Overview
- Nakamichi, K. et al. (1992) Biochem. Biophys. Res. Commun. 182, 144.
![Alomone Labs Ala[1,3,11,15] Endothelin-1 activates Endothelin B receptor-mediated Ca2+ mobilization in CHO-K1-mt Aequorin cells.](https://assets.alomone.com/wp-content/uploads/2017/08/SPE-240_gr.gif)
Alomone Labs Ala[1,3,11,15] Endothelin-1 activates Endothelin B receptor-mediated Ca2+ mobilization in CHO-K1-mt Aequorin cells.Dose-response curve of normalized activation of the Endothelin B receptor-mediated Ca2+ mobilization, evoked by Ala[1,3,11,15] Endothelin-1 (#SPE-240). Ca2+ response was detected by measuring aequorin-derived fluorescence following application of Ala[1,3,11,15] Endothelin-1 and Endothelin-1 at different concentrations. The EC50 measured for Ala[1,3,11,15] Endothelin-1 is 0.38 pM.
[Ala1,3,11,15 ] Endothelin-1 is a potent ET-B (endothelin B) receptor agonist, a receptor that belongs to the G-protein coupled receptor (GPCR) superfamily. [Ala1,3,11,15] Endothelin-1 is a linear synthetic peptide analog of endothelin 1 (ET-1) that shows very high affinity for the receptor. The analog includes a substitution of Ala residue for Cys residues that removes the disulfide bridges that exist in endothelin-11-3.
Endothelin-1 (ET-1) and its receptor ET-B play an important role in regulating renal function and blood pressure. ET-B Receptor and ET-1 are both expressed in sensory nerves. They are mainly present in medium- and large-sized cell bodies of human trigeminal ganglia1.
Studies have shown that acute administration of an ET-B receptor agonist into the rat renal medulla leads to natriuresis and diuresis via a mechanism that is NOS1-dependent3.
