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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4924
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pubmed:dateCreated |
1989-10-16
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pubmed:abstractText |
GABAA (gamma-aminobutyric acid A)-benzodiazepine receptors expressed in mammalian cells and assembled from one of three different alpha subunit variants (alpha 1, alpha 2, or alpha 3) in combination with a beta 1 and a gamma 2 subunit display the pharmacological properties of either type I or type II receptor subtypes. These receptors contain high-affinity binding sites for benzodiazepines. However, CL 218 872, 2-oxoquazepam, and methyl beta-carboline-3-carboxylate (beta-CCM) show a temperature-modulated selectivity for alpha 1 subunit-containing receptors. There were no significant differences in the binding of clonazepam, diazepam, Ro 15-1788, or dimethoxy-4-ethyl-beta-carboline-3-carboxylate (DMCM) to all three recombinant receptors. Receptors containing the alpha 3 subunit show greater GABA potentiation of benzodiazepine binding than receptors containing the alpha 1 or alpha 2 subunit, indicating that there are subtypes within the type II class. Thus, diversity in benzodiazepine pharmacology is generated by heterogeneity of the alpha subunit of the GABAA receptor.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/CL 218872,
http://linkedlifedata.com/resource/pubmed/chemical/Diazepam,
http://linkedlifedata.com/resource/pubmed/chemical/Flumazenil,
http://linkedlifedata.com/resource/pubmed/chemical/Flunitrazepam,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridazines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, GABA-A,
http://linkedlifedata.com/resource/pubmed/chemical/Recombinant Proteins
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0036-8075
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
22
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pubmed:volume |
245
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1389-92
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pubmed:dateRevised |
2007-3-19
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pubmed:meshHeading |
pubmed-meshheading:2551039-Cell Line,
pubmed-meshheading:2551039-Diazepam,
pubmed-meshheading:2551039-Flumazenil,
pubmed-meshheading:2551039-Flunitrazepam,
pubmed-meshheading:2551039-Humans,
pubmed-meshheading:2551039-Molecular Weight,
pubmed-meshheading:2551039-Pyridazines,
pubmed-meshheading:2551039-Receptors, GABA-A,
pubmed-meshheading:2551039-Recombinant Proteins,
pubmed-meshheading:2551039-Transfection
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pubmed:year |
1989
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pubmed:articleTitle |
Type I and type II GABAA-benzodiazepine receptors produced in transfected cells.
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pubmed:affiliation |
Department of Molecular Neuroendocrinology, Zentrum für Molekulare Biologie, Universität Heidelberg, Federal Republic of Germany.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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