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© Marie Prévost, Institut Pasteur
Image of a portion of a Xenopus oocyte expressing a channel receptor.
Publication : Molecular pharmacology

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

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Molecular pharmacology - 01 Feb 1998

Krause RM, Buisson B, Bertrand S, Corringer PJ, Galzi JL, Changeux JP, Bertrand D

Link to Pubmed [PMID] – 9463487

Mol. Pharmacol. 1998 Feb;53(2):283-94

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.

http://www.ncbi.nlm.nih.gov/pubmed/9463487