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Artículo

Inhibition of the α9α10 nicotinic cholinergic receptor by neramexane, an open channel blocker of N-methyl-d-aspartate receptors

Plazas, Paola VivianaIcon ; Savino, Jessica; Kracun, Sebastian; Gomez Casati, Maria EugeniaIcon ; Katz, EleonoraIcon ; Parsons, Christopher G.; Millar, Neil S.; Elgoyhen, Ana BelenIcon
Fecha de publicación: 07/2007
Editorial: Elsevier Science
Revista: European Journal of Pharmacology
ISSN: 0014-2999
Idioma: Inglés
Tipo de recurso: Artículo publicado
Clasificación temática:
Biología Celular, Microbiología

Resumen

In this study we report the effects of neramexane, a novel amino-alkyl-cyclohexane derivative that is a non-competitive N-methyl-d-aspartate (NMDA) receptor antagonist, on recombinant rat α9α10 nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes. We compared its effects with those of memantine, a well-studied pore blocker of NMDA receptors, currently used in therapeutics for the treatment of Alzheimer's disease. Our results indicate that both compounds block acetylcholine-evoked responses at micromolar concentrations with a rank order of potency of neramexane > memantine, P < 0.05. Block by neramexane of acetylcholine responses was not overcome at high concentrations of the agonist, indicative of a non-competitive inhibition. The lack of interaction of neramexane with the ligand binding domain was confirmed by radioligand binding experiments in transfected tsA201 cells. Moreover, block did not involve an increase in desensitization kinetics, it was independent of the resting potential of the membrane at low concentrations of neramexane and slightly voltage-dependent at concentrations higher than 1 μM. Finally, clinically-relevant concentrations of neramexane blocked native α9α10-containing nicotinic acetylcholine receptors of rat inner hair cells, thus demonstrating a possible in vivo relevance in potentially unexplored therapeutic areas.
Palabras clave: Acetylcholine , Hair Cells , N-Methyl-D-Aspartate Receptor Antagonist , Neramexane , Nicotinic Acetylcholine Receptors
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info:eu-repo/semantics/openAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Creative Commons Attribution-NonCommercial-ShareAlike 2.5 Unported (CC BY-NC-SA 2.5)
Identificadores
URI: http://hdl.handle.net/11336/79674
URL: https://www.ncbi.nlm.nih.gov/pubmed/17466293
DOI: http://dx.doi.org/10.1016/j.ejphar.2007.03.026
URL: https://www.sciencedirect.com/science/article/pii/S001429990700341X
Colecciones
Articulos(INGEBI)
Articulos de INST.DE INVEST.EN ING.GENETICA Y BIOL.MOLECULAR "DR. HECTOR N TORRES"
Citación
Plazas, Paola Viviana; Savino, Jessica; Kracun, Sebastian; Gomez Casati, Maria Eugenia; Katz, Eleonora; et al.; Inhibition of the α9α10 nicotinic cholinergic receptor by neramexane, an open channel blocker of N-methyl-d-aspartate receptors; Elsevier Science; European Journal of Pharmacology; 566; 1-3; 7-2007; 11-19
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