Click here to close
Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly.
We suggest using a current version of Chrome,
FireFox, or Safari.
Br J Pharmacol
2003 Dec 01;1407:1313-9. doi: 10.1038/sj.bjp.0705559.
Show Gene links
Show Anatomy links
Inhibition of human alpha 7 nicotinic acetylcholine receptors by open channel blockers of N-methyl-D-aspartate receptors.
Maskell PD
,
Speder P
,
Newberry NR
,
Bermudez I
.
???displayArticle.abstract???
1. Human alpha 7 nicotinic acetylcholine (ACh) receptors were expressed in Xenopus oocytes and the effects of the N-methyl-D-aspartate (NMDA) receptor open channel blockers memantine and cerestat on this receptor were examined using two-electrode voltage-clamp recordings and 125I-alpha-bungarotoxin (125I-alpha-bgtx) binding. 2. Memantine and cerestat produced complete inhibition of ACh-induced inward currents with affinities similar to that reported for native NMDA receptors. Cerestat, IC50 1.7 (-1; +2) microm, was more potent than memantine, IC50 5 (-3;+8) microM, and the effects of both drugs were fully and rapidly reversible. 3. Inhibition of alpha 7 receptor function was voltage-independent, and it occurred at concentrations far lower than those needed to inhibit (never completely) binding of 125I-alpha-bgtx to alpha 7 receptors, suggesting that the effects of memantine or cerestat are noncompetitive. 4. These results provide evidence that human alpha 7 receptors are inhibited by memantine and cerestat and suggest that caution should be applied when using these compounds to study systems in which NMDA and nACh receptors co-exist.
Albers,
Aptiganel hydrochloride in acute ischemic stroke: a randomized controlled trial.
2001, Pubmed
Albers,
Aptiganel hydrochloride in acute ischemic stroke: a randomized controlled trial.
2001,
Pubmed
Buisson,
Open-channel blockers at the human alpha4beta2 neuronal nicotinic acetylcholine receptor.
1998,
Pubmed
Carlson,
Nicotine blocks TNF-alpha-mediated neuroprotection to NMDA by an alpha-bungarotoxin-sensitive pathway.
1998,
Pubmed
Champtiaux,
Subunit composition of functional nicotinic receptors in dopaminergic neurons investigated with knock-out mice.
2003,
Pubmed
Chen,
Open-channel block of N-methyl-D-aspartate (NMDA) responses by memantine: therapeutic advantage against NMDA receptor-mediated neurotoxicity.
1992,
Pubmed
Connolly,
Alpha 4-2 beta 2 and other nicotinic acetylcholine receptor subtypes as targets of psychoactive and addictive drugs.
1992,
Pubmed
,
Xenbase
Conroy,
Nicotinic receptor subtypes in the developing chick brain: appearance of a species containing the alpha4, beta2, and alpha5 gene products.
1998,
Pubmed
Dajas-Bailador,
The alpha7 nicotinic acetylcholine receptor subtype mediates nicotine protection against NMDA excitotoxicity in primary hippocampal cultures through a Ca(2+) dependent mechanism.
2000,
Pubmed
Danysz,
Aminoadamantanes as NMDA receptor antagonists and antiparkinsonian agents--preclinical studies.
1997,
Pubmed
Fryer,
Antidepressants noncompetitively inhibit nicotinic acetylcholine receptor function.
1999,
Pubmed
García-Colunga,
Modulation of nicotinic acetylcholine receptors by strychnine.
1999,
Pubmed
,
Xenbase
Gotti,
Human neuronal nicotinic receptors.
1997,
Pubmed
Groot Kormelink,
Cloning and sequence of full-length cDNAs encoding the human neuronal nicotinic acetylcholine receptor (nAChR) subunits beta3 and beta4 and expression of seven nAChR subunits in the human neuroblastoma cell line SH-SY5Y and/or IMR-32.
1997,
Pubmed
Halliwell,
The mechanism of action and pharmacological specificity of the anticonvulsant NMDA antagonist MK-801: a voltage clamp study on neuronal cells in culture.
1989,
Pubmed
Herrero,
Differential blockade of rat alpha3beta4 and alpha7 neuronal nicotinic receptors by omega-conotoxin MVIIC, omega-conotoxin GVIA and diltiazem.
