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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
1982-12-16
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pubmed:abstractText |
The evidence for direct muscle relaxant effects of benzodiazepines is controversial. We now show that a crude membrane preparation of rat diaphragm possesses binding sites for [3H]flunitrazepam (FNZ). Scatchard analysis gave a binding site density of 1689 +/- 143 fmol/mg protein (Kd = 25.6 +/- 2.6 nM). These sites are of the "peripheral" type since clonazepam fails to displace [3H]FNZ as effectively as R05-4864 (IC50 values: 7.5 x 10(-6) M and 8 x 10(-9) M, respectively). Diazepam is almost as effective as R05-4864 and potently displaces [3H]FNZ binding (IC50 = 3 x 10(-8) M). We propose that the previously described effects of diazepam on rat diaphragm are mediated through high-affinity binding sites.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0008-4212
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
60
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1003-5
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:6127152-Animals,
pubmed-meshheading:6127152-Anti-Anxiety Agents,
pubmed-meshheading:6127152-Benzodiazepines,
pubmed-meshheading:6127152-Binding Sites,
pubmed-meshheading:6127152-Diaphragm,
pubmed-meshheading:6127152-Flunitrazepam,
pubmed-meshheading:6127152-Male,
pubmed-meshheading:6127152-Neuromuscular Junction,
pubmed-meshheading:6127152-Rats,
pubmed-meshheading:6127152-Rats, Inbred Strains,
pubmed-meshheading:6127152-Receptors, Drug,
pubmed-meshheading:6127152-Receptors, GABA-A
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pubmed:year |
1982
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pubmed:articleTitle |
Flunitrazepam binding sites in rat diaphragm. Receptors for direct neuromuscular effects of benzodiazepines?
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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