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Two ligands may bind simultaneously to the muscarine receptor

Academic Article
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Overview

authors

  • Hedlund, B.
  • Grynfarb, M.
  • Bartfai, Tamas

publication date

  • 1982

journal

  • Naunyn-Schmiedebergs Archives of Pharmacology  Journal

abstract

  • Competition between 3H-3-quinuclidinyl benzilate (2 and 18 nM) and varying concentrations of antagonists (4-N-methyl piperidinyl benzilate (4-NMPB), atropine, scopolamine and pirenzepine (0-1000 nM) and agonists (acetylcholine, carbamylcholine, oxotremorine and pilocarpine (0.10(-10) to 10(-2) M)) was studied. Inhibition of specific 3H-3-quinuclidinyl benzilate binding was evaluated by Dixon plots which for both competing agonists and antagonists showed deviations from linearity. The best nonlinear least square fit to the Dixon plots was offered by a hyperbola, parabola or a straight line, depending on the ligand used. The data support a model of equilibrium binding which assumes that 3H-3-quinuclidinyl benzilate and one competing ligand molecule may simultaneously bind to the receptor at high concentrations of the competing ligand.

subject areas

  • Animals
  • Atropine
  • Benzilates
  • Benzodiazepinones
  • Binding Sites
  • Binding, Competitive
  • In Vitro Techniques
  • Kinetics
  • Ligands
  • Male
  • Models, Biological
  • Piperidines
  • Pirenzepine
  • Quinuclidinyl Benzilate
  • Rats
  • Receptors, Cholinergic
  • Receptors, Muscarinic
  • Scopolamine Hydrobromide
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Identity

International Standard Serial Number (ISSN)

  • 0028-1298

Digital Object Identifier (DOI)

  • 10.1007/bf00499064

PubMed ID

  • 6896905
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Additional Document Info

start page

  • 3

end page

  • 13

volume

  • 320

issue

  • 1

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