Beta-3 Adrenoceptors as New Therapeutic Targets for Cardiovascular Pathologies

Abstract Catecholamines play a key role in the regula-tion of cardiovascular function, classically through ß1/2-adrenoreceptors (AR) activation. After ß3-AR cloning in the late 1980s, convincing evidence for ß3-AR expression and function in cardiovascular tissues recently initiated a reexamination of their involvement in the pathophysiology of cardiovascular diseases. Their upregulation in diseased cardiovascular tissues and resistance to desensitization sug-gest they may be attractive therapeutic targets. They may substitute for inoperant ß1/2-AR to mediate vasodilation in diabetic or atherosclerotic vessels. In cardiac ventricle, their contractile effects are functionally antipathetic to those of ß1/2-AR; in normal heart, ß3-ARs may mediate a moderate negative inotropic effect, but in heart failure, it may protect against adverse effects of excessive catecholamine stimula