Source:http://linkedlifedata.com/resource/pubmed/id/17644086
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
1-3
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| pubmed:dateCreated |
2007-10-1
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| pubmed:abstractText |
We examined the effect of SN-6, a new benzyloxyphenyl Na(+)/Ca(2+) exchange (NCX) inhibitor on the Na(+)/Ca(2+) exchange current (I(NCX)) and other membrane currents in isolated guinea pig ventricular myocytes using the whole-cell voltage-clamp technique. SN-6 suppressed I(NCX) in a concentration-dependent manner. The IC(50) values of SN-6 were 2.3 microM and 1.9 microM for the outward and inward components of the bi-directional I(NCX), respectively. On the other hand, SN-6 suppressed the outward uni-directional I(NCX) more potently (IC(50) value of 0.6 microM) than the inward uni-directional I(NCX). SN-6 at 10 microM inhibited the uni-directional inward I(NCX) by only 22.4+/-3.1%. SN-6 and KB-R7943 suppressed I(NCX) more potently when intracellular Na(+) concentration was higher. Thus, both drugs inhibit NCX in an intracellular Na(+) concentration-dependent manner. Intracellular application of trypsin via a pipette solution did not change the blocking effect of SN-6 on I(NCX). Therefore, SN-6 is categorized as an intracellular-trypsin-insensitive NCX inhibitor. SN-6 at 10 microM inhibited I(Na), I(Ca), I(K) and I(K1) by about 13%, 34%, 33% and 13%, respectively. SN-6 at 10 microM shortened the action potential duration at 50% repolarization (APD(50)) by about 34%, and that at 90% repolarization (APD(90)) by about 25%. These results indicate that SN-6 inhibits NCX in a similar manner to that of KB-R7943. However, SN-6 at 10 microM affected other membrane currents less potently than KB-R7943.
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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/2-(2-(4-(4-nitrobenzyloxy)phenyl)eth...,
http://linkedlifedata.com/resource/pubmed/chemical/2-(4-(4-nitrobenzyloxy)benzyl)thiazo...,
http://linkedlifedata.com/resource/pubmed/chemical/Anti-Arrhythmia Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Benzyl Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium,
http://linkedlifedata.com/resource/pubmed/chemical/Diacetyl,
http://linkedlifedata.com/resource/pubmed/chemical/Sodium,
http://linkedlifedata.com/resource/pubmed/chemical/Sodium-Calcium Exchanger,
http://linkedlifedata.com/resource/pubmed/chemical/Thiazolidines,
http://linkedlifedata.com/resource/pubmed/chemical/Thiourea,
http://linkedlifedata.com/resource/pubmed/chemical/Trypsin,
http://linkedlifedata.com/resource/pubmed/chemical/diacetylmonoxime
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| pubmed:status |
MEDLINE
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| pubmed:month |
Nov
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| pubmed:issn |
0014-2999
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| pubmed:author | |
| pubmed:issnType |
Print
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| pubmed:day |
14
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| pubmed:volume |
573
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| pubmed:owner |
NLM
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| pubmed:authorsComplete |
Y
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| pubmed:pagination |
161-9
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| pubmed:meshHeading |
pubmed-meshheading:17644086-Analysis of Variance,
pubmed-meshheading:17644086-Animals,
pubmed-meshheading:17644086-Anti-Arrhythmia Agents,
pubmed-meshheading:17644086-Benzyl Compounds,
pubmed-meshheading:17644086-Calcium,
pubmed-meshheading:17644086-Diacetyl,
pubmed-meshheading:17644086-Dose-Response Relationship, Drug,
pubmed-meshheading:17644086-Guinea Pigs,
pubmed-meshheading:17644086-Heart Ventricles,
pubmed-meshheading:17644086-Ion Transport,
pubmed-meshheading:17644086-Membrane Potentials,
pubmed-meshheading:17644086-Molecular Structure,
pubmed-meshheading:17644086-Myocytes, Cardiac,
pubmed-meshheading:17644086-Patch-Clamp Techniques,
pubmed-meshheading:17644086-Sodium,
pubmed-meshheading:17644086-Sodium-Calcium Exchanger,
pubmed-meshheading:17644086-Thiazolidines,
pubmed-meshheading:17644086-Thiourea,
pubmed-meshheading:17644086-Trypsin
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| pubmed:year |
2007
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| pubmed:articleTitle |
Characterization of SN-6, a novel Na+/Ca2+ exchange inhibitor in guinea pig cardiac ventricular myocytes.
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| pubmed:affiliation |
Department of Internal Medicine III, Hamamatsu University School of Medicine, Hamamatsu 431-3192, Japan.
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| pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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