Alpha-1 adrenergic receptor

See also: Adrenergic receptor

alpha-1 (α1) adrenergic receptors are G protein-coupled receptors (GPCRs) associated with the Gq heterotrimeric G protein. α1-adrenergic receptors are subdivided into three highly homologous subtypes, i.e., α1A-, α1B-, and α1D-adrenergic receptor subtypes. There is no α1C receptor. At one time, there was a subtype known as α1C, but it was found to be identical to the previously discovered α1A receptor subtype.[1] To avoid confusion, naming was continued with the letter D. Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α1-adrenergic receptors in the central and peripheral nervous systems. The crystal structure of the α1B-adrenergic receptor subtype has been determined in complex with the inverse agonist (+)-cyclazosin.[2]

  1. ^ Graham RM, Perez DM, Hwa J, Piascik MT (May 1996). "alpha 1-adrenergic receptor subtypes. Molecular structure, function, and signaling". Circulation Research. 78 (5): 737–49. doi:10.1161/01.RES.78.5.737. PMID 8620593.
  2. ^ Deluigi M, Morstein L, Schuster M, Klenk C, Merklinger L, Cridge RR, de Zhang LA, Klipp A, Vacca S, Vaid TM, Mittl PR, Egloff P, Eberle SA, Zerbe O, Chalmers DK, Scott DJ, Plückthun A (January 2022). "Crystal structure of the α1B-adrenergic receptor reveals molecular determinants of selective ligand recognition". Nature Communications. 13 (1): 382. Bibcode:2022NatCo..13..382D. doi:10.1038/s41467-021-27911-3. PMC 8770593. PMID 35046410.