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Vol. 53, Issue 2, 283-294, February 1998
7
Neuronal Nicotinic Acetylcholine Receptor
Department of Physiology, University Medical Center, 1211 Geneva 4, Switzerland (R.M.K., B.B., S.B., D.B.), and
URA Centre National de la
Recherche Scientifique D1284, Neurobiologie Moléculaire, Institut
Pasteur, 75724 Paris Cedex 15, France (P.-J.C., J.-L.G., J.-P.C.)
We report that preapplication of ivermectin, in the micromolar range,
strongly enhances the subsequent acetylcholine-evoked current of the
neuronal chick or human 
7 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 7 nicotinic acetylcholine receptors.
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