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rdf:type |
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lifeskim:mentions |
umls-concept:C0005064,
umls-concept:C0012010,
umls-concept:C0020885,
umls-concept:C0021467,
umls-concept:C0021469,
umls-concept:C0026845,
umls-concept:C0205127,
umls-concept:C0999699,
umls-concept:C1140999,
umls-concept:C1167622,
umls-concept:C1533691
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pubmed:issue |
2
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pubmed:dateCreated |
1983-5-27
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pubmed:abstractText |
1--The longitudinal muscle-myenteric plexus strip preparation of the guinea-pig ileum was used to study the binding of [3H]-diazepam and the effect of benzodiazepines on its contraction. 2--Scatchard analysis of binding indicated a single class of binding sites with KD = 43 nM and Bmax = 229 fmol/mg prótein. Binding was of peripheral type based on the much greater binding affinity of Ro5-4864 as compared to clonazepam. Binding of [3H]-diazepam reached equilibrium at 10 min and dissociated rapidly (T1/2 = 1.3 min). The KD derived from the rate constants agreed with that from the Scatchard analysis. 3--Benzodiazepines produced a dose-dependent decrease in the electrically induced contractions of the longitudinal muscle strip, but their potencies in this effect did not correlate with their binding affinities. 4--Diazepam antagonized the contractions of the longitudinal muscle strip induced by K+, Ca2+, histamine and carbachol. The inhibition of Ca2+-induced contractions was reversed by increasing the concentration of Ca2+ in the medium.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/6131717-14190470,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6131717-14907713,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6131717-20632,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6131717-430037,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6131717-4965383,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6131717-6101294,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6131717-6157072,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6131717-6257998,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6131717-6273185,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6131717-6279112,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6131717-682122,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6131717-876354,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6131717-918669
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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 |
Feb
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pubmed:issn |
0007-1188
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
78
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
321-7
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:6131717-Animals,
pubmed-meshheading:6131717-Anti-Anxiety Agents,
pubmed-meshheading:6131717-Binding, Competitive,
pubmed-meshheading:6131717-Carbachol,
pubmed-meshheading:6131717-Diazepam,
pubmed-meshheading:6131717-Electric Stimulation,
pubmed-meshheading:6131717-Guinea Pigs,
pubmed-meshheading:6131717-Histamine,
pubmed-meshheading:6131717-Ileum,
pubmed-meshheading:6131717-Kinetics,
pubmed-meshheading:6131717-Muscle, Smooth,
pubmed-meshheading:6131717-Muscle Contraction,
pubmed-meshheading:6131717-Potassium Chloride
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pubmed:year |
1983
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pubmed:articleTitle |
The binding of [3H]-diazepam to guinea-pig ileal longitudinal muscle and the in vitro inhibition of contraction by benzodiazepines.
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pubmed:publicationType |
Journal Article,
In Vitro
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