The subunit composition and pharmacology of α-Conotoxin MII-binding nicotinic acetylcholine receptors studied by a novel membrane-binding assay
Copyright policy )The subunit composition and pharmacology of α-Conotoxin MII-binding nicotinic acetylcholine receptors studied by a novel membrane-binding assay
The subunit composition and pharmacology of alpha-Conotoxin MII-binding (alpha-CtxMII) nicotinic acetylcholine receptors (nAChR) was studied by an improved [(125)I]-alpha-CtxMII membrane binding method. This binding method facilitates pharmacological studies that have been difficult to accomplish with [(125)I]-alpha-CtxMII autoradiography or alpha-CtxMII inhibition of [(125)I]-epibatidine binding. Binding densities and K(d)-values obtained by this [(125)I]-alpha-CtxMII membrane binding were similar to the values obtained by autoradiography or alpha-CtxMII inhibition of [(125)I]-epibatidine binding, verifying that each of these approaches measures the same nAChR population. Binding results with nAChR subunit-null mutant mice confirm and extend observations from earlier studies: [(125)I]-alpha-CtxMII binding measures two sets of alpha6beta2* nAChR (alpha4alpha6beta2beta3 or alpha6beta2beta3). Most nicotinic agonists and antagonists show monophasic inhibition of [(125)I]-alpha-CtxMII binding, indicating that alpha4alpha6beta2beta3 and alpha6beta2beta3 have similar binding properties. Comparison of the binding and activation profiles of alpha6beta2* nAChR to those of other nAChR subtypes (alpha4beta2* and beta4*) indicates that these receptors have distinctly different pharmacology indicating that it may be possible to target alpha6beta2* nAChR selectively to develop compounds that might be therapeutically useful.
- University of Colorado System United States
- University of Colorado Boulder United States
- University of Utah United States
Male, Nicotine, Dose-Response Relationship, Drug, Cell Membrane, Brain, Hydrogen-Ion Concentration, Bridged Bicyclo Compounds, Heterocyclic, Azocines, Binding, Competitive, Acetylcholine, Mice, Mutant Strains, Mice, Inbred C57BL, Mice, Alkaloids, Iodine Isotopes, Animals, Azetidines, Drug Interactions, Nicotinic Agonists, Conotoxins
Male, Nicotine, Dose-Response Relationship, Drug, Cell Membrane, Brain, Hydrogen-Ion Concentration, Bridged Bicyclo Compounds, Heterocyclic, Azocines, Binding, Competitive, Acetylcholine, Mice, Mutant Strains, Mice, Inbred C57BL, Mice, Alkaloids, Iodine Isotopes, Animals, Azetidines, Drug Interactions, Nicotinic Agonists, Conotoxins
citations This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).65 popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.Average influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).Top 10% impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.Top 10%
Citations provided by BIP!Popularity provided by BIP!