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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
1994-1-24
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pubmed:abstractText |
cis-Methyldioxolane (CD) is a muscarinic receptor agonist. [3H]CD has been used to label a subpopulation of muscarinic receptors described as exhibiting high agonist affinity. Pharmacological evidence suggests that the population of receptors labeled by [3H]CD consists of m2 and/or m4 subtypes; however, no studies have directly addressed the subtype selectivity of [3H]CD. The present study characterizes binding of this ligand to individual human receptor subtypes expressed in transfected Chinese hamster ovary cells. Results indicate that [3H]CD binds with high affinity only to Hm2 receptors but not to all Hm2 receptors. Twenty-eight percent of Hm2 receptors bound [3H]CD with a KD of 3.5 +/- 0.5 nM. Binding was eliminated in the presence of guanosine 5'-O-(3-thiotriphosphate), indicating that the Hm2 receptors labeled by [3H]CD are those that are associated with GDP-bound G protein. Binding of [3H]CD by only a subpopulation of Hm2 receptors is in agreement with data generated from studies of [3H]CD binding in mammalian brain. Because muscarinic receptors have been implicated to play a role in the pathogenesis of both Alzheimer's and Parkinson's disease, as well as the neurotoxicity of organophosphorus compounds, knowledge of the binding specificity of the muscarinic agonist [3H]CD should aid research in these areas.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/2-methyldioxolane,
http://linkedlifedata.com/resource/pubmed/chemical/Dioxolanes,
http://linkedlifedata.com/resource/pubmed/chemical/Guanosine 5'-O-(3-Thiotriphosphate),
http://linkedlifedata.com/resource/pubmed/chemical/Parasympathomimetics,
http://linkedlifedata.com/resource/pubmed/chemical/Quinuclidinyl Benzilate,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Muscarinic
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0022-3042
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
62
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
388-91
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:8263542-Animals,
pubmed-meshheading:8263542-Binding, Competitive,
pubmed-meshheading:8263542-CHO Cells,
pubmed-meshheading:8263542-Cell Membrane,
pubmed-meshheading:8263542-Cricetinae,
pubmed-meshheading:8263542-Dioxolanes,
pubmed-meshheading:8263542-Guanosine 5'-O-(3-Thiotriphosphate),
pubmed-meshheading:8263542-Kinetics,
pubmed-meshheading:8263542-Parasympathomimetics,
pubmed-meshheading:8263542-Quinuclidinyl Benzilate,
pubmed-meshheading:8263542-Receptors, Muscarinic
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pubmed:year |
1994
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pubmed:articleTitle |
cis-Methyldioxolane specifically recognizes the m2 muscarinic receptor.
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pubmed:affiliation |
Department of Pharmacology, Duke University Medical Center, Durham, North Carolina 27710.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, U.S. Gov't, P.H.S.
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