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EVIDENCE FOR THE STABILISATION OF THE HIGH-AFFINITY STATE OF β-ADRENOCEPTORS BY AN ENDOGENOUS FACTOR IN RAT BRAIN
- Source :
- Pharmacological Research. 37:365-373
- Publication Year :
- 1998
- Publisher :
- Elsevier BV, 1998.
-
Abstract
- Inhibition of binding of the labelled antagonist (-)[3H]CGP 12177 by the full agonist (-)isoproterenol results in shallow competition curves, characteristic of the presence of both high- and low-affinity states of beta-adrenoceptors (betaAR). When in excess, the GTP analog 5'-guanylylimidodiphosphate (GppNHp) is expected to convert all receptors in the high-affinity state to the low-affinity state. However, in the rat cortex and cerebellum synaptosomes, a proportion of the betaAR in the high-affinity state was GppNHp-insensitive. This apparent GppNHp-insensitivity decreased with decreasing temperature of incubation. Moreover, it was totally abolished by the gentle treatment of membranes with 3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate (CHAPS). We propose that a protein factor interacts with the betaAR/Gs protein complex and that it induces the GppNHp-insensitivity. This factor would be released by CHAPS in a functional form because it may regenerate the GppNHp-insensitivity after concentration and reconstitution with CHAPS-treated membranes. It is likely that the factor acts as a stabiliser of betaAR in the high-affinity state.
- Subjects :
- Male
Agonist
medicine.medical_specialty
GTP'
medicine.drug_class
G protein
Endogeny
Propanolamines
GTP-Binding Proteins
Chaps
Internal medicine
Receptors, Adrenergic, beta
medicine
Animals
Rats, Wistar
Receptor
Pharmacology
Guanylyl Imidodiphosphate
Chemistry
Isoproterenol
Temperature
Antagonist
Brain
Cholic Acids
Rats
Membrane
Endocrinology
Biophysics
Synaptosomes
Subjects
Details
- ISSN :
- 10436618
- Volume :
- 37
- Database :
- OpenAIRE
- Journal :
- Pharmacological Research
- Accession number :
- edsair.doi.dedup.....ff2a9596e550c1643a2f5cf30a4a1179