Adrenergic receptor beta-3 (ADRB3) (ADRB3)

The Adrenergic receptor beta-3 (ADRB3) is a G protein-coupled receptor predominantly expressed in white and brown adipose tissue, the urinary bladder, and the heart [1, 3, 12]. Its primary biological function involves the regulation of energy metabolism through lipolysis and thermogenesis via the activation of adenylate cyclase and the subsequent increase in intracellular cyclic AMP (cAMP) [1, 5, 21]. In the urinary bladder, ADRB3 activation mediates the relaxation of the detrusor muscle, which facilitates urine storage and increases bladder capacity [11, 20]. Consequently, ADRB3 has become a primary therapeutic target for the treatment of overactive bladder (OAB) syndrome [9, 11]. Beyond its role in the urinary system, ADRB3 is investigated for its contributions to metabolic and cardiovascular health [16, 17]. Genetic polymorphisms, such as the Trp64Arg variant, have been linked to an increased risk of obesity, insulin resistance, and type 2 diabetes in various populations [3, 13, 16]. In the heart, ADRB3 signaling may provide a cardioprotective effect or act as a 'brake' against excessive sympathetic stimulation, although its exact role in heart failure is still being elucidated [16, 18, 20]. Selective agonists like mirabegron and vibegron are currently the most prominent clinical drugs targeting this receptor to manage symptoms of urinary urgency and frequency [11, 21].

Other names

Beta-3 adrenergic receptorBeta-3 adrenoceptorBeta-3 adrenoreceptorBETA3AR

Selective agonism of the ADRB3 receptor leading to Gs protein coupling, activation of adenylate cyclase, and increased intracellular cAMP levels, which facilitates detrusor muscle relaxation in the bladder or stimulation of metabolic pathways such as lipolysis in adipose tissue.