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The relationship between the binding site of [3H]-d-cis-diltiazem and that of other non-dihydropyridine calcium entry blockers in cardiac sarcolemma

JL Balwierczak, CL Johnson and A Schwartz

[3H]-d-cis-Diltiazem binds to canine cardiac sarcolemma in a specific, saturable, and reversible manner with a KD = 58.0 +/- 9.5 nM and a receptor site density (maximum binding) of 2.19 +/- 0.24 pmol/mg of protein. Bepridil and verapamil, Ca2+ channel inhibitors, can completely inhibit this binding at nM concentrations. This inhibition was determined from saturation binding data to be due to a change in affinity of the radioligand, suggesting a competitive interaction between the three drugs. However, in dissociation experiments, both bepridil and verapamil increased the dissociation rate of the radioligand. This effect is uncharacteristic of competitive inhibitors and suggests that bepridil and verapamil regulate [3H]-d-cis-diltiazem binding in a negative allosteric fashion through their own distinct binding sites.

Volume 31, Issue 2, pp. 175-179, 02/01/1987
Copyright © 1987 by American Society for Pharmacology and Experimental Therapeutics




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