Receptor Pharmacology of Carvedilol in the Human Heart

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Abstract
The β-blocker and vasodilator carvedilol was examined in preparations of human ventricular myocardium. Carvedilol is a high-affinity, slightly β1-selective competitive β-blocking agent, with a KD for β1-receptors of approximately 4-5 nM and a selectivity of sixfold to 39-fold for β1-receptors rather than β2-receptors, depending on the method used to assess subtype potency. Carvedilol also is a potent α1-blocking agent, with a β1:α1-blocking relative potency of 1.7-fold. In human lymphocytes containing β2-receptors and human myocardial membranes containing both β1-and β2-receptors, carvedilol exhibited the unique property of guanine nucleotide-modulatable binding. This is a property shared with bucindolol, another β-blocker and vasodilator that is structurally similar to carvedilol. Despite the presence of guanine nucleotide-modulatable binding, no intrinsic activity of carvedilol was detected in preparations of isolated human heart or in myocardial membranes.

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