or adrenergic receptor or adrenoreceptor or adrenotropic receptor
any receptor on an effector cell that is activated by epinephrine or related catecholamines. Structurally, they are all of the
7TM type. Adrenoceptors may be classified phenomenologically into different types according to their sensitivities to agonists and antagonists.
α Adrenoceptors have a relative order of agonist potency: epinephrine > norepinephrine > isoprenaline (isoproterenol), and a relative order of antagonist potency: phentolamine >> propranolol. They are associated with stimulatory effects, such as vasoconstriction and contraction of the iris, nictitating membrane, urinary bladder, seminal vesicles, and vas deferens, and with relaxation of propulsive smooth muscle in the gut. In some species, they mediate stimulation of gluconeogenesis and hepatic glycogenolysis. There are two groups, α
1 and α
2. α
1 receptors act through the phosphoinositide/Ca
2+ second messenger system and are of four subtypes: α
1A, norepinephrine > epinephrine; α
1B, norepinephrine = epinephrine; α
1C, norepinephrine = epinephrine (different antagonist sensitivity from α
1B); α
1D. α
2A receptors all inhibit the formation of cyclic AMP; they also open K
+ channels and inhibit Ca
2+ channels. α
2B receptors inhibit Ca
2+ channels. α
2C receptors have no effect on ion channels.
β Adrenoceptors have actions that can be ascribed to the activation of adenylate cyclase. They may be divided phenomenologically into three classes: (1) β
1 adrenoceptors, in which the relative order of agonist potency is isoprenaline > norepinephrine > epinephrine, and the relative order of antagonist potency is practolol > propranolol. They are associated with cardiac stimulation and glycogenolysis, lipolysis in white adipose tissue, and calorigenesis in brown adipose tissue; (2) β
2 adrenoceptors, in which the relative order of agonist potency is isoprenaline > epinephrine > norepinephrine, and the relative order of antagonist potency is propranolol > practolol; they are associated with skeletal muscle glycogenolysis, promotion of secretion of glucagon and insulin, vasodepression and bronchodilation; and (3) β
3 adrenoceptors, with agonist potency norepinephrine > epinephrine. See also
β-adrenergic receptor kinase,
β-arrestin.