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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
1993-12-14
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pubmed:abstractText |
1. The effect of trimebutine on the voltage-dependent inward Ca2+ current was investigated by the whole-cell voltage-clamp technique in single smooth muscle cells from rabbit ileum. 2. Trimebutine (3-100 microM) reduced the Ca2+ current in a concentration-dependent manner. The inhibitory effect on the Ca2+ current was also dependent on the holding potential. The Ca2+ current after a low holding potential was inhibited to a greater extent than that after a high membrane potential: the IC50 values were 7 microM and 36 microM at holding potentials of -40 mV and -60 mV, respectively. The Ca2+ current elicited from a holding potential of -80 mV could not be reduced by as much as 50% of the control by trimebutine at concentrations as high as 100 microM. 3. Trimebutine (30 microM) shifted the voltage-dependent inactivation curve for the Ca2+ current by 18 mV in the negative direction. The affinity of the drug for Ca2+ channels was calculated to be 36 times higher in the inactivated state than in the closed-available state. 4. Blockade of the Ca2+ current by trimebutine, unlike verapamil, was not use-dependent. 5. The results suggest that trimebutine inhibits the voltage-dependent inward Ca2+ current through a preferential binding to Ca2+ channels in the inactivated state in the smooth muscle cell from rabbit ileum. The inhibitory effect of trimebutine on gastrointestinal motility is discussed in the light of the present findings.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/8220900-1665731,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8220900-1868878,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8220900-2161373,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8220900-2171963,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8220900-2432624,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8220900-2439984,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8220900-3601643,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8220900-3959348,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8220900-456734,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8220900-6088117,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8220900-6270629,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8220900-6306139,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8220900-6748369,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8220900-6988171,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8220900-7173739,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8220900-7214854,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8220900-8389715
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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 |
Sep
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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 |
110
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
399-403
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:8220900-Action Potentials,
pubmed-meshheading:8220900-Animals,
pubmed-meshheading:8220900-Calcium Channel Blockers,
pubmed-meshheading:8220900-Calcium Channels,
pubmed-meshheading:8220900-Electrophysiology,
pubmed-meshheading:8220900-Ileum,
pubmed-meshheading:8220900-Male,
pubmed-meshheading:8220900-Muscle, Smooth,
pubmed-meshheading:8220900-Rabbits,
pubmed-meshheading:8220900-Trimebutine,
pubmed-meshheading:8220900-Verapamil
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pubmed:year |
1993
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pubmed:articleTitle |
Effect of trimebutine on voltage-activated calcium current in rabbit ileal smooth muscle cells.
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pubmed:affiliation |
Department of Veterinary Science, Faculty of Agriculture, Gifu University, Japan.
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pubmed:publicationType |
Journal Article,
In Vitro
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