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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
9
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pubmed:dateCreated |
1981-12-22
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pubmed:abstractText |
alpha-[3H]Dihydropicrotoxinin (DHP) and [3H]diazepam binding proteins were solubilized from rat brain membranes with 1% Lubrol-Px. Gel filtration of the Lubrol-solubilized fraction revealed that [3H]DHP and [3H]diazepam bind to two distinct peaks with apparent molecular weights of 185,000 and 61,000, respectively. The signal-to-noise ratio of [3H]DHP binding to 185,000-dalton fractions was improved significantly. [3H]DHP bound to the 185,000-dalton fraction with two binding constants. Muscimol and pentobarbital, while enhancing [3H]diazepam binding to membrane and crude Lubrol-solubilized fractions, failed to enhance [3H]diazepam binding to the 61,000-dalton fraction. Pentobarbital inhibited the binding of [3H]DHP to the 185,000-dalton fraction with an IC50 value of 60 +/- 12 micro M. The binding of [3H]DHP alos was inhibited by several depressant and convulsant drugs which affect gamma-aminobutyric acid (GABA)-mediated transmission. These results provide strong evidence that picrotoxinin and diazepam bind to two distinct proteins and that pentobarbital may act at the picrotoxinin-sensitive site of the benzodiazepine . GABA receptor . ionophore complex.
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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/Diazepam,
http://linkedlifedata.com/resource/pubmed/chemical/Pentobarbital,
http://linkedlifedata.com/resource/pubmed/chemical/Picrotoxin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Drug,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, GABA-A,
http://linkedlifedata.com/resource/pubmed/chemical/dihydropicrotoxinin,
http://linkedlifedata.com/resource/pubmed/chemical/dihydropicrotoxinin receptor,
http://linkedlifedata.com/resource/pubmed/chemical/picrotoxinin
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0270-6474
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
1
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1036-42
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:6270285-Animals,
pubmed-meshheading:6270285-Brain,
pubmed-meshheading:6270285-Cell Membrane,
pubmed-meshheading:6270285-Diazepam,
pubmed-meshheading:6270285-Kinetics,
pubmed-meshheading:6270285-Male,
pubmed-meshheading:6270285-Molecular Weight,
pubmed-meshheading:6270285-Pentobarbital,
pubmed-meshheading:6270285-Picrotoxin,
pubmed-meshheading:6270285-Rats,
pubmed-meshheading:6270285-Rats, Inbred Strains,
pubmed-meshheading:6270285-Receptors, Drug,
pubmed-meshheading:6270285-Receptors, GABA-A
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pubmed:year |
1981
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pubmed:articleTitle |
Picrotoxinin and diazepam bind to two distinct proteins: further evidence that pentobarbital may act at the picrotoxinin site.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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