Molecular Pharmacology of Human α1-Adrenergic Receptors:Unique Features of the α1a-Subtype

Abstract
α1-Adrenergic receptors (α1ARs) are G protein-coupled receptors important in the dynamic component of benign prostatic hyperplasia. α1ARs stimulate predominantly phospholipase C-β, resulting in mobilization of calcium from intracellular stores and, ultimately, smooth muscle contraction. cDNAs encoding three human α1ARs (α1a, α1b, α1d) have been cloned, expressed stably in cells, and characterized pharmacologically. Extensive species heterogeneity in tissue distribution emphasizes the importance of studying α1ARs in human tissues. Because of the important role of α1aARs in mediating prostate smooth muscle contraction, this current review describes α1a carboxyl terminal splice variants, examines α1AR subtype distribution in various tissues and the role of the putative α1LAR in human prostate, provides a brief discussion regarding regulation of this receptor by agonist, and finally discusses implications of distinct α1AR subtype distribution in human bladder compared with prostate.

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