No extraction of the peptide is necessary, and the lack of sequence homologies excludes cross-reactivity of the assay antibodies against other members of the endothelin
Alterations in endothelin
B receptor sites in cavernosal tissue of diabetic rabbits: potential relevance to the pathogenesis of erectile dysfunction.
Hjelmqvist, "Mixed endothelin
receptor antagonism with tezosentan improves intestinal microcirculation in endotoxemic shock," Journal of Surgical Research, vol.
Kaiser et al., "Radiocontrast agents induce endothelin
Release in vivo and in vitro," Journal of the American Society of Nephrology, vol.
Pittrow, "Role of endothelin
receptor antagonists in renal disease," European Journal of Clinical Investigation, vol.
The present study addresses the hypothesis that the endothelin
receptor antagonist, bosentan, can ameliorate fibrotic agent abnormalities in diabetic mice.
Endothelium derived NO, Prostcyclins, Bradykinin, Heparin sulfate, transforming growth factor, etc are the inhibitors of the smooth cell growth which tend to balance the effect of the smooth cell growth promoters which are Platelet derived growth factors, Basic fibroblast growth factor, Insulin like growth factor-1, Endothelin
and Angiotensin etc.
In two studies that were the basis of approval, the most common side effects associated with the drug were peripheral edema (a known class effect of endothelin
receptor antagonists), which was usually mild to moderate; nasal congestion; sinusitis; and flushing, according to an Food and Drug Administration statement announcing the approval.
levels have been shown to occur with obesity, atherosclerosis, myocardial infarction, and diabetes.
Of the three endothelin
peptides, endothelin-1, -2, and -3, endothelin-1 (EDN1) is the predominant isoform in the vascular system.
This implies a direct relationship between NO production and the vascular changes in normal pregnant women and preeclamptic patients, and various substances including CGRP and endothelin
modulators have been examined in L-NAME-treated pregnant rats (Richer, 1996; Yallampalli, 1996; Gangula, 1997; Wight, 1998; Wimalawansa, 1998; Makino, 1999; Olson, 1999; Zlatnik, 1999).
Texas Biotechnology also has two highly selective endothelin
A receptor antagonists in clinical development for pulmonary arterial hypertension and congestive heart failure.