Muscarinic cholinergic binding in rat brain.

Proceedings of the National Academy of Sciences of the United States of America ·Vol. 71 ·No. 5 ·1974-05-00 ·Pages 1725-9

Yamamura HI, Snyder SH

Abstract

Binding sites with high affinity and specificity for [(3)H]quinuclidinyl benzilate (QNB) are present in homogenates of rat brain. The characteristics of the binding sites resemble those of muscarinic cholinergic receptors. Specific binding is saturable with respect to [(3)H]QNB and tissue concentration and is time-, temperature-, and pH-dependent. The bimolecular rate of association (2.0 x 10(8) M(-1) min(-1)) and dissociation (1.2 x 10(-2) min(-1)) at 35 degrees indicate a dissociation constant of 60 pM and a density of 65 pmol/g of brain. Muscarinic antagonists and agonists displace specific [(3)H]QNB binding, while nicotinic and non-cholinergic drugs possess little affinity for [(3)H]QNB-binding sites.

MeSH Terms

Acetylcholine/pharmacology Animals Arecoline/pharmacology Atropine/pharmacology Benzilates/metabolism Binding Sites Binding, Competitive Brain/metabolism Brompheniramine/pharmacology Carbachol/pharmacology Chlorpheniramine/pharmacology Hydrogen-Ion Concentration In Vitro Techniques Kinetics Male Methacholine Compounds/pharmacology Microsomes/metabolism Mitochondria/metabolism Oxotremorine/metabolism Pilocarpine/pharmacology Quaternary Ammonium Compounds/pharmacology Quinuclidines/metabolism Rats Receptors, Cholinergic Scopolamine/pharmacology Temperature Time Factors Tritium

Chemicals

Benzilates Methacholine Compounds Quaternary Ammonium Compounds Quinuclidines Receptors, Cholinergic Pilocarpine Tritium Chlorpheniramine Arecoline Oxotremorine Atropine Carbachol Scopolamine Brompheniramine Acetylcholine

Authors & Affiliations

2 authors, click to expand affiliations / ORCID

Yamamura H I

Snyder S H

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35 references, click to expand

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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.71.5.1725

Published

1974-05-00

Pages

1725-9

Language

English

Region

United States

NLM ID

7505876

PMCID

PMC388311

Subset

External Links

PubMed source DOI: 10.1073/pnas.71.5.1725 PMC Full Text View journal details

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Muscarinic cholinergic binding in rat brain.

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