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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
4
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pubmed:dateCreated |
2007-4-10
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pubmed:abstractText |
This study tested whether sarcoplasmic-endoplasmic reticulum Ca(2+)-ATPase regulates the ability of endothelin receptor antagonist to inhibit the endothelin-1 constriction. The endothelin A receptor antagonist BQ-123 (1 microM) completely relaxed constriction to 10 nM endothelin-1 in endothelium-denuded rat aorta. Challenge with cyclopiazonic acid (10 microM), a sarcoplasmic-endoplasmic reticulum Ca(2+)-ATPase inhibitor, during the plateau of endothelin-1 constriction enhanced the constriction by approximately 30%. BQ-123 relaxed the endothelin-1 plus cyclopiazonic acid constriction by only approximately 10%. In contrast, prazosin (1 microM), an alpha-adrenergic receptor antagonist, still completely relaxed the 0.3 muM phenylephrine constriction in the presence of cyclopiazonic acid. Verapamil relaxed the endothelin-1 plus cyclopiazonic acid constriction by approximately 30%, whereas Ni(2+) and 2-aminoethoxydiphenyl borate, nonselective cation channel and store-operated channel blockers, respectively, completely relaxed the constriction. These results suggest that lowered sarcoplasmic-endoplasmic reticulum Ca(2+)-ATPase activity selectively decreases the ability of endothelin receptor antagonist to inhibit the endothelin A receptor. The decreased antagonism may be related to the opening of store-operated channels and subsequent greater internalization of endothelin A receptor.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic alpha-Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic alpha-Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Antihypertensive Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium-Transporting ATPases,
http://linkedlifedata.com/resource/pubmed/chemical/Endothelin-1,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/Peptides, Cyclic,
http://linkedlifedata.com/resource/pubmed/chemical/Phenylephrine,
http://linkedlifedata.com/resource/pubmed/chemical/Prazosin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Endothelin A,
http://linkedlifedata.com/resource/pubmed/chemical/cyclo(Trp-Asp-Pro-Val-Leu),
http://linkedlifedata.com/resource/pubmed/chemical/cyclopiazonic acid
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0363-6135
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
292
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
H1961-6
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:17172280-Adrenergic alpha-Agonists,
pubmed-meshheading:17172280-Adrenergic alpha-Antagonists,
pubmed-meshheading:17172280-Animals,
pubmed-meshheading:17172280-Antihypertensive Agents,
pubmed-meshheading:17172280-Aorta, Thoracic,
pubmed-meshheading:17172280-Calcium,
pubmed-meshheading:17172280-Calcium-Transporting ATPases,
pubmed-meshheading:17172280-Drug Interactions,
pubmed-meshheading:17172280-Endoplasmic Reticulum,
pubmed-meshheading:17172280-Endothelin-1,
pubmed-meshheading:17172280-Enzyme Inhibitors,
pubmed-meshheading:17172280-Indoles,
pubmed-meshheading:17172280-Male,
pubmed-meshheading:17172280-Muscle, Smooth, Vascular,
pubmed-meshheading:17172280-Peptides, Cyclic,
pubmed-meshheading:17172280-Phenylephrine,
pubmed-meshheading:17172280-Prazosin,
pubmed-meshheading:17172280-Rats,
pubmed-meshheading:17172280-Rats, Sprague-Dawley,
pubmed-meshheading:17172280-Receptor, Endothelin A,
pubmed-meshheading:17172280-Sarcoplasmic Reticulum,
pubmed-meshheading:17172280-Vasoconstriction
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pubmed:year |
2007
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pubmed:articleTitle |
Sarcoplasmic-endoplasmic reticulum Ca2+-ATPase inhibition prevents endothelin A receptor antagonism in rat aorta.
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pubmed:affiliation |
Department of Pharmacology, Faculty of Pharmacy, Ege University, Izmir, Turkey. metiner.tosun@ege.edu.tr
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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