Structure, function, and regulation of adrenergic receptors

Abstract

Adrenergic receptors for adrenaline and noradrenaline belong to the large multigenic family of receptors coupled to GTP‐binding proteins. Three pharmacologic types have been identified: α₁‐, α₂‐, and β‐adrenergic receptors. Each of these has three subtypes, characterized by both structural and functional differences. The α₂ and β receptors are coupled negatively and positively, respectively, to adenylyl cyclase via G_i or G_s regulatory proteins, and the α₁ receptors modulate phospholipase C via the G_o protein. Subtype expression is regulated at the level of the gene, the mRNA, and the protein through various transcriptional and postsynthetic mechanisms. Adrenergic receptors constitute, after rhodopsin, one of the best studied models for the other receptors coupled to G proteins that are likely to display similar structural and functional properties.