1999,
Pubmed
,
Xenbase
Houlihan,
Effects of diltiazem on human nicotinic acetylcholine and GABA(A) receptors.
2000,
Pubmed
,
Xenbase
Houlihan,
Activity of cytisine and its brominated isosteres on recombinant human alpha7, alpha4beta2 and alpha4beta4 nicotinic acetylcholine receptors.
2001,
Pubmed
,
Xenbase
Kaneko,
Nicotine protects cultured cortical neurons against glutamate-induced cytotoxicity via alpha7-neuronal receptors and neuronal CNS receptors.
1997,
Pubmed
Klink,
Molecular and physiological diversity of nicotinic acetylcholine receptors in the midbrain dopaminergic nuclei.
2001,
Pubmed
Laudenbach,
Selective activation of central subtypes of the nicotinic acetylcholine receptor has opposite effects on neonatal excitotoxic brain injuries.
2002,
Pubmed
Le Novère,
The diversity of subunit composition in nAChRs: evolutionary origins, physiologic and pharmacologic consequences.
2002,
Pubmed
López,
The nicotinic acetylcholine receptor of the bovine chromaffin cell, a new target for dihydropyridines.
1993,
Pubmed
Lukas,
International Union of Pharmacology. XX. Current status of the nomenclature for nicotinic acetylcholine receptors and their subunits.
1999,
Pubmed
Mansvelder,
Long-term potentiation of excitatory inputs to brain reward areas by nicotine.
2000,
Pubmed
Minematsu,
Effects of a novel NMDA antagonist on experimental stroke rapidly and quantitatively assessed by diffusion-weighted MRI.
1993,
Pubmed
O'Dell,
Mecamylamine is a selective non-competitive antagonist of N-methyl-D-aspartate- and aspartate-induced currents in horizontal cells dissociated from the catfish retina.
1988,
Pubmed
Oliver,
Memantine inhibits efferent cholinergic transmission in the cochlea by blocking nicotinic acetylcholine receptors of outer hair cells.
2001,
Pubmed
,
Xenbase
Parsons,
Memantine is a clinically well tolerated N-methyl-D-aspartate (NMDA) receptor antagonist--a review of preclinical data.
1999,
Pubmed
Parsons,
Amino-alkyl-cyclohexanes are novel uncompetitive NMDA receptor antagonists with strong voltage-dependency and fast blocking kinetics: in vitro and in vivo characterization.
1999,
Pubmed
,
Xenbase
Parsons,
Comparative patch-clamp studies with freshly dissociated rat hippocampal and striatal neurons on the NMDA receptor antagonistic effects of amantadine and memantine.
1996,
Pubmed
Peng,
Human alpha 7 acetylcholine receptor: cloning of the alpha 7 subunit from the SH-SY5Y cell line and determination of pharmacological properties of native receptors and functional alpha 7 homomers expressed in Xenopus oocytes.
1994,
Pubmed
,
Xenbase
Peng,
Inducible, heterologous expression of human alpha7-nicotinic acetylcholine receptors in a native nicotinic receptor-null human clonal line.
1999,
Pubmed
Radcliffe,
Nicotinic stimulation produces multiple forms of increased glutamatergic synaptic transmission.
1998,
Pubmed
Radcliffe,
Nicotinic modulation of glutamate and GABA synaptic transmission of hippocampal neurons.
1999,
Pubmed
Rammes,
The N-methyl-D-aspartate receptor channel blockers memantine, MRZ 2/579 and other amino-alkyl-cyclohexanes antagonise 5-HT(3) receptor currents in cultured HEK-293 and N1E-115 cell systems in a non-competitive manner.
2001,
Pubmed
Rana,
Inhibition of neuronal nicotinic acetylcholine receptors by imipramine and desipramine.
1993,
Pubmed
Ryan,
Dose-related neuroprotective effects of chronic nicotine in 6-hydroxydopamine treated rats, and loss of neuroprotection in alpha4 nicotinic receptor subunit knockout mice.
2001,
Pubmed
Slater,
Effects of the plant alkaloid tetrandrine on human nicotinic acetylcholine receptors.
2002,
Pubmed
,
Xenbase
Zoli,
Increased neurodegeneration during ageing in mice lacking high-affinity nicotine receptors.
1999,
Pubmed
Zoli,
Identification of the nicotinic receptor subtypes expressed on dopaminergic terminals in the rat striatum.
2002,
Pubmed
