Click here to close Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly. We suggest using a current version of Chrome, FireFox, or Safari.
XB-ART-15324
Mol Pharmacol 1998 Feb 01;532:283-94.
Show Gene links Show Anatomy links

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

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


???displayArticle.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.

???displayArticle.pubmedLink??? 9463487
???displayArticle.link??? Mol Pharmacol