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PMID: 226997 Published · ppublish English Journal Article Research Support, U.S. Gov't, P.H.S.

Cholinergic activity regulates muscarinic receptors in central nervous system cultures.

Proceedings of the National Academy of Sciences of the United States of America ·Vol. 76 ·No. 8 ·1979-08-00 ·Pages 4141-5

Siman RG, Klein WL

Abstract

Muscarinic acetylcholine receptor activation induces a loss of muscarinic receptors from cultured neuroblastoma and embryonic chicken cerebrum cells. As measured by specific binding of [3H]quinuclidinyl benzilate, steady-state receptor concentrations decrease 75% in response to receptor-saturating concentrations of cholinomimetic drugs. Both the degree and duration of activation determine the extent of receptor loss. A method for analyzing receptor turnover, which does not rely upon protein synthesis inhibitors, shows that activated receptors have a half-life of 1.6 hr. The regulated rate of receptor disappearance begins as soon as activators are added, and the rate is maintained as long as activators are present. The receptor blocker atropine causes an increase in receptor levels in central nervous system cultures but has no effect on receptors in cultures of adrenergic neuroblastoma cells. Because spontaneous cholinergic activity is expected only in the central nervous system cultures, the increase likely reflects blockade of endogenous regulation. Cytochalasin B blocks receptor regulation, suggesting that regulation may be mediated by a process involving microfilaments.

MeSH Terms
Animals Brain/metabolism Cells, Cultured Chick Embryo Dose-Response Relationship, Drug Kinetics Neoplasms, Experimental/metabolism Neuroblastoma/metabolism Parasympathomimetics/metabolism Quinolinic Acids/metabolism Quinuclidinyl Benzilate Receptors, Cholinergic/metabolism Receptors, Muscarinic/metabolism Synaptic Transmission
Chemicals
Parasympathomimetics Quinolinic Acids Receptors, Cholinergic Receptors, Muscarinic Quinuclidinyl Benzilate
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Siman R G
Klein W L
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Article Info
Journal
Proceedings of the National Academy of Sciences of the United States of America
Abbr.
Proc Natl Acad Sci U S A
ISSN
0027-8424
DOI
10.1073/pnas.76.8.4141
Published
1979-08-00
Pages
4141-5
Language
English
Region
United States
NLM ID
7505876
PMCID
PMC383994
Subset
IM
External Links
PubMed source DOI: 10.1073/pnas.76.8.4141 PMC Full Text View journal details
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