Open AccessDesensitization of beta-adrenergic receptors by beta-adrenergic agonists in a cell-free system: resensitization by guanosine 5'-(beta, gamma-imino)triphosphate and other purine nucleotides.
Author(s) -
Chhabirani Mukherjee,
Robert J. Lefkowitz
Publication year - 1976
Publication title -
proceedings of the national academy of sciences of the united states of america
Language(s) - English
Resource type - Journals
eISSN - 1091-6490
pISSN - 0027-8424
DOI - 10.1073/pnas.73.5.1494
Subject(s) - adenylate kinase , receptor , adrenergic receptor , cyclase , beta (programming language) , beta adrenergic receptor kinase , dihydroalprenolol , chemistry , endocrinology , desensitization (medicine) , medicine , guanosine , adrenergic , biochemistry , biology , antagonist , g protein coupled receptor , partial agonist , computer science , programming language
Incubation of purified frog erythrocyte membranes with beta-adrenergic agonists at 25 degrees produces relatively rapid (half-time about 10 min) desensitization (inactivation) of about 60% of the beta-adrenergic receptor binding sites. The desensitized receptors no longer bind the specific beta-adrenergic ligand (-)[3H]dihydroalprenolol. The decrease in the number of functional beta-adrenergic receptors is also manifest as a decreased ability of isoproterenol to stimulate the membrane-bound adenylate cyclase.