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PMID: 5723 Published · ppublish English Journal Article Research Support, U.S. Gov't, P.H.S.

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.

Proceedings of the National Academy of Sciences of the United States of America ·Vol. 73 ·No. 5 ·1976-05-00 ·Pages 1494-8

Mukherjee C, Lefkowitz RJ

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.

MeSH Terms
Adenylyl Cyclases/metabolism Adrenergic beta-Agonists/pharmacology Alprenolol/analogs & derivatives,metabolism Animals Cell Membrane/enzymology,metabolism Cell-Free System Dose-Response Relationship, Drug Enzyme Activation/drug effects Erythrocytes/metabolism,ultrastructure Guanosine Triphosphate/analogs & derivatives,pharmacology Isoproterenol/pharmacology Kinetics Propranolol/pharmacology Purine Nucleotides/pharmacology Receptors, Adrenergic/drug effects Structure-Activity Relationship
Chemicals
Adrenergic beta-Agonists Purine Nucleotides Receptors, Adrenergic Guanosine Triphosphate Alprenolol Propranolol Adenylyl Cyclases Isoproterenol
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Mukherjee C
Lefkowitz R J
References (15)
15 references, click to expand
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Article Info
Journal
Proceedings of the National Academy of Sciences of the United States of America
Abbr.
Proc Natl Acad Sci U S A
ISSN
0027-8424
DOI
10.1073/pnas.73.5.1494
Published
1976-05-00
Pages
1494-8
Language
English
Region
United States
NLM ID
7505876
PMCID
PMC430323
Subset
IM
External Links
PubMed source DOI: 10.1073/pnas.73.5.1494 PMC Full Text View journal details
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