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Br J Pharmacol
1999 Jan 01;1261:285-95. doi: 10.1038/sj.bjp.0702299.
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Selective effects of a 4-oxystilbene derivative on wild and mutant neuronal chick alpha7 nicotinic receptor.
Maggi L
,
Palma E
,
Eusebi F
,
Moretti M
,
Balestra B
,
Clementi F
,
Gotti C
.
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1. We assessed the pharmacological activity of triethyl-(beta-4-stilbenoxy-ethyl) ammonium (MG624), a drug that is active on neuronal nicotinic receptors (nicotinic AChR). Experiments on the major nicotinic AChR subtypes present in chick brain, showed that it inhibits the binding of [125I]-alphaBungarotoxin (alphaBgtx) to the alpha7 subtype, and that of [3H]-epibatidine (Epi) to the alpha4beta2 subtype, with Ki values of respectively 106 nM and 84 microM. 2. MG624 also inhibited ACh elicited currents (I(ACh)) in the oocyte-expressed alpha7 and alpha4beta2 chick subtypes with half-inhibitory concentrations (IC50) of respectively 109 nM and 3.2 microM. 3. When tested on muscle-type AChR, it inhibited [125I]-alphaBgtx binding with a Ki of 32 microM and ACh elicited currents (I(ACh)) in the oocyte-expressed alpha1beta1gammadelta chick subtype with an IC50 of 2.9 microM. 4. The interaction of MG624 with the alpha7 subtype was investigated using an alpha7 homomeric mutant receptor with a threonine-for-leucine 247 substitution (L247T alpha7). MG624 did not induce any current in oocytes expressing the wild type alpha7 receptor, but did induce large currents in the oocyte-expressed L247T alpha7 receptor. The MG624 elicited current (I(MG62)) has an EC50 of 0.2 nM and a Hill coefficient nH of 1.9, and is blocked by the nicotinic receptor antagonist methyllycaconitine (MLA). 5. These binding and electrophysiological studies show that MG624 is a potent antagonist of neuronal chick alpha7 nicotinic AChR, and becomes a competitive agonist following the mutation of the highly conserved leucine residue 247 located in the M2 channel domain.
Albuquerque,
Properties of neuronal nicotinic acetylcholine receptors: pharmacological characterization and modulation of synaptic function.
1997, Pubmed
Albuquerque,
Properties of neuronal nicotinic acetylcholine receptors: pharmacological characterization and modulation of synaptic function.
1997,
Pubmed
Anand,
Homomeric and native alpha 7 acetylcholine receptors exhibit remarkably similar but non-identical pharmacological properties, suggesting that the native receptor is a heteromeric protein complex.
1993,
Pubmed
,
Xenbase
Bertrand,
Paradoxical allosteric effects of competitive inhibitors on neuronal alpha7 nicotinic receptor mutants.
1997,
Pubmed
,
Xenbase
Bertrand,
Unconventional pharmacology of a neuronal nicotinic receptor mutated in the channel domain.
1992,
Pubmed
,
Xenbase
Bertrand,
Stratification of the channel domain in neurotransmitter receptors.
1993,
Pubmed
Colquhoun,
Effects of inhibitors of the binding of iodinated alpha-bungarotoxin to acetylcholine receptors in rat muscle.
1976,
Pubmed
Conroy,
The alpha 5 gene product assembles with multiple acetylcholine receptor subunits to form distinctive receptor subtypes in brain.
1992,
Pubmed
Conroy,
Neurons can maintain multiple classes of nicotinic acetylcholine receptors distinguished by different subunit compositions.
1995,
Pubmed
Corriveau,
Expression of neuronal acetylcholine receptor genes in vertebrate skeletal muscle during development.
1995,
Pubmed
Couturier,
A neuronal nicotinic acetylcholine receptor subunit (alpha 7) is developmentally regulated and forms a homo-oligomeric channel blocked by alpha-BTX.
1990,
Pubmed
,
Xenbase
Covernton,
Comparison of neuronal nicotinic receptors in rat sympathetic neurones with subunit pairs expressed in Xenopus oocytes.
1994,
Pubmed
,
Xenbase
Dani,
Molecular and cellular aspects of nicotine abuse.
1996,
Pubmed
Decker,
Diversity of neuronal nicotinic acetylcholine receptors: lessons from behavior and implications for CNS therapeutics.
1995,
Pubmed
Forsayeth,
Formation of oligomers containing the beta3 and beta4 subunits of the rat nicotinic receptor.
1997,
Pubmed
Fucile,
The neuronal alpha6 subunit forms functional heteromeric acetylcholine receptors in human transfected cells.
1998,
Pubmed
Fucile,
Alpha 5 subunit forms functional alpha 3 beta 4 alpha 5 nAChRs in transfected human cells.
1997,
Pubmed
,
Xenbase
Galzi,
Identification of calcium binding sites that regulate potentiation of a neuronal nicotinic acetylcholine receptor.
1996,
Pubmed
,
Xenbase
Gerzanich,
Comparative pharmacology of epibatidine: a potent agonist for neuronal nicotinic acetylcholine receptors.
1995,
Pubmed
,
Xenbase
Gotti,
Pharmacology and biophysical properties of alpha 7 and alpha 7-alpha 8 alpha-bungarotoxin receptor subtypes immunopurified from the chick optic lobe.
1994,
Pubmed
,
Xenbase
Gotti,
Alpha7 and alpha8 nicotinic receptor subtypes immunopurified from chick retina have different immunological, pharmacological and functional properties.
1997,
Pubmed
Gotti,
4-Oxystilbene compounds are selective ligands for neuronal nicotinic alphaBungarotoxin receptors.
1998,
Pubmed
Gotti,
Human neuronal nicotinic receptors.
1997,
Pubmed
Gotti,
Detection of antibody classes and subpopulations in myasthenia gravis patients using a new nonradioactive enzyme immunoassay.
1997,
Pubmed
Johnson,
alpha-Conotoxin ImI exhibits subtype-specific nicotinic acetylcholine receptor blockade: preferential inhibition of homomeric alpha 7 and alpha 9 receptors.
1995,
Pubmed
,
Xenbase
Kem,
Anabaseine is a potent agonist on muscle and neuronal alpha-bungarotoxin-sensitive nicotinic receptors.
1997,
Pubmed
,
Xenbase
Kuryatov,
Mutation causing autosomal dominant nocturnal frontal lobe epilepsy alters Ca2+ permeability, conductance, and gating of human alpha4beta2 nicotinic acetylcholine receptors.
1997,
Pubmed
,
Xenbase
Lewis,
The ion channel properties of a rat recombinant neuronal nicotinic receptor are dependent on the host cell type.
1997,
Pubmed
,
Xenbase
Lindstrom,
Nicotinic acetylcholine receptors in health and disease.
1997,
Pubmed
Léna,
Pathological mutations of nicotinic receptors and nicotine-based therapies for brain disorders.
1997,
Pubmed
MANTEGAZZA,
Central antinicotinic activity of 4-oxystilbene and 4-oxydiphenylethane derivatives.
1955,
Pubmed
McGehee,
Physiological diversity of nicotinic acetylcholine receptors expressed by vertebrate neurons.
1995,
Pubmed
Mileo,
Protein kinase C modulates exogenous acetylcholine current in Xenopus oocytes.
1995,
Pubmed
,
Xenbase
Munson,
Ligand: a versatile computerized approach for characterization of ligand-binding systems.
1980,
Pubmed
Palma,
Neuronal nicotinic alpha 7 receptor expressed in Xenopus oocytes presents five putative binding sites for methyllycaconitine.
1996,
Pubmed
,
Xenbase
Palma,
Threonine-for-leucine mutation within domain M2 of the neuronal alpha(7) nicotinic receptor converts 5-hydroxytryptamine from antagonist to agonist.
1996,
Pubmed
,
Xenbase
Revah,
Mutations in the channel domain alter desensitization of a neuronal nicotinic receptor.
1991,
Pubmed
,
Xenbase
Role,
Nicotinic receptors in the development and modulation of CNS synapses.
1996,
Pubmed
Sargent,
The diversity of neuronal nicotinic acetylcholine receptors.
1993,
Pubmed
Tzartos,
Characteristics of monoclonal antibodies to denatured Torpedo and to native calf acetylcholine receptors: species, subunit and region specificity.
1986,
Pubmed
Ullian,
Pronounced cellular diversity and extrasynaptic location of nicotinic acetylcholine receptor subunit immunoreactivities in the chicken pretectum.
1995,
Pubmed
Vernallis,
Neurons assemble acetylcholine receptors with as many as three kinds of subunits while maintaining subunit segregation among receptor subtypes.
1993,
Pubmed
Ward,
Methyllycaconitine: a selective probe for neuronal alpha-bungarotoxin binding sites.
1990,
Pubmed
Whiting,
Characterization of bovine and human neuronal nicotinic acetylcholine receptors using monoclonal antibodies.
1988,
Pubmed
Whiting,
Structurally different neuronal nicotinic acetylcholine receptor subtypes purified and characterized using monoclonal antibodies.
1987,
Pubmed
Whiting,
Structural and pharmacological characterization of the major brain nicotinic acetylcholine receptor subtype stably expressed in mouse fibroblasts.
1991,
Pubmed
Whiting,
Expression of nicotinic acetylcholine receptor subtypes in brain and retina.
1991,
Pubmed
Wonnacott,
Presynaptic nicotinic ACh receptors.
1997,
Pubmed
