Characterization ofβ_1-selectivity, adrenoceptor-G_s-protein interaction and inverse agonism of nebivolol in human myocardium

摘要

Intrinsic activity andβ_1-selectivity are important features ofβ-blockers in the treatment of patients with coronary syndromes and heart failure. In human myocardium, intrinsic activity andβ_1- selectivity of the novelβ-adrenoceptor antagonist nebivolol have not yet been determined. The study examines intrinsic activity,β-adrenoceptor-G-protein coupling andβ_-selectivity of Nebivolol and bisoprolol in human ventricular myocardium. Furthermore, intrinsic activity of both Compounds is compared to the one of bucindolol, carvedilol and metoprolol in human atrial Myocardium.