CLONING, EXPRESSION AND CHARACTERIZATION OF HUMAN ALPHA-ADRENERGIC RECEPTORS ALPHA(1A), ALPHA(1B) AND ALPHA(1C)

The three human alpha adrenergic receptor subtypes, alpha(1a), alpha(1 b), and alpha(1c), have been cloned, expressed in COS-7 cells, and cha racterized pharmacologically. Competition binding studies of several a drenergic ligands with the three human receptor subtypes reveals a dis tinct pharmacological profile for each receptor subtype. RNase protect ion analysis demonsrates that the three receptor subtypes have differe nt patterns of distribution in human tissue. The availability of the t hree human alpha(1) receptor subtypes will facilitate the development of subtype-selective alpha(1) antagonists for a variety of therapeutic indications. (C) 1994 Academic Press, Inc.