[3H]N-methylscopolamine dissociation from muscarine receptors affected by low concentrations of allosteric modulators

Arthur Christopoulos, Fred Mitchelson

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)

Abstract

The ability of allosteric ligands to modulate the dissociation rate of [3H]N-methylscopolamine from atrial muscarinic receptors in the presence of varying concentrations of unlabelled N-methylscopolamine or atropine was evaluated. Gallamine, at a concentration approximating its KD value, slowed the dissociation of [3H] N-methylscopolamine in the presence of ca. 30× KD of both unlabelled NMS or atropine. This was less evident when concentrations of ca. 1000× KD of the unlabelled antagonists were employed. Similar findings were made with another allosteric modulator. These results indicate that gallamine can act allosterically at low concentrations.

Original languageEnglish
Pages (from-to)259-262
Number of pages4
JournalEuropean Journal of Pharmacology: Molecular Pharmacology
Volume290
Issue number3
DOIs
Publication statusPublished - 15 Aug 1995

Keywords

  • Allosterism
  • Dissociation kinetics
  • Gallamine
  • [H]N-methylscopolamine

Cite this

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abstract = "The ability of allosteric ligands to modulate the dissociation rate of [3H]N-methylscopolamine from atrial muscarinic receptors in the presence of varying concentrations of unlabelled N-methylscopolamine or atropine was evaluated. Gallamine, at a concentration approximating its KD value, slowed the dissociation of [3H] N-methylscopolamine in the presence of ca. 30× KD of both unlabelled NMS or atropine. This was less evident when concentrations of ca. 1000× KD of the unlabelled antagonists were employed. Similar findings were made with another allosteric modulator. These results indicate that gallamine can act allosterically at low concentrations.",
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[3H]N-methylscopolamine dissociation from muscarine receptors affected by low concentrations of allosteric modulators. / Christopoulos, Arthur; Mitchelson, Fred.

In: European Journal of Pharmacology: Molecular Pharmacology, Vol. 290, No. 3, 15.08.1995, p. 259-262.

Research output: Contribution to journalArticleResearchpeer-review

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T1 - [3H]N-methylscopolamine dissociation from muscarine receptors affected by low concentrations of allosteric modulators

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AU - Mitchelson, Fred

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N2 - The ability of allosteric ligands to modulate the dissociation rate of [3H]N-methylscopolamine from atrial muscarinic receptors in the presence of varying concentrations of unlabelled N-methylscopolamine or atropine was evaluated. Gallamine, at a concentration approximating its KD value, slowed the dissociation of [3H] N-methylscopolamine in the presence of ca. 30× KD of both unlabelled NMS or atropine. This was less evident when concentrations of ca. 1000× KD of the unlabelled antagonists were employed. Similar findings were made with another allosteric modulator. These results indicate that gallamine can act allosterically at low concentrations.

AB - The ability of allosteric ligands to modulate the dissociation rate of [3H]N-methylscopolamine from atrial muscarinic receptors in the presence of varying concentrations of unlabelled N-methylscopolamine or atropine was evaluated. Gallamine, at a concentration approximating its KD value, slowed the dissociation of [3H] N-methylscopolamine in the presence of ca. 30× KD of both unlabelled NMS or atropine. This was less evident when concentrations of ca. 1000× KD of the unlabelled antagonists were employed. Similar findings were made with another allosteric modulator. These results indicate that gallamine can act allosterically at low concentrations.

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