6533b7d9fe1ef96bd126b92c

RESEARCH PRODUCT

Identification of Purine Binding Sites on Torpedo Acetylcholine Receptor

Edson X. AlbuquerqueAlfred MaelickeAndré SchrattenholzA. SchuhenHans-jochen SchäferUli RothJasminka Godovac-zimmermann

subject

PharmacologyPurineAzidesBinding SitesbiologyChemistryAffinity labelAffinity LabelsReceptors NicotinicTorpedolaw.inventionchemistry.chemical_compoundAdenosine TriphosphateNicotinic agonistBiochemistrylawbiology.proteinmedicineAnimalsBinding siteReceptorTorpedoAcetylcholinemedicine.drugAcetylcholine receptor

description

Electrophysiological studies from this and other laboratories have suggested a direct action of ATP on nicotinic acetylcholine receptors (nAChR). To determine the site of binding of this purine derivative, we have covalently modified the nAChR from Torpedo marmorata electrocytes employing 2-[3H]-8-azido-ATP as a photoactivable affinity label. Covalently attached radioactivity was predominantly found in the beta-polypeptide of the receptor. Based on the results of protection studies with several nAChR ligands whose target sites at the receptor are known, we conclude that the purine site(s) differ from those of acetylcholine and of physostigmine, galanthamine and related ligands, and those of local anesthetics.

https://doi.org/10.3109/10799899409066031