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Binding of [3H]-pilocarpine to membranes from rat cerebral cortex

Academic Article
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Overview

authors

  • Hedlund, B.
  • Bartfai, Tamas

publication date

  • 1981

journal

  • Naunyn-Schmiedebergs Archives of Pharmacology  Journal

abstract

  • Binding of [3H]-pilocarpine to synaptic membranes in rat cerebral cortex was investigated, pilocarpine binding was also studied by competition of unlabelled pilocarpine with the [3H]-labelled muscarinic antagonist, [3H]-N-methyl-4-piperidinyl benzilate. 1. [3H]-pilocarpine binding sites are of protein nature, and the highest specific activity of binding is found in the synaptosomal fraction of all subcellular fractions. 2. Competition studies show that only muscarinic drugs inhibit [3H]-pilocarpine binding in their pharmacologically active concentration range. 3. Binding of [3H]-pilocarpine is influenced by GMPP-(NH)P (0.1 mM) similarly to the binding of other muscarinic agonists. 4. Examination of pilocarpine binding with [3H]-pilocarpine and the competition experiments with unlabelled pilocarpine indicate the presence of three sites with different affinities: 5 nM, 0.2 microM and 30 microM respectively. 5. Experiments with [3H]-4-NMPB and [3H]-pilocarpine indicate that there are more [3H]-pilocarpine binding sites than [3H]-4-NMPB binding sites in rat cerebral cortex.

subject areas

  • Animals
  • Binding Sites
  • Cerebral Cortex
  • In Vitro Techniques
  • Kinetics
  • Male
  • Membranes
  • Pilocarpine
  • Protein Binding
  • Rats
  • Rats, Inbred Strains
  • Receptors, Muscarinic
  • Synaptosomes
  • Trypsin
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Identity

International Standard Serial Number (ISSN)

  • 0028-1298

Digital Object Identifier (DOI)

  • 10.1007/bf00500067

PubMed ID

  • 7300915
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Additional Document Info

start page

  • 126

end page

  • 130

volume

  • 317

issue

  • 2

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