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Abstract
AbstractCalcium antagonists have the ability to relax vesical smooth muscle in vitro and in vivo. The presumed mechanism of action is through the inhibition of calcium translocation, yet these agents have also been shown to bind to several different pharmacological receptors. By employing radioligand binding assays, the affinity of verapamil and diltiazem for several receptor populations in the rabbit detrusor was studied. Verapamil and diltiazem displayed binding affinities for receptor populations in the following order: alpha1‐ and alpha2‐ adrenergic > muscarinic cholinergic > beta‐adrenergic. In all instances verapamil affinity was greater than that of diltiazem. The relatively high Ic50's for both muscarinic and beta receptors indicate that the interactions of verapamil and diltiazem with these receptors are of little physiological significance.
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