β3-adrenoceptors in human detrusor muscle

摘要: The detrusor muscle contains beta-adrenoceptors (beta-AR), and 2 subtypes-beta1-AR beta2-AR-have been identified in most species. Although beta2-AR has an important role relaxation via activation of adenylate cyclase, evidence suggests that a third subtype, beta3-AR, which is implicated metabolic functions endogenous catecholamines, mediates human muscle. There predominant expression beta3-AR messenger RNA (mRNA) bladder tissue, with 97% total beta-AR mRNA being represented by the subtype only 1.5% 1.4% beta1-AR subtypes, respectively. Functionally, selective agonists relax isolated detrusor, whereas beta1-AR/beta2-AR do not. Isoproterenol-induced inhibited antagonists but not or antagonists. In animal models, increase capacity have weak cardiovascular side effects. this points toward clinical utility as therapy for overactive bladder, trials models antiobesity agents indicate effects tremor tachycardia. Development compounds high selectivity screening techniques using cell lines transfected beta1-AR, beta2-AR, genes, may mitigate such problems. Together preliminary finding 49% (21 43) patients idiopathic instability tryptophan 64 arginine mutation gene, be useful genetic marker, therapeutic target treatment disorder.