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Vol. 298, Issue 2, 403-410, August 2001
1-Adrenergic Receptors: New Insights and
Directions
Department of Pharmacology, the Vascular Biology Research Group,
University of Kentucky, College of Medicine, Lexington, Kentucky
(M.T.P.); and Department of Molecular Cardiology, Lerner Research
Institute, The Cleveland Clinic Foundation, Cleveland, Ohio (D.M.P.)
The adrenergic receptors play a key role in the modulation of
sympathetic nervous system activity as well as a site of action for
many therapeutic agents. The 
1-adrenergic receptor
subtypes (1A-, 1B-, 1D)
are the prime mediators of smooth muscle contraction and hypertrophic
growth, but their characterization in both binding and function have
lagged the other adrenergic family members. Although they are derived
from a related ancestral gene and all nine adrenergic receptor family
members bind the endogenous ligands, epinephrine and norepinephrine,
with roughly similar affinities, there are major differences in the
mode of binding, second messenger utilization, and physiological
effects of the 1-subtypes compared with 
- or
2-subtypes. Here, we review the recent literature on
aspects of its binding pocket and how it differs from the
-adrenergic receptor paradigms. We also review the signaling
components and aspects of its function and provide new insights into
its roles in smooth muscle, growth, neurological, and cardiovascular function.
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H. Zhang, C. S. Facemire, A. J. Banes, and J. E. Faber Different alpha -adrenoceptors mediate migration of vascular smooth muscle cells and adventitial fibroblasts in vitro Am J Physiol Heart Circ Physiol, June 1, 2002; 282(6): H2364 - H2370. [Abstract] [Full Text] [PDF]
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