Desensitization of β -adrenergic Receptors by β -adrenergic Agonists in a Cell-Free System: Resensitization by Guanosine 5'-(β ,γ -imino) Triphosphate and other Purine Nucleotides
Abstract
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.
- Publication:
-
Proceedings of the National Academy of Science
- Pub Date:
- May 1976
- DOI:
- 10.1073/pnas.73.5.1494
- Bibcode:
- 1976PNAS...73.1494M