Determination of the desensitization of beta-adrenergic receptors by [3H]CGP-12177.

The Biochemical journal ·Vol. 216 ·No. 3 ·1983-12-15 ·Pages 669-74

Hertel C, Müller P, Portenier M, Staehelin M

Abstract

Isoprenaline treatment of C6-glioma cells induced a fast decrease in the number of beta-adrenergic receptors as determined by binding of [3H]CGP-12177, which paralleled the decrease in the hormonally stimulated adenylate cyclase activity. The total number of receptors, as determined by binding of (-)-[3H]dihydroalprenolol, did not decrease. Separation of the beta-adrenergic receptors on a sucrose density gradient showed that the decrease in the number of receptors detectable with CGP-12177 was due to a movement of the receptors from the plasma membrane to a vesicular cell compartment. By using both (-)-[3H]dihydroalprenolol and [3H]CGP-12177 it is thus possible to differentiate between the total number of receptors and those present at the plasma membrane in an unfractionated cell lysate.

MeSH Terms

Adenylyl Cyclases/metabolism Adrenergic beta-Antagonists/metabolism Binding Sites Binding, Competitive Cell Line Cell Membrane/metabolism Centrifugation, Density Gradient Dihydroalprenolol/metabolism Glioma/metabolism Humans Isoproterenol/pharmacology Propanolamines/metabolism Receptors, Adrenergic, beta/drug effects

Chemicals

Adrenergic beta-Antagonists Propanolamines Receptors, Adrenergic, beta Dihydroalprenolol Adenylyl Cyclases Isoproterenol CGP 12177

Authors & Affiliations

4 authors, click to expand affiliations / ORCID

Hertel C

Müller P

Portenier M

Staehelin M

References (18)

18 references, click to expand

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Article Info

Journal

The Biochemical journal

Abbr.

Biochem J

ISSN

0264-6021

DOI

10.1042/bj2160669

Published

1983-12-15

Pages

669-74

Language

English

Region

England

NLM ID

2984726R

PMCID

PMC1152560

Subset

External Links

PubMed source DOI: 10.1042/bj2160669 PMC Full Text View journal details

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Determination of the desensitization of beta-adrenergic receptors by [3H]CGP-12177.

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