Solubilization of a mammalian ?-adrenergic receptor
- 1 December 1978
- journal article
- research article
- Published by Springer Nature in Naunyn-Schmiedebergs Archiv für experimentelle Pathologie und Pharmakologie
- Vol. 305 (3), 191-200
- https://doi.org/10.1007/bf00498810
Abstract
Binding sites for iodohydroxybenzylpindolol with characteristics of a β2-adrenergic receptor have been identified in a crude membrane fraction from guinea-pig lung. The binding sites could be solubilized by treatment of the membrane fraction with digitonin. Upon solubilization receptors retain their β2-adrenergic type as indicated by the rank order of potencies of agonists in binding-inhibition experiments. The solubilized receptors demonstrate a marked increase in affinity for agonists compared with particulate receptors whereas antagonist affinity remains unchanged. Solubilized receptors are insensitive to divalent cations (Mg2+, Mn2+, Ca2+) which increase the potency of agonists for particulate receptors. The effects of Mg2+ can be reversed by Gpp(NH)p in particulate preparations; Gpp(NH)p is ineffective for the solubilized preparation. These experiments establish that β-adrenergic receptors can be solubilized even from crude mammalian membrane preparations. They also show that the mammalian β-adrenergic receptor in situ is under constraints with respect to agonist affinity and is modulated by divalent cations and guanyl nucleotides in the intact membrane.Keywords
This publication has 16 references indexed in Scilit:
- Catecholamine receptorsReviews of physiology, biochemistry and pharmacology, 2005
- Interaction of ligands with the opiate receptors of brain membranes: Regulation by ions and nucleotidesProceedings of the National Academy of Sciences, 1978
- Isolation of adenylate cyclase-free, beta-adrenergic receptor from turkey erythrocyte membranes by affinity chromatography.Proceedings of the National Academy of Sciences, 1977
- The receptor concept in evolutionBiochemical Pharmacology, 1977
- In Vitro Study of beta-Adrenergic ReceptorsAnnual Review of Pharmacology and Toxicology, 1977
- Binding of (125I)iodohydroxybenzylpindolol to putative beta-adrenergic receptors of rat glioma cells and other cell clones.Journal of Biological Chemistry, 1976
- ?-Adrenergic receptors in guinea-pig myocardial tissueNaunyn-Schmiedebergs Archiv für experimentelle Pathologie und Pharmakologie, 1976
- Cation Dependence of High-Affinity Angiotensin II Binding to Adrenal Cortex ReceptorsScience, 1974
- A highly sensitive adenylate cyclase assayAnalytical Biochemistry, 1974
- Angiotensin II Receptors in Bovine Adrenal CortexPublished by Elsevier ,1974