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.