Physiological and pharmacological aspects of adrenergic receptor classification

Abstract

The questions raised are: what is the physiological or pharmacological basis for the differentiation into beta 1- and beta 2-, and alpha 1- and alpha 2-adrenergic receptors?; and do the neurotransmitter norepinephrine and the hormone epinephrine differ in their receptors? On the basis of a preference of beta 2- and alpha 2-adrenergic receptors for epinephrine, the hormone, and of beta 1-and alpha 1-receptors for norepinephrine, the neurotransmitter, it was postulated that the alpha 2- and beta 2-receptors are predominantly epinephrinergic in nature and located extrajunctionally and presynaptically whereas the alpha 1- and beta 1-receptors are predominantly norepinephrinergic in nature and located postsynaptically in the sympathetic terminal junction. The alpha 2- and beta 2-character of the presynaptic receptors matches that of the corresponding extrajunctional receptors. This indicates that a circulating catecholamine, namely epinephrine, is involved in the regulation of adrenergic transmitter release.