Linked Life Data

8587367

Source:http://linkedlifedata.com/resource/pubmed/id/8587367

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:dateCreated
1996-3-28
pubmed:abstractText
The overall effects of endothelin-1 (ET-1) on blood pressure are caused by a composite activation of constrictor ETA and ETB receptors and dilator ETB receptors. Therefore, it is difficult to accurately compare the ETA activity of selective ETA receptor antagonists (BQ 123 and BMS 182874) with mixed ETA/ETB antagonists (SB 209670 and bosentan) on the cumulative dose-response curve to ET-1. The development of a selective ETB antagonist (BQ 788), which inhibits both the dilator and constrictor ETB receptors, offered the opportunity to investigate the role of ETB receptors in the response to exogenous ET-1 in the pithed rat. BQ 788 (3 mg/kg) resulted in an eightfold leftward shift in the ET-1 dose-response curve, suggesting a significant involvement of ETB dilator receptors. In the absence or presence of BQ 788, each ET antagonist evoked a rightward shift from vehicle. With the exception of BMS 182874, BQ 788 increased the magnitude of the shifts. Furthermore, the profile of the shifts changed from nonparallel to parallel in the presence of BQ 788. The inclusion of BQ 788 also altered the rank order of the ET antagonists tested. The results presented describe an in vivo system that accurately characterizes the ETA activity of ET antagonists.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0160-2446
pubmed:author
pubmed:issnType
Print
pubmed:volume
26 Suppl 3
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
S216-8
pubmed:dateRevised
2003-11-14
pubmed:meshHeading
pubmed:year
1995
pubmed:articleTitle
Effect of endothelin antagonists with or without BQ 788 on ET-1 responses in pithed rats.
pubmed:affiliation
Department of Vascular Biology, Rhône-Poulenc Rorer, Dagenham Research Centre, Essex, England.
pubmed:publicationType
Journal Article