α1-Adrenergic Receptor Subtypes Molecular Structure, Function, and Signaling

摘要: The α1ARs are important mediators of sympathetic nervous system responses, particularly those involved in cardiovascular homeostasis, such as arteriolar smooth muscle constriction and cardiac contraction.1 2 In addition, have more recently been implicated the pathogenesis hypertrophy, ischemia-induced arrhythmias, ischemic preconditioning.1 3 Like other ARs, activated by catecholamines, norepinephrine epinephrine. They intrinsic membrane glycoproteins members GPCR superfamily. Over past 10 to 15 years, data initially based on functional, radioligand, biochemical studies accumulated, indicating that a heterogeneous group distinct but related proteins. This conclusion has confirmed with molecular cloning three α1-receptor subtypes, although until discrepancies between properties cloned expressed receptors characterized pharmacologically biochemically led confusion classification subtypes their coupled effector responses. As detailed present review, much this now clarified for α1ARs. These recent insights into structure, function, signaling α1ARs, control α1AR-gene expression, pharmacological evidence additional α1AR will be reviewed here. For information, reader is also referred several previous reviews α1ARs.4 5 6 7 Functional AR from laboratories McGrath8 Ruffolo,9 provided initial there may indicated postjunctional responses mediated could not explained adequately basis single population receptors. concept was further advanced …