PT - JOURNAL ARTICLE AU - Krause, Ryoko M. AU - Buisson, Bruno AU - Bertrand, Sonia AU - Corringer, Pierre-Jean AU - Galzi, Jean-Luc AU - Changeux, Jean-Pierre AU - Bertrand, Daniel TI - Ivermectin: A Positive Allosteric Effector of the α7 Neuronal Nicotinic Acetylcholine Receptor AID - 10.1124/mol.53.2.283 DP - 1998 Feb 01 TA - Molecular Pharmacology PG - 283--294 VI - 53 IP - 2 4099 - http://molpharm.aspetjournals.org/content/53/2/283.short 4100 - http://molpharm.aspetjournals.org/content/53/2/283.full SO - Mol Pharmacol1998 Feb 01; 53 AB - We report that preapplication of ivermectin, in the micromolar range, strongly enhances the subsequent acetylcholine-evoked current of the neuronal chick or human α7 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 α7 nicotinic acetylcholine receptors.