Desensitization 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.
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.
D000262:Adenylyl Cyclases / Q000378:metabolism; D000318:Adrenergic beta-Agonists / Q000494:pharmacology*; D000526:Alprenolol / Q000031:analogs & derivatives / Q000378:metabolism; D000818:Animals; D002462:Cell Membrane / Q000201:enzymology / Q000378:metabolism; D002474:Cell-Free System; D004305:Dose-Response Relationship, Drug; D004789:Enzyme Activation / Q000187:drug effects; D004912:Erythrocytes / Q000378:metabolism / Q000648:ultrastructure; D006160:Guanosine Triphosphate / Q000031:analogs & derivatives / Q000494:pharmacology; D007545:Isoproterenol / Q000494:pharmacology; D007700:Kinetics; D011433:Propranolol / Q000494:pharmacology; D011685:Purine Nucleotides / Q000494:pharmacology*; D011941:Receptors, Adrenergic / Q000187:drug effects*; D013329:Structure-Activity Relationship
D000318:Adrenergic beta-Agonists; D011685:Purine Nucleotides; D011941:Receptors, Adrenergic; D006160:Guanosine Triphosphate; D000526:Alprenolol; D011433:Propranolol; D000262:Adenylyl Cyclases; D007545:Isoproterenol