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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2005-4-7
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pubmed:abstractText |
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.
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pubmed:grant |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/A 85380,
http://linkedlifedata.com/resource/pubmed/chemical/Acetylcholine,
http://linkedlifedata.com/resource/pubmed/chemical/Alkaloids,
http://linkedlifedata.com/resource/pubmed/chemical/Azetidines,
http://linkedlifedata.com/resource/pubmed/chemical/Azocines,
http://linkedlifedata.com/resource/pubmed/chemical/Bicyclo Compounds, Heterocyclic,
http://linkedlifedata.com/resource/pubmed/chemical/Conotoxins,
http://linkedlifedata.com/resource/pubmed/chemical/Iodine Isotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Nicotine,
http://linkedlifedata.com/resource/pubmed/chemical/Nicotinic Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Nicotinic Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Protein Subunits,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridines,
http://linkedlifedata.com/resource/pubmed/chemical/Quinolizines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Nicotinic,
http://linkedlifedata.com/resource/pubmed/chemical/alpha-conotoxin MII,
http://linkedlifedata.com/resource/pubmed/chemical/cytisine,
http://linkedlifedata.com/resource/pubmed/chemical/epibatidine
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0028-3908
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
48
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
696-705
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:15814104-Acetylcholine,
pubmed-meshheading:15814104-Alkaloids,
pubmed-meshheading:15814104-Animals,
pubmed-meshheading:15814104-Azetidines,
pubmed-meshheading:15814104-Azocines,
pubmed-meshheading:15814104-Bicyclo Compounds, Heterocyclic,
pubmed-meshheading:15814104-Binding, Competitive,
pubmed-meshheading:15814104-Brain,
pubmed-meshheading:15814104-Cell Membrane,
pubmed-meshheading:15814104-Conotoxins,
pubmed-meshheading:15814104-Dose-Response Relationship, Drug,
pubmed-meshheading:15814104-Drug Interactions,
pubmed-meshheading:15814104-Hydrogen-Ion Concentration,
pubmed-meshheading:15814104-Iodine Isotopes,
pubmed-meshheading:15814104-Male,
pubmed-meshheading:15814104-Mice,
pubmed-meshheading:15814104-Mice, Inbred C57BL,
pubmed-meshheading:15814104-Mice, Mutant Strains,
pubmed-meshheading:15814104-Nicotine,
pubmed-meshheading:15814104-Nicotinic Agonists,
pubmed-meshheading:15814104-Nicotinic Antagonists,
pubmed-meshheading:15814104-Protein Binding,
pubmed-meshheading:15814104-Protein Subunits,
pubmed-meshheading:15814104-Pyridines,
pubmed-meshheading:15814104-Quinolizines,
pubmed-meshheading:15814104-Radioligand Assay,
pubmed-meshheading:15814104-Receptors, Nicotinic,
pubmed-meshheading:15814104-Time Factors
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pubmed:year |
2005
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pubmed:articleTitle |
The subunit composition and pharmacology of alpha-Conotoxin MII-binding nicotinic acetylcholine receptors studied by a novel membrane-binding assay.
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pubmed:affiliation |
Institute for Behavioral Genetics, University of Colorado, Boulder, 80309, USA. outi.salminen@helsinki.fi
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
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