Measurement of bigET-1, which has slower clearance (14), has been proposed as an alternative approach for estimation of ET-1 release, but alterations in plasma bigET-1 may also not reflect changes in ET-1 synthesis because bigET-1 is cleaved at the tissue level not only into active ET-1, but also into the 31-amino acid endothelin
peptide ET-[1.sub.(1-31)] by the action of chymase (15).
Bosentan is the only endothelin
antagonist currently approved by the FDA.
. New England Journal of Medicine 333, 356-363.
Role of endothelin
receptors and relationship with nitric oxide synthase in impaired erectile response in diabetic rats.
Khalil, "The vascular endothelin
system in hypertension--recent patents and discoveries.," Recent Patents on Cardiovascular Drug Discovery, vol.
receptor antagonists in particular endothelin
ETA receptor blockers might also be useful in the prevention of CIN , particularly in diabetic patients, characterized by markedly enhanced endothelin
synthesis following radiocontrast administration [35, 36].
Salloukh, "Role of endothelin
in fibrosis and anti-fibrotic potential of bosentan," Annals of Medicine, vol.
The present study was designed to investigate the changes of VEGF (a potent angiogenic factor) and fibrotic genes (TGF-[beta], CTGF and Collagen-1), and the potential protective effect of bosentan (non-selective endothelin
receptor antagonist) in diabetic cardiac fibrosis.
Nitric oxide, Bradykinin, Prostacyclin, Serotonin, Histamin, Substance P and Endothelium- derived hyperpolarizing factor are the vasodilators while the substances like Angiotensin, Endothelin
(ETI), Thromboxane A2, Serotonin, Arachidonic acid, Prostaglandin H2 and Thrombin are the vasoconstrictor molecules released by the endothelium (16).
Under the agreement Pfizer will acquire the rights to Thelin (sitaxsentan sodium), an oral, once-daily endothelin
A receptor antagonist (ETRA) for the treatment of PAH, as well as Encysive's other pipeline candidates.
receptor antagonist for treating pulmonary arterial hypertension (PAH).
Pharmacopeia's most advanced internal program is a dual-acting angiotensin and endothelin
receptor antagonist for hypertension and diabetic kidney disease for which Phase 1 clinical trials are underway.