Vinburnine decelerates [3H]N-methylscopolamine binding to recombinant human muscarinic M1-M4 acetylcholine receptors

Gábor Maksay, Tímea Bíró, Béla Kiss

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3 Citations (Scopus)

Abstract

The kinetics of [3H]N-methylscopolamine binding to membranes of Chinese hamster ovary (CHO) cells expressing muscarinic M1-M 4 acetylcholine receptors was studied. [3H]N- methylscopolamine dissociation was used for the "single-point" analysis of allosteric modulation by vinburnine (L-eburnamonine). [ 3H]N-methylscopolamine dissociation was decelerated by vinburnine with EC50 values of 29.5, 4.1, 9.5 and 15.0 μM for muscarinic M1-M4 receptors, respectively. Acetylcholine doubled the EC50 of vinburnine for muscarinic M3 receptors. These kinetic EC50 values correlated with equilibrium binding constants, supporting the ternary allosteric model. Vinburnine also decelerated the association of [3H]N-methylscopolamine binding, resulting in opposite cooperativity for muscarinic M1 and M2 receptors.

Original languageEnglish
Pages (from-to)229-232
Number of pages4
JournalEuropean Journal of Pharmacology
Volume483
Issue number2-3
DOIs
Publication statusPublished - Jan 12 2004

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Keywords

  • Acetylcholine
  • Eburnamonine
  • Kinetics of
  • Muscarinic M-M receptor
  • [H]N- methylscopolamine binding

ASJC Scopus subject areas

  • Pharmacology

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