Overview
- Bax, W.A. et al. (1994) Br. J. Pharmacol. 113, 1471.
- Maggi, C.A. et al. (1990) Gen. Pharmacol. 21, 247.
Alomone Labs Sarafotoxin S6b activates Endothelin-B receptor-mediated Ca2+ Luminescence in CHO-K1-mt Aequorin cells.Dose-response curve of normalized activation of Endothelin-B receptor-mediated Ca2+ mobilization evoked by Sarafotoxin S6b (#SPE-160). Ca2+ response was detected by measuring aequorin-derived fluorescence following application of Sarafotoxin S6b and Endothelin-1 at different concentrations. The EC50 measured for Sarafotoxin S6b is 43 pM.
Sarafotoxin S6b is a non-selective potent endothelin receptor agonist designed from the Lys-2-Arg-1 dipeptide of the endothelin pro-sequence. Sarafotoxin S6b has the ability to induce contractions of the human isolated coronary artery1,2.
Studies have shown that acute infusion of an ET-B receptor agonist into the rat renal medulla leads to natriuresis and diuresis via a mechanism that is NOS1-dependent3. Thus, endothelin receptors pharmacology play an important role in studying the function of the receptors.
Endothelin receptors include two subtypes: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. ETA receptors are predominantly expressed in peripheral tissues, especially in vascular smooth muscle tissues to mediate vasoconstriction. They are also detected in several different regions of the brain. ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while ET-B receptor has equally high affinity for all endothelin isopeptides4.
