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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1 Pt 1
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pubmed:dateCreated |
1997-3-28
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pubmed:abstractText |
Experiments were undertaken to study the possibility that the calcium channel blocker D-600 (gallopamil), which penetrates into muscle cells (20), facilitates excitation-contraction coupling in skeletal muscle (7) by a direct effect on the sarcoplasmic reticulum (SR). The effects of D-600 were studied on single phasic muscle fibers, either intact or split open. D-600 potentiated twitches in intact fibers at concentrations lower than those reported in whole muscles. In split fibers, the force produced by caffeine-induced Ca2+ release from the SR was reversibly inhibited by 5 microM D-600, when added to the Ca2+ loading solution. This inhibitory effect was inversely related to temperature, and it was dose dependent. When D-600 was added after Ca2+ loading and before caffeine exposure, or during the caffeine exposure itself, it did not inhibit Ca2+ release, but rather increased the development of force. We conclude that, apart from the blocking effect that D-600 may have on the voltage sensor, the drug penetrates into the myoplasm and affects excitation-contraction coupling by inhibiting the SR Ca2+ pump. This may be the consequence of a conformational change in the transmembrane Ca2+ binding domain of the ATPase.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0002-9513
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
272
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
C310-7
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:9038837-Animals,
pubmed-meshheading:9038837-Caffeine,
pubmed-meshheading:9038837-Calcium,
pubmed-meshheading:9038837-Calcium Channel Blockers,
pubmed-meshheading:9038837-Dose-Response Relationship, Drug,
pubmed-meshheading:9038837-Gallopamil,
pubmed-meshheading:9038837-Muscle, Skeletal,
pubmed-meshheading:9038837-Muscle Contraction,
pubmed-meshheading:9038837-Muscle Fibers, Skeletal,
pubmed-meshheading:9038837-Osmolar Concentration,
pubmed-meshheading:9038837-Rana temporaria,
pubmed-meshheading:9038837-Sarcoplasmic Reticulum,
pubmed-meshheading:9038837-Temperature
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pubmed:year |
1997
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pubmed:articleTitle |
Effect of the organic Ca2+ channel blocker D-600 on sarcoplasmic reticulum Ca2+ uptake in skeletal muscle.
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pubmed:affiliation |
Department of Physiology, University of Maryland, Baltimore 21201, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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