Ivermectin: a positive allosteric effector of the alpha7 neuronal nicotinic acetylcholine receptor.
Mol Pharmacol
; 53(2): 283-94, 1998 Feb.
Article
em En
| MEDLINE
| ID: mdl-9463487
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.
Buscar no Google
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ivermectina
/
Receptores Nicotínicos
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Mol Pharmacol
Ano de publicação:
1998
Tipo de documento:
Article
País de afiliação:
Suíça