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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3-4
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pubmed:dateCreated |
1984-5-7
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pubmed:abstractText |
Ro 5-4864 (4'-chlorodiazepam) elicited convulsions in mice with a CD50 of 23.5 mg/kg (i.p.) and increased the firing rate of substantia nigra zona reticulata neurons in a dose dependent fashion (0.5-4 mg/kg i.v.). Diazepam and clonazepam, but not Ro 15-1788, were potent inhibitors of Ro 5-4864 induced convulsions. Ro 15-1788 was also ineffective in reversing Ro 5-4864 induced increases in cell firing of zone reticulata neurons. Muscimol potently inhibited the seizures and reversed increases in cell firing elicited by Ro 5-4864. Phenobarbital and pentobarbital inhibited Ro 5-4864 induced convulsions with moderate potencies, while phenytoin and carbamazepine were ineffective at doses of up to 100 mg/kg. These observations suggest that Ro 5-4864 does not elicit its pharmacologic actions through a direct action at a 'brain-type' benzodiazepine receptor. However, both the profile and potency of compounds effective in inhibiting the electrophysiological and pharmacological effects of Ro 5-4864 suggest that this compound may act by perturbation of a component of the GABA-benzodiazepine receptor chloride ionophore complex. These findings do not, however, rule out a direct involvement of the high affinity 'peripheral-type' benzodiazepine receptors found in brain.
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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/4'-chlorodiazepam,
http://linkedlifedata.com/resource/pubmed/chemical/Benzodiazepinones,
http://linkedlifedata.com/resource/pubmed/chemical/Convulsants,
http://linkedlifedata.com/resource/pubmed/chemical/Muscimol,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Cell Surface,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, GABA-A
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0014-2999
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pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
27
|
pubmed:volume |
97
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
257-63
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:6323193-Animals,
pubmed-meshheading:6323193-Benzodiazepinones,
pubmed-meshheading:6323193-Binding Sites,
pubmed-meshheading:6323193-Brain,
pubmed-meshheading:6323193-Convulsants,
pubmed-meshheading:6323193-Electrophysiology,
pubmed-meshheading:6323193-Male,
pubmed-meshheading:6323193-Muscimol,
pubmed-meshheading:6323193-Rats,
pubmed-meshheading:6323193-Rats, Inbred Strains,
pubmed-meshheading:6323193-Receptors, Cell Surface,
pubmed-meshheading:6323193-Receptors, GABA-A,
pubmed-meshheading:6323193-Seizures,
pubmed-meshheading:6323193-Substantia Nigra
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pubmed:year |
1984
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pubmed:articleTitle |
Electrophysiological and pharmacological actions of the convulsant benzodiazepine Ro 5-4864.
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pubmed:publicationType |
Journal Article
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