| PD156707: a potent antagonist of endothelin-1 in human diseased coronary arteries and vein grafts. | |
| | |
MedLine Citation:
|
PMID: 9595448 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
We have determined the ability of the endothelin A (ETA)-selective antagonist PD156707 to block constrictor ET-1 responses in blood vessels from the diseased human heart. ET-1 potently contracted nonatherosclerotic coronary arteries from patients with cardiomyopathy (pD2 = 7.96 +/- 0.15; n = 6), atherosclerotic coronary arteries from patients with ischemic heart disease (pD2 = 8.26 +/- 0.20; n = 4), and saphenous vein grafts that had developed "atherosclerotic" disease after coronary artery bypass (pD2 = 8.41 +/- 0.09; n = 6). PD156707 (100 nM) antagonized the vasoconstrictor response to ET-1 in each of the three preparations, with estimated pA2 values of 7.91 +/- 0.20, 8.05 +/- 0.14, and 8.07 +/- 0.02, respectively. These data suggest that the upregulation of ETB receptors that has been reported in human atherosclerotic coronary arteries does not contribute significantly to the ET-1-mediated constrictor response in these vessels in vitro. |
| | |
Authors:
|
J J Maguire; A P Davenport |
Related Documents
:
|
2456378 - Prevention of giant coronary artery aneurysms in kawasaki disease by intravenous gamma ... 3383468 - Effect of aging on doppler echocardiographic filling parameters in normal subjects and ... 2877578 - Perspectives on treating hypertension. 9869478 - Quantitative gated blood pool spect for the assessment of coronary artery disease at rest. 3101928 - Vasodilator actions of trk-100, a new prostaglandin i2 analogue. 8527918 - Management of traumatic aneurysms caused by high-velocity missile head wounds. |
Publication Detail:
|
Type: In Vitro; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
|
Title: Journal of cardiovascular pharmacology Volume: 31 Suppl 1 ISSN: 0160-2446 ISO Abbreviation: J. Cardiovasc. Pharmacol. Publication Date: 1998 |
Date Detail:
|
Created Date: 1998-07-17 Completed Date: 1998-07-17 Revised Date: 2006-11-15 |
Medline Journal Info:
|
Nlm Unique ID: 7902492 Medline TA: J Cardiovasc Pharmacol Country: UNITED STATES |
Other Details:
|
Languages: eng Pagination: S239-40 Citation Subset: IM |
Affiliation:
|
Clinical Pharmacology Unit, University of Cambridge, Addenbrooke's Hospital, England. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Adult Arteries / drug effects, transplantation Arteriosclerosis / physiopathology Coronary Artery Bypass Coronary Disease / physiopathology* Coronary Vessels / drug effects*, transplantation Dioxoles / pharmacology* Endothelin-1 / antagonists & inhibitors*, pharmacology Female Humans Male Middle Aged Receptor, Endothelin A Receptors, Endothelin / antagonists & inhibitors Saphenous Vein / drug effects, transplantation |
| Chemical | |
Reg. No./Substance:
|
0/Dioxoles; 0/Endothelin-1; 0/PD 156707; 0/Receptor, Endothelin A; 0/Receptors, Endothelin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Chronic effects of a novel, orally active endothelin receptor antagonist, T-0201, in dogs with conge...
Next Document: LU 302 872 and its racemate (LU 224 332) show balanced endothelin-A/B receptor affinity, high oral a...