Endothelin converting enzyme (ECE) activity in human vascular smooth muscle

British Journal of Pharmacology
J J MaguireA P Davenport

Abstract

1. We have characterized the human smooth muscle endothelin converting enzyme (ECE) present in the media of the endothelium-denuded human umbilical vein preparation. 2. Endothelin-1 (ET-1) and ET-2 were potent constrictors of umbilical vein with EC50 values of 9.2 nM and 29.6 nM, respectively. ET-1 was at least 30 times more potent than ET-3 suggesting the presence of constrictor ETA receptors. Little or no response was obtained to the ETB-selective agonist sarafotoxin 6c. These data suggest that endothelin-mediated vasoconstriction is via ETA receptors in this preparation. 3. Autoradiographical visualization of endothelin receptors with subtype selective ligands confirmed the predominance of the ETA receptor in the media of umbilical vein. High density of binding was obtained with the ETA selective [125I]-PD151242, with much lower levels detected with the ETB selective [125I]-BQ3020. 4. Big ET-1 (EC50 = 42.7 nM) and big ET-2(1-38) (EC50 = 99.0 nM) were less potent than ET-1 and ET-2, respectively. Big ET-2(1-38) was more potent than its isoform big ET-2(1-37) with concentration-response curves to big ET-2(1-37) incomplete at 300 nM. No response was obtained to big ET-3 at concentrations up to 700 nM. The C-terminal fragments, ...Continue Reading

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Citations

Oct 2, 2003·Life Sciences·Manoj C RodrigoKathleen M Eyster
Mar 17, 1999·British Journal of Pharmacology·F D Russell, A P Davenport
Aug 7, 2002·British Journal of Pharmacology·Katherine E Wiley, Anthony P Davenport
Jan 5, 2002·Expert Opinion on Investigational Drugs·R G TiltonR A Dixon
Oct 2, 2007·Vascular Pharmacology·Stephanie W WattsGregory D Fink
May 2, 2003·The Journal of Pharmacy and Pharmacology·Irén KrassóiJulius Gy Papp
Apr 25, 2006·British Journal of Pharmacology·Carlos R TirapelliPedro D'Orleans-Juste
Aug 19, 2014·British Journal of Pharmacology·J J Maguire, A P Davenport
Jan 13, 2016·Therapeutic Advances in Cardiovascular Disease·Langeza SalehA H Jan Danser
Feb 3, 2005·Circulation·Karina LaflammeLucie Germain
May 28, 2008·Fetal Diagnosis and Therapy·Eva MildenbergerHans T Versmold

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