Source:http://linkedlifedata.com/resource/pubmed/id/12049621
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6
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pubmed:dateCreated |
2002-6-6
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pubmed:abstractText |
Endothelin-1 (ET-1) has been proposed to contribute to the regulation of vascular tone in humans. BQ-123, an ET(A) receptor antagonist, has also been reported to increase forearm blood flow (FBF) in vivo; however, the efficacy of BQ-123 as an antagonist of ET-1 has not been evaluated in the forearm. The present study investigated the effects of BQ-123 on changes in FBF in response to ET-1 and noradrenaline (NA; norepinephrine), taking into account the possible influence of vasodilator effects of BQ-123 on responses to vasoconstrictors. Six subjects (age 25-34 years) participated in a double-blind randomized study. FBF was measured by forearm occlusion plethysmography. Drugs were infused intra-arterially into the non-dominant arm (study arm) on four separate occasions; the non-infused arm was used as a control. The effects of BQ-123 (50 nmol/min for 60 min, or 300 nmol/min for 5 min followed by saline for 55 min) were compared with the effects of infusion of sodium nitroprusside (SNP; 12 nmol/min for 60 min) or saline on vasoconstriction induced by ET-1 (10 pmol/min for 7 min) and NA (120 pmol/min for 7 min). Infusion of BQ-123 at either dose did not significantly increase FBF, whereas SNP increased FBF by 134% (P=0.03). ET-1 significantly reduced FBF, and this effect was almost completely inhibited by both doses of BQ-123, but was unaffected by SNP. NA also reduced FBF, and this action was unaffected by BQ-123 or SNP. The data show that BQ-123 is a selective ET-1 antagonist, but do not confirm a major role for ET-1 in influencing resting forearm vascular tone in young normotensive subjects.
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pubmed:commentsCorrections | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antihypertensive Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Endothelin-1,
http://linkedlifedata.com/resource/pubmed/chemical/Nitroprusside,
http://linkedlifedata.com/resource/pubmed/chemical/Norepinephrine,
http://linkedlifedata.com/resource/pubmed/chemical/Peptides, Cyclic,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Endothelin,
http://linkedlifedata.com/resource/pubmed/chemical/Vasodilator Agents,
http://linkedlifedata.com/resource/pubmed/chemical/cyclo(Trp-Asp-Pro-Val-Leu)
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0143-5221
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
102
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
661-6
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:12049621-Adult,
pubmed-meshheading:12049621-Antihypertensive Agents,
pubmed-meshheading:12049621-Double-Blind Method,
pubmed-meshheading:12049621-Endothelin-1,
pubmed-meshheading:12049621-Forearm,
pubmed-meshheading:12049621-Humans,
pubmed-meshheading:12049621-Nitroprusside,
pubmed-meshheading:12049621-Norepinephrine,
pubmed-meshheading:12049621-Peptides, Cyclic,
pubmed-meshheading:12049621-Plethysmography,
pubmed-meshheading:12049621-Receptors, Endothelin,
pubmed-meshheading:12049621-Regional Blood Flow,
pubmed-meshheading:12049621-Vasoconstriction,
pubmed-meshheading:12049621-Vasodilator Agents
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pubmed:year |
2002
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pubmed:articleTitle |
Action of the endothelin receptor (ETA) antagonist BQ-123 on forearm blood flow in young normotensive subjects.
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pubmed:affiliation |
Clinical Pharmacology, NHLI, Imperial College School of Medicine, St Mary's Hospital, London W2 1NY, UK. r.wimalasundera@ic.ac.uk
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pubmed:publicationType |
Journal Article,
Clinical Trial,
Randomized Controlled Trial,
Research Support, Non-U.S. Gov't
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