Alpha-2A Adrenergic Receptor
The human α2A adrenergic receptor (α2AAR) was first cloned in human platelet cells in 1987 (Kobilka et al. 1987) and was further characterized upon creation of a stable Chinese hamster ovary (CHO) cell line expressing the human α2AAR (Fraser et al. 1989). Cloning of the rat (Chalberg et al. 1990) and pig (Guyer et al. 1990) α2AAR revealed high sequence homology with the human receptor. This conservation across species indicates that the α2AAR plays an important physiological role.
Activation and Signaling
The α2AAR is a G-protein coupled receptor (GPCR) that couples mainly to Gi/o proteins and inhibits voltage dependent Ca2+ channel activation and adynyl cyclase. Additionally, the α2AAR activates inwardly rectifying K+channels and induces phosphorylation of mitogen-activated protein kinase (MAPK) and Akt,...
- Fraser CM, Arakawa S, McCombie WR, Venter JC. Cloning, sequence analysis, and permanent expression of a human alpha 2-adrenergic receptor in Chinese hamster ovary cells. Evidence for independent pathways of receptor coupling to adenylate cyclase attenuation and activation. J Biol Chem. 1989;264:11754–61.PubMedPubMedCentralGoogle Scholar
- Lu R, Chen Y, Cottingham C, Peng N, Jiao K, Limbird LE, et al. Enhanced hypotensive, bradycardic, and hypnotic responses to alpha2-adrenergic agonists in spinophilin-null mice are accompanied by increased G protein coupling to the alpha2A-adrenergic receptor. Mol Pharmacol. 2010;78:279–86. https://doi.org/10.1124/mol.110.065300.CrossRefPubMedPubMedCentralGoogle Scholar