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Item No. 24412

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Endothelin-2 is a peptide vasoconstrictor and ligand for the endothelin (ET) receptors ETA and ETB (Kbs= 32.8 and 1.33 nM, respectively).1 It induces β-arrestin recruitment in CHO-K1 cells expressing human ETA and ETB (pD2s =8.75 and 8.55, respectively). Ex vivo, endothelin-2 induces vformal asoconstriction in isolated rat mesenteric arterial beds (ED50 = 90.8 pmol).2 Endothelin-2 also induces contraction of isolated rat uteri, an effect which is reversed by the ETA antagonist BQ-123 but not the ETB antagonist BQ-788 (Item No. 17403).3 Infusion of endothelin-2 restores vasoconstriction of vessels at the follicular apex of the ovarian follicle and ovulation in Amhr2cre/+Smo2 mice.4
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1. Comparison of human ETA and ETB receptor signalling via G-
2. Endothelium-
3. Endopeptidase 24.11 inhibition does not modify uterotonic effects of endothelins in rat uterus. Peptides 19(9), 1585-1593 (1998).
4. In vivo imaging reveals an essential role of vasoconstriction in rupture of the ovarian follicle at ovulation. Proc. Natl. Acad. Sci. USA 113(8), 2294-2299 (2016).