Beta-adrenergic receptors: biochemical mechanisms of physiological regulation

GL Stiles, MG Caron, RJ Lefkowitz - Physiological reviews, 1984 - journals.physiology.org
Physiological reviews, 1984journals.physiology.org
Catecholamines such as epinephrine and norepinephrine regulate physiological processes
via their interactions with a variety of cellular receptors. Ahlquist (5) originally classified
these receptors as cy-and, 6-adrenergic receptors on the basis of the relative potency of
various agonists in stimulating responses through these receptors. Later it became clear that
at least two major subtypes of both p-and a-adrenergic receptors-the &-and &-(138) and cyl-
and cy2-(24, 139) adrenergic receptors-can be distinguished by a variety of …
Catecholamines such as epinephrine and norepinephrine regulate physiological processes via their interactions with a variety of cellular receptors. Ahlquist (5) originally classified these receptors as cy-and, 6-adrenergic receptors on the basis of the relative potency of various agonists in stimulating responses through these receptors. Later it became clear that at least two major subtypes of both p-and a-adrenergic receptors-the &-and &-(138) and cyl-and cy2-(24, 139) adrenergic receptors-can be distinguished by a variety of pharmacological criteria. These receptor subtypes are discussed in some detail below.
Both PI-and p2-adrenergic receptors stimulate the membrane-bound enzyme adenylate cyclase; this action leads to the intracellular accumulation of adenosine 3’: 5’-cyclic phosphate [cyclic AMP (CAMP)], the second messenger of@-adrenergic action in virtually all tissues examined to date (252). In some systems cY,-adrenergic receptors inhibit adenylate cyclase (NO), whereas cyladrenergic receptors are not clearly linked to the adenylate cyclase system.
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