Skip to main content
Journal cover image

Agonist-induced increase in apparent beta-adrenergic receptor size.

Publication ,  Journal Article
Limbird, LE; Lefkowitz, RJ
Published in: Proc Natl Acad Sci U S A
January 1978

The properties of digitonin-solubilized beta-adrenergic receptors from frog erythrocyte membranes were studied by gel exclusion chromatography on AcA 34 Ultragel. beta-Adrenergic receptor binding activity in these membranes can be identified by both an agonist ligand, [(3)H]hydroxybenzylisoproterenol, and the antagonist ligands, [(3)H]dihydroalprenolol and (125)I-labeled hydroxybenzylpindolol. Occupancy of the beta-adrenergic receptors with the [(3)H]hydroxybenzylisoproterenol agonist prior to their solubilization from the membrane leads to an increase in apparent receptor size. Alterations in the molecular size of the receptor cannot be mimicked by occupancy of the binding site with the antagonist ligands. Exposure of frog erythrocyte membranes to [(3)H]hydroxybenzylisoproterenol agonist in the presence of 10 muM Gpp(NH)(p), a guanyl nucleotide analog that exerts multiple regulatory effects on the catecholamine-sensitive adenylate cyclase [ATP pyrophosphate-lyase (cyclizing); EC 4.6.1.1] system, results in the elution of the [(3)H]hydroxybenzylisoproterenol radioligand in both the region characteristic of the agonist-receptor complex and the region characteristic of the antagonist-receptor complex. The precise molecular interactions responsible for the agonist-induced increase in apparent beta-adrenergic receptor size are still unresolved. However, the low concentrations of agonist that are capable of altering apparent receptor size and the sensitivity of this effect to guanyl nucleotides suggest that these phenomena may be intimately involved in eliciting the physiological effects of beta-adrenergic catecholamines at the molecular level.

Duke Scholars

Published In

Proc Natl Acad Sci U S A

DOI

ISSN

0027-8424

Publication Date

January 1978

Volume

75

Issue

1

Start / End Page

228 / 232

Location

United States

Related Subject Headings

  • Receptors, Adrenergic, beta
  • Receptors, Adrenergic
  • Protein Conformation
  • Pindolol
  • Isoproterenol
  • Guanylyl Imidodiphosphate
  • Erythrocyte Membrane
  • Chromatography, Gel
  • Anura
  • Animals
 

Citation

APA
Chicago
ICMJE
MLA
NLM
Limbird, L. E., & Lefkowitz, R. J. (1978). Agonist-induced increase in apparent beta-adrenergic receptor size. Proc Natl Acad Sci U S A, 75(1), 228–232. https://doi.org/10.1073/pnas.75.1.228
Limbird, L. E., and R. J. Lefkowitz. “Agonist-induced increase in apparent beta-adrenergic receptor size.Proc Natl Acad Sci U S A 75, no. 1 (January 1978): 228–32. https://doi.org/10.1073/pnas.75.1.228.
Limbird LE, Lefkowitz RJ. Agonist-induced increase in apparent beta-adrenergic receptor size. Proc Natl Acad Sci U S A. 1978 Jan;75(1):228–32.
Limbird, L. E., and R. J. Lefkowitz. “Agonist-induced increase in apparent beta-adrenergic receptor size.Proc Natl Acad Sci U S A, vol. 75, no. 1, Jan. 1978, pp. 228–32. Pubmed, doi:10.1073/pnas.75.1.228.
Limbird LE, Lefkowitz RJ. Agonist-induced increase in apparent beta-adrenergic receptor size. Proc Natl Acad Sci U S A. 1978 Jan;75(1):228–232.
Journal cover image

Published In

Proc Natl Acad Sci U S A

DOI

ISSN

0027-8424

Publication Date

January 1978

Volume

75

Issue

1

Start / End Page

228 / 232

Location

United States

Related Subject Headings

  • Receptors, Adrenergic, beta
  • Receptors, Adrenergic
  • Protein Conformation
  • Pindolol
  • Isoproterenol
  • Guanylyl Imidodiphosphate
  • Erythrocyte Membrane
  • Chromatography, Gel
  • Anura
  • Animals