Overview
- Webb, M.L. et al. (1995) J. Pharmacol. Exp. Ther. 272, 1124.
- Holm, P. et al. (1998) Cardiovasc. Res. 37, 765.
Alomone Labs BMS 182874 hydrochloride inhibits ET-A receptor-mediated Ca2+ mobilization in CHO cells.Dose-response curve of BMS 182874 hydrochloride (#B-500) inhibition of ET-A receptor-mediated, endothelin-1-evoked Ca2+ mobilization. IC50 was determined at 331.2 nM. Cells were loaded with Calcium 6 dye, incubated with BMS 182874 hydrochloride, and stimulated with 15 nM endothelin-1 (EC80). Changes in intracellular Ca2+ levels were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
BMS 182874 hydrochloride is a synthetic compound that acts as a selective, potent, and competitive antagonist of endothelin A (ET-A) receptors. BMS 182874 exhibits a 1000-fold selectivity for ET-A over ET-B receptors. The compound is a useful tool for understanding the role of endothelin in normal and disease conditions. BMS 182874 inhibits the binding of radioligand binding of ET-1 to ET-A receptors in rat vascular smooth muscle cell membranes with Ki of 61 nM and in Chinese ovary hamster cells with Ki of 48 nM1.
Endothelin receptors include two subtypes: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. ET-A receptors are predominantly detected in peripheral tissues, especially in vascular smooth muscle tissues where they mediate vasoconstriction. They are also expressed in several different regions of the brain. The ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while the ET-B receptor has high affinity for all endothelin isopeptides2.
