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In vivo, A-192621 inhibits ETB-mediated dilatory and pressor responses induced by Sarafotoxin 6c (ED50 = 30 mg/kg), and causes an elevation of arterial blood pressure and plasma ET-1 level2.
- Wu-Wong, J.R. et al. (2002) Clin. Sci. 103, 418S.
- Wessale, J.L. et al. (2002) Clin. Sci. 103, 112S.
Alomone Labs A-192621 inhibits ET-B receptor-mediated Ca2+ mobilization in CHO cells.Dose-response plot of A-192621 (#A-360) inhibition of ET-B receptor-mediated, endothelin-1-evoked Ca2+ mobilization. Complete inhibition was attained at 10 nM. Cells were loaded with Calcium 6 dye, incubated with A-192621, and stimulated with 30 nM endothelin-1 (EC80). Changes in intracellular