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Ivermectin: a positive allosteric effector of the alpha7 neuronal nicotinic acetylcholine receptor.

Abstract : We report that preapplication of ivermectin, in the micromolar range, strongly enhances the subsequent acetylcholine-evoked current of the neuronal chick or human alpha7 nicotinic acetylcholine receptors reconstituted in Xenopus laevis oocytes and K-28 cells. This potentiation does not result from nonspecific Cl- currents. The concomitant increase in apparent affinity and cooperativity of the dose-response curve suggest that ivermectin acts as a positive allosteric effector. This interpretation is supported by the observation of an increase in efficiency of a partial agonist associated with the potentiation and by the differential effect of ivermectin on mutants within the M2 channel domain. Ivermectin effects reveal a novel allosteric site for pharmacological agents on neuronal alpha7 nicotinic acetylcholine receptors.
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Submitted on : Tuesday, February 27, 2018 - 1:45:08 PM
Last modification on : Wednesday, October 14, 2020 - 4:09:52 AM

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Ryoko Krause, Bruno Buisson, Sonia Bertrand, Pierre-Jean Corringer, Jean-Luc Galzi, et al.. Ivermectin: a positive allosteric effector of the alpha7 neuronal nicotinic acetylcholine receptor.. Molecular Pharmacology, American Society for Pharmacology and Experimental Therapeutics, 1998, 53 (2), pp.283-94. ⟨10.1124/mol.53.2.283⟩. ⟨pasteur-01718414⟩

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