doi: 10.1016/0922-4106(95)90002-0.
[3H]N-methylscopolamine dissociation from muscarine receptors affected by low concentrations of allosteric modulators
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- PMID: 7589221
- DOI: 10.1016/0922-4106(95)90002-0
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[3H]N-methylscopolamine dissociation from muscarine receptors affected by low concentrations of allosteric modulators
Eur J Pharmacol.
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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 x KD of both unlabelled NMS or atropine. This was less evident when concentrations of ca. 1000 x 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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