Haemodynamic and renal effects of endothelin
receptor antagonism in patients with chronic kidney disease.
Acet, "Selective endothelin
a (ETA) receptor antagonist (BQ123) reduces both myocardial infarct size and oxidant injury," Toxicology, vol.
and big endothelin
in coronary heart disease and acute coronary syndromes.
Subdepressor dose of benidipine ameliorates diabetic cardiac remodeling accompanied by normalization of upregulated endothelin
system in rats.
Human pulmonary circulation is an important site for both clearance and production of endothelin
in the anesthetized dog.
A second selective ETa endothelin
receptor antagonist, ambrisentan, was evaluated in a doubleblind, dose-ranging study that included 64 adult patients with PAH.
A receptor antagonism improves pulmonary arterial hypertension that is primary or autoimmune and related to congenital heart disease.
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
According to the research, since the overproduction of melanine is induced by endothelin
and SCF even if the skin is no longer exposed to ultraviolet rays, skin flecks tend to be persistent.
Based on those results and results of the associated extension study, Myogen believes ambrisentan's profile may position it as the best-in-class endothelin
receptor antagonist with demonstrated:
TracleerTM, the first orally available dual endothelin
receptor antagonist, is already approved and available in major markets worldwide for the treatment of pulmonary arterial hypertension (PAH), a chronic life-threatening condition that severely compromises the function of the lungs and heart.
In the recent study, polyphenols inhibited production of endothelin
1--a substance that stimulates hardening of the arteries.