, while verapamil decreased [ 3H](+)-PN200-110 binding in a dose-dependent manner. Scatchard analysis of saturation binding data revealed that diltiazem (50 μM) increased the maximal binding site density and verapamil (100 μM) increased the dissociation constant (K D) of [ 3H](+)-PN200-110 binding. The kinetic experiments demonstrated that diltiazem reduced both the association and the dissociation rate of [ 3H](+)-PN200-110 binding, resulting in no significant change in the apparent K D. In contrast, verapamil accelerated dissociation and slowed down association of [ 3H](+)-PN200-110 binding. Diltiazem appears to alter both the number of [ 3H](+)-PN200-110 binding sites and the characteristics of [ 3H](+)-PN200-110 binding.
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