Inhibition of the α9α10 nicotinic cholinergic receptor by neramexane, an open channel blocker of N-methyl-d-aspartate receptors
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...
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| Otros Autores: | , , , , , , |
| Formato: | Capítulo de libro |
| Lenguaje: | Inglés |
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2007
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| Acceso en línea: | Registro en Scopus DOI Handle Registro en la Biblioteca Digital |
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| LEADER | 15834caa a22017657a 4500 | ||
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| 001 | PAPER-6496 | ||
| 003 | AR-BaUEN | ||
| 005 | 20230518203611.0 | ||
| 008 | 190411s2007 xx ||||fo|||| 00| 0 eng|d | ||
| 024 | 7 | |2 scopus |a 2-s2.0-34249046017 | |
| 024 | 7 | |2 cas |a memantine, 19982-08-2, 41100-52-1; neramexane, 209185-99-9, 219810-59-0, 457068-92-7; acetylcholine, 51-84-3, 60-31-1, 66-23-9; Acetylcholine, 51-84-3; Cyclopentanes; Memantine, 19982-08-2; MRZ 2579; Nicotinic Antagonists; Protein Subunits; Receptors, N-Methyl-D-Aspartate; Receptors, Nicotinic; Recombinant Proteins | |
| 040 | |a Scopus |b spa |c AR-BaUEN |d AR-BaUEN | ||
| 030 | |a EJPHA | ||
| 100 | 1 | |a Plazas, P.V. | |
| 245 | 1 | 0 | |a Inhibition of the α9α10 nicotinic cholinergic receptor by neramexane, an open channel blocker of N-methyl-d-aspartate receptors |
| 260 | |c 2007 | ||
| 270 | 1 | 0 | |m Plazas, P.V.; Instituto de Investigaciones en Ingeniería Genética y Biología Molecular, Consejo Nacional de Investigaciones Científicas y TécnicasArgentina; email: plazas@dna.uba.ar |
| 506 | |2 openaire |e Política editorial | ||
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| 504 | |a Herrero, C.J., Garcia-Palomero, E., Pintado, A.J., Garcia, A.G., Montiel, C., Differential blockade of rat alpha3beta4 and alpha7 neuronal nicotinic receptors by omega-conotoxin MVIIC, omega-conotoxin GVIA and diltiazem (1999) Br. J. Pharmacol., 127, pp. 1375-1387 | ||
| 504 | |a Hesselink, M.B., Parsons, C.G., Wollenburg, C., Danysz, W., Brain distribution of an non-competitive NMDA receptor antagonist; comparison to its in vitro potency in electrophysiological studies (1999) Naunyn-Schmiedeberg's Arch. Pharmacol., 360, pp. 144-150 | ||
| 504 | |a Houghton, A.K., Parsons, C.G., Headley, P.M., Mrz 2/579, a fast kinetic NMDA channel blocker, reduces the development of morphine tolerance in awake rats (2001) Pain, 91, pp. 201-207 | ||
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| 504 | |a Katz, E., Elgoyhen, A.B., Gomez-Casati, M.E., Knipper, M., Vetter, D.E., Fuchs, P.A., Glowatzki, E., Developmental regulation of nicotinic synapses on cochlear inner hair cells (2004) J. Neurosci., 24, pp. 7814-7820 | ||
| 504 | |a Kotlinska, J., Biala, G., Rafalski, P., Bochenski, M., Danysz, W., Effect of neramexane on ethanol dependence and reinforcement (2004) Eur. J. Pharmacol., 503, pp. 95-98 | ||
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| 504 | |a Liu, Y., Belayev, L., Zhao, W., Busto, R., Ginsberg, M.D., MRZ 2/579, a novel non-competitive N-methyl-d-aspartate antagonist, reduces infarct volume and brain swelling and improves neurological deficit after focal cerebral ischemia in rats (2000) Brain Res., 862, pp. 111-119 | ||
| 504 | |a Lopez, M.G., Fonteriz, R.I., Gandia, L., de la Fuente, M., Villarroya, M., Garcia-Sancho, J., Garcia, A.G., The nicotinic acetylcholine receptor of the bovine chromaffin cell, a new target for dihydropyridines (1993) Eur. J. Pharmacol., 247, pp. 199-207 | ||
| 504 | |a Malyshkin, A.A., Medvedev, I.O., Danysz, W., Bespalov, A.Y., Anti-allodynic interactions between NMDA receptor channel blockers and morphine or clonidine in neuropathic rats (2005) Eur. J. Pharmacol., 519 (1-2), pp. 80-85 | ||
| 504 | |a Maskell, P.D., Speder, P., Newberry, N.R., Bermudez, I., Inhibition of human alpha 7 nicotinic acetylcholine receptors by open channel blockers of N-methyl-d-aspartate receptors (2003) Br. J. Pharmacol., 140, pp. 1313-1319 | ||
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| 504 | |a Parsons, C.G., Gruner, R., Rozental, J., Millar, J., Lodge, D., Patch clamp studies on the kinetics and selectivity of N-methyl-d-aspartate receptor antagonism by memantine (1-amino-3,5-dimethyladamantan) (1993) Neuropharmacology, 32, pp. 1337-1350 | ||
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| 520 | 3 | |a 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. © 2007 Elsevier B.V. All rights reserved. |l eng | |
| 536 | |a Detalles de la financiación: Universidad de Buenos Aires | ||
| 536 | |a Detalles de la financiación: Umweltbundesamt | ||
| 536 | |a Detalles de la financiación: Howard Hughes Medical Institute | ||
| 536 | |a Detalles de la financiación: Agencia Nacional de Promoción Científica y Tecnológica | ||
| 536 | |a Detalles de la financiación: Consejo Nacional de Investigaciones Científicas y Técnicas | ||
| 536 | |a Detalles de la financiación: This work was supported by an International Research Scholar grant from the Howard Hughes Medical Institute, ANPCyT and UBA (A.B.E.) and the Welcome Trust (N.S.M.). P.V.P. and M.E.G-C are supported by a CONICET fellowship, J.S. by an undergraduate fellowship from the University of Buenos Aires, and S.K. by a Welcome Trust studentship in Neuroscience. | ||
| 593 | |a Instituto de Investigaciones en Ingeniería Genética y Biología Molecular, Consejo Nacional de Investigaciones Científicas y Técnicas, Argentina | ||
| 593 | |a Departamento de Fisiología, Biología Molecular y Celular, FCEyN, Universidad de Buenos Aires, Argentina | ||
| 593 | |a Departamento de Farmacología, Facultad de Medicina, Universidad de Buenos Aires, Argentina | ||
| 593 | |a Merz Pharmaceuticals GmbH, Frankfurt am Main, Germany | ||
| 593 | |a Department of Pharmacology, University College London, London, United Kingdom | ||
| 690 | 1 | 0 | |a ACETYLCHOLINE |
| 690 | 1 | 0 | |a HAIR CELLS |
| 690 | 1 | 0 | |a N-METHYL-D-ASPARTATE RECEPTOR ANTAGONIST |
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| 690 | 1 | 0 | |a NICOTINIC ACETYLCHOLINE RECEPTORS |
| 690 | 1 | 0 | |a CYCLOHEXANE DERIVATIVE |
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| 690 | 1 | 0 | |a N METHYL DEXTRO ASPARTIC ACID RECEPTOR BLOCKING AGENT |
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| 690 | 1 | 0 | |a MEMANTINE |
| 690 | 1 | 0 | |a N METHYL DEXTRO ASPARTIC ACID RECEPTOR |
| 690 | 1 | 0 | |a NERAMEXANE |
| 690 | 1 | 0 | |a NICOTINIC RECEPTOR |
| 690 | 1 | 0 | |a NICOTINIC RECEPTOR BLOCKING AGENT |
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| 700 | 1 | |a Savino, J. | |
| 700 | 1 | |a Kracun, S. | |
| 700 | 1 | |a Gomez-Casati, M.E. | |
| 700 | 1 | |a Katz, E. | |
| 700 | 1 | |a Parsons, C.G. | |
| 700 | 1 | |a Millar, N.S. | |
| 700 | 1 | |a Elgoyhen, A.B. | |
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