Overview
Alomone Labs IRL-1620 activates Endothelin B receptor-mediated Ca2+ mobilization in CHO-K1-mt Aequorin cells.Dose-response curve of normalized activation of Endothelin B receptor-mediated Ca2+ mobilization, evoked by IRL-1620 (#SPE-220). Ca2+ response was detected by measuring aequorin-derived fluorescence following application of IRL-1620 and Endothelin-1 at different concentrations. The EC50 measured for IRL-1620 is 1.53 nM.
- Takai, M. et al. (1992) Biochem. Biophys. Res. Commun. 184, 953.
- Mazzoni, M.R. et al. (1999) Br. J. of Phrmacol. 127, 1406.
IRL-1620 is a synthetic peptide that acts as a selective and potent ET-B (endothelin B) receptor agonist, a receptor belonging to the G-protein coupled receptors (GPCR) superfamily. IRL-1620 is a C-terminal linear peptide analog of endothelin (ET-1) with a structure that is based on the carboxy-terminal end of ET-1. IRL-1620 has the ability to produce vasodilation or vasoconstriction1.
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 ganglia2.
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.
