The beta-adrenergic receptor. Configuration, regulation, mechanism of action.
Much has been learned in the 25 years since a beta-blocking drug was first administered to humans. The beta-adrenergic receptor has been divided into two general subtypes, and these have been purified to homogeneity. The beta 2-receptor gene has been cloned, and the primary structure of the beta 2 receptor has been deduced. Additionally, important details of the receptor-adenylate cyclase complex have been elucidated. Another general category of information relates to the unique features of the myocardial beta-adrenergic receptor population. These include (1) a relatively high proportion of beta 2 receptors and coupling of these receptors to muscle contraction; (2) the apparent lack of spare receptors; (3) selective down-regulation of the beta 1-receptor population in heart failure, with preservation of the beta 2 and alpha 1 populations; and (4) mediation of the most powerful inotropic stimulus that can be delivered by a receptor-coupled pathway. In the next 25 years, investigations will emphasize the use of molecular biologic techniques to discover crucial information about the control of beta-receptor structure and function. From this research will come both new pharmacologic agents and new applications of currently available agents.
D000262:Adenylyl Cyclases / Q000378:metabolism; D000319:Adrenergic beta-Antagonists / Q000494:pharmacology; D000242:Cyclic AMP / Q000378:metabolism / Q000502:physiology; D006321:Heart / Q000187:drug effects / Q000502:physiology*; D006331:Heart Diseases / Q000188:drug therapy / Q000378:metabolism / Q000503:physiopathology; D006801:Humans; D009200:Myocardial Contraction; D009206:Myocardium / Q000378:metabolism; D011943:Receptors, Adrenergic, beta / Q000187:drug effects / Q000378:metabolism / Q000502:physiology*
D000319:Adrenergic beta-Antagonists; D011943:Receptors, Adrenergic, beta; D000242:Cyclic AMP; D000262:Adenylyl Cyclases