 |
Journal articles
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.
https://hal-pasteur.archives-ouvertes.fr/pasteur-01718414
Contributor : Ana Cova Rodrigues <>
Submitted on : Tuesday, February 27, 2018 - 1:45:08 PM
Last modification on : Wednesday, October 14, 2020 - 4:09:52 AM
Contributor : Ana Cova Rodrigues <>
Submitted on : Tuesday, February 27, 2018 - 1:45:08 PM
Last modification on : Wednesday, October 14, 2020 - 4:09:52 AM
Links full text
