Description
Endothelin-3 is an endogenous peptide agonist at endothelin B (ET-B) receptors that exhibits anti-inflammatory, neuromodulatory, and pro-angiogenic activities. In animal models, endothelin-3 inhibits platelet-activating factor-induced edema. In other models, this peptide decreases tyrosine hydroxylase activity in an NO/cGMP/PKG-dependent manner, suppressing hypothalamic release of norepinephrine. In vitro, endothelin-3 activates ET-B receptors, increasing expression of VEGF, COX1/2, HIF-1α, and PGE2.
References
Sato A, Ebina K. Endothelin-3 at low concentrations attenuates inflammatory responses via the endothelin B2 receptor. Inflamm Res. 2013 Apr;62(4):417-24. PMID: 23370722.
Spinella F, Rosanò L, Di Castro V, et al. Endothelin-1 and endothelin-3 promote invasive behavior via hypoxia-inducible factor-1alpha in human melanoma cells. Cancer Res. 2007 Feb 15;67(4):1725-34. PMID: 17308114.
Morgazo C, Perfume G, Legaz G, et al. Involvement of nitric oxide pathways in short term modulation of tyrosine hydroxylase activity by endothelins 1 and 3 in the rat anterior hypothalamus. Biochem Biophys Res Commun. 2005 Sep 2;334(3):796-802. PMID: 16023617.