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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.

Publication ,  Journal Article
Mukherjee, C; Lefkowitz, RJ
Published in: Proc Natl Acad Sci U S A
May 1976

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.

Duke Scholars

Published In

Proc Natl Acad Sci U S A

DOI

ISSN

0027-8424

Publication Date

May 1976

Volume

73

Issue

5

Start / End Page

1494 / 1498

Location

United States

Related Subject Headings

  • Structure-Activity Relationship
  • Receptors, Adrenergic
  • Purine Nucleotides
  • Propranolol
  • Kinetics
  • Isoproterenol
  • Guanosine Triphosphate
  • Erythrocytes
  • Enzyme Activation
  • Dose-Response Relationship, Drug
 

Citation

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Mukherjee, C., & Lefkowitz, R. J. (1976). 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. Proc Natl Acad Sci U S A, 73(5), 1494–1498. https://doi.org/10.1073/pnas.73.5.1494
Mukherjee, C., and R. J. Lefkowitz. “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.Proc Natl Acad Sci U S A 73, no. 5 (May 1976): 1494–98. https://doi.org/10.1073/pnas.73.5.1494.
Mukherjee, C., and R. J. Lefkowitz. “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.Proc Natl Acad Sci U S A, vol. 73, no. 5, May 1976, pp. 1494–98. Pubmed, doi:10.1073/pnas.73.5.1494.
Journal cover image

Published In

Proc Natl Acad Sci U S A

DOI

ISSN

0027-8424

Publication Date

May 1976

Volume

73

Issue

5

Start / End Page

1494 / 1498

Location

United States

Related Subject Headings

  • Structure-Activity Relationship
  • Receptors, Adrenergic
  • Purine Nucleotides
  • Propranolol
  • Kinetics
  • Isoproterenol
  • Guanosine Triphosphate
  • Erythrocytes
  • Enzyme Activation
  • Dose-Response Relationship, Drug