Source:http://linkedlifedata.com/resource/pubmed/id/11259552
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
2001-3-22
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pubmed:abstractText |
The cardioprotective efficacy of zoniporide (CP-597,396), a novel, potent, and selective inhibitor of the sodium-hydrogen exchanger isoform 1 (NHE-1), was evaluated both in vitro and in vivo using rabbit models of myocardial ischemia-reperfusion injury. In these models, myocardial injury was elicited with 30 min of regional ischemia and 120 min of reperfusion. Zoniporide elicited a concentration-dependent reduction in infarct size (EC(50) of 0.25 nM) in the isolated heart (Langendorff) and reduced infarct size by 83% (50 nM). This compound was 2.5- to 20-fold more potent than either eniporide or cariporide (EC(50) of 0.69 and 5.11 nM, respectively), and reduced infarct size to a greater extent than eniporide (58% reduction in infarct size). In open-chest, anesthetized rabbits, zoniporide also elicited a dose-dependent reduction in infarct size (ED(50) of 0.45 mg/kg/h) and inhibited NHE-1-mediated platelet swelling (maximum inhibition 93%). Furthermore, zoniporide did not cause any in vivo hemodynamic (mean arterial pressure, heart rate, rate pressure product) changes. Zoniporide represents a novel class of potent NHE-1 inhibitors with potential utility for providing clinical cardioprotection.
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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/Guanidines,
http://linkedlifedata.com/resource/pubmed/chemical/Protective Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Sodium-Hydrogen Antiporter,
http://linkedlifedata.com/resource/pubmed/chemical/growth factor-activatable Na-H...
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0022-3565
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pubmed:author |
pubmed-author:ElleryS SSS,
pubmed-author:FlynnD MDM,
pubmed-author:Guzman-PerezAA,
pubmed-author:HillR JRJ,
pubmed-author:KnightD RDR,
pubmed-author:KongJ XJX,
pubmed-author:MacAndrewJ TJT,
pubmed-author:MageeW PWP,
pubmed-author:MaralaR BRB,
pubmed-author:SmithA HAH,
pubmed-author:TraceyW RWR,
pubmed-author:WesterR TRT
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pubmed:issnType |
Print
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pubmed:volume |
297
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
254-9
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:11259552-Animals,
pubmed-meshheading:11259552-Dose-Response Relationship, Drug,
pubmed-meshheading:11259552-Guanidines,
pubmed-meshheading:11259552-Hemodynamics,
pubmed-meshheading:11259552-Male,
pubmed-meshheading:11259552-Myocardial Infarction,
pubmed-meshheading:11259552-Myocardial Ischemia,
pubmed-meshheading:11259552-Protective Agents,
pubmed-meshheading:11259552-Pyrazoles,
pubmed-meshheading:11259552-Rabbits,
pubmed-meshheading:11259552-Sodium-Hydrogen Antiporter
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pubmed:year |
2001
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pubmed:articleTitle |
A novel sodium-hydrogen exchanger isoform-1 inhibitor, zoniporide, reduces ischemic myocardial injury in vitro and in vivo.
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pubmed:affiliation |
Department of Cardiovascular and Metabolic Diseases, Pfizer Global Research and Development, Pfizer Inc., 3125 Eastern Point Road, Groton, CT 06340, USA.
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pubmed:publicationType |
Journal Article
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