This manuscript is intended to provide a comprehensive review of the a
lpha-adrenoceptors (ARs) and their role in vascular regulation. The hi
storical development of the concept of receptors and the division of t
he alpha-ARs into alpha(1) and alpha(2) subtypes is traced. Emphasis w
ill be placed on current understanding of the specific contribution of
discrete alpha(1)- and alpha(2)-AR subtypes in the regulation of the
vasculature, selective agonists and antagonists for these receptors, t
he second messengers utilized by these receptors, the myoplasmic calci
um pathways activated to initiate smooth muscle contraction, as well a
s the clinical uses of agonists and antagonists that work at these rec
eptors. New information is presented that deals with the molecular asp
ects of ligand interactions with specific subdomains of these receptor
s, as well as mRNA distribution and the regulation of alpha(1)- and al
pha(2)-AR gene transcription and translation. Copyright (C) 1996 Elsev
ier Science Inc.