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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6
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pubmed:dateCreated |
1985-10-3
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pubmed:abstractText |
We have shown that diazepam (ED50 2.4 microM), flunitrazepam (ED50 10.2 microM) and Ro5-4864 (ED50 5 microM) are able to enhance both total and specific [3H]phenytoin binding. Picrotoxin (IC50 1.43 microM) and chloride, either NaCl or KCl (IC50 42.4 microM) inhibit both the increase in total and specific binding of [3H]phenytoin, Ro15-1788 does not. The optimum time for this enhancement was 3-4 hours. While the ED50's for the benzodiazepines are high their order of potency suggests that an involvement of both the "peripheral type" benzodiazepine receptor and the GABA-chloride ionophore complex is likely. Clonazepam (IC50 23 microM), oxazepam (IC50 12 microM) chlordiazepoxide (IC50 35 microM) and Ro8682-10, a convulsant benzodiazepine (IC50 16 microM) all inhibit both total and specific [3H]phenytoin binding. These effects were not blocked by chloride ions, picrotoxin or Ro 15-1788, and reached equilibrium within 45 minutes. This order of potency also parallels that for the "peripheral' benzodiazepine receptor in rat brain. These data suggest the presence of a micromolar benzodiazepine receptor site which may play a role in the control of CNS excitability. Nitrazepam, medazepam, bromazepam and the tetralobenzodiazepines U38335, U42794, U43434, and U37834 had no effect on total or specific [3H]phenytoin binding nor on the actions of the other benzodiazepines described in concentrations up to 50 microM.
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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/Anti-Anxiety Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Benzodiazepines,
http://linkedlifedata.com/resource/pubmed/chemical/Benzodiazepinones,
http://linkedlifedata.com/resource/pubmed/chemical/Flumazenil,
http://linkedlifedata.com/resource/pubmed/chemical/Phenytoin,
http://linkedlifedata.com/resource/pubmed/chemical/Picrotoxin,
http://linkedlifedata.com/resource/pubmed/chemical/Potassium Chloride,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, GABA-A,
http://linkedlifedata.com/resource/pubmed/chemical/Sodium Chloride
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0364-3190
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
10
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
755-65
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:2863767-Animals,
pubmed-meshheading:2863767-Anti-Anxiety Agents,
pubmed-meshheading:2863767-Benzodiazepines,
pubmed-meshheading:2863767-Benzodiazepinones,
pubmed-meshheading:2863767-Flumazenil,
pubmed-meshheading:2863767-Male,
pubmed-meshheading:2863767-Phenytoin,
pubmed-meshheading:2863767-Picrotoxin,
pubmed-meshheading:2863767-Potassium Chloride,
pubmed-meshheading:2863767-Rats,
pubmed-meshheading:2863767-Receptors, GABA-A,
pubmed-meshheading:2863767-Sodium Chloride,
pubmed-meshheading:2863767-Stimulation, Chemical,
pubmed-meshheading:2863767-Time Factors
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pubmed:year |
1985
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pubmed:articleTitle |
Modulation of specific [3H]phenytoin binding by benzodiazepines.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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