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Solubilization of rat liver alpha 1-adrenergic receptors. Agonist specific alteration in receptor binding affinity.

Publication ,  Journal Article
Wikberg, JE; Lefkowitz, RJ; Caron, MG
Published in: Biochem Pharmacol
November 1, 1983

An improved method for the solubilization of the alpha 1-adrenergic receptors in rat liver, utilizing digitonin, glycerol and sonication, is described. The yield of solubilized receptors was approximately 20%. The soluble receptors showed characteristics similar to the membrane-bound alpha 1 receptors. However, upon solubilization, the affinity for the agonists (-)norepinephrine and (-)epinephrine increased 35- to 66-fold when compared to the affinity in the membranes. The affinity for antagonists remained unchanged. A number of synthetic partial agonists showed a less marked (5- to 10-fold) increase in affinity upon solubilization. These data are consistent with the notion that these receptors might be capable of existing in two distinct conformational states with the high affinity state for agonists being favored by solubilization.

Duke Scholars

Published In

Biochem Pharmacol

DOI

ISSN

0006-2952

Publication Date

November 1, 1983

Volume

32

Issue

21

Start / End Page

3171 / 3178

Location

England

Related Subject Headings

  • Tetralones
  • Solubility
  • Receptors, Adrenergic, alpha
  • Rats
  • Protein Conformation
  • Protein Binding
  • Phenethylamines
  • Pharmacology & Pharmacy
  • Liver
  • Kinetics
 

Citation

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ICMJE
MLA
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Wikberg, J. E., Lefkowitz, R. J., & Caron, M. G. (1983). Solubilization of rat liver alpha 1-adrenergic receptors. Agonist specific alteration in receptor binding affinity. Biochem Pharmacol, 32(21), 3171–3178. https://doi.org/10.1016/0006-2952(83)90200-9
Wikberg, J. E., R. J. Lefkowitz, and M. G. Caron. “Solubilization of rat liver alpha 1-adrenergic receptors. Agonist specific alteration in receptor binding affinity.Biochem Pharmacol 32, no. 21 (November 1, 1983): 3171–78. https://doi.org/10.1016/0006-2952(83)90200-9.
Wikberg JE, Lefkowitz RJ, Caron MG. Solubilization of rat liver alpha 1-adrenergic receptors. Agonist specific alteration in receptor binding affinity. Biochem Pharmacol. 1983 Nov 1;32(21):3171–8.
Wikberg, J. E., et al. “Solubilization of rat liver alpha 1-adrenergic receptors. Agonist specific alteration in receptor binding affinity.Biochem Pharmacol, vol. 32, no. 21, Nov. 1983, pp. 3171–78. Pubmed, doi:10.1016/0006-2952(83)90200-9.
Wikberg JE, Lefkowitz RJ, Caron MG. Solubilization of rat liver alpha 1-adrenergic receptors. Agonist specific alteration in receptor binding affinity. Biochem Pharmacol. 1983 Nov 1;32(21):3171–3178.
Journal cover image

Published In

Biochem Pharmacol

DOI

ISSN

0006-2952

Publication Date

November 1, 1983

Volume

32

Issue

21

Start / End Page

3171 / 3178

Location

England

Related Subject Headings

  • Tetralones
  • Solubility
  • Receptors, Adrenergic, alpha
  • Rats
  • Protein Conformation
  • Protein Binding
  • Phenethylamines
  • Pharmacology & Pharmacy
  • Liver
  • Kinetics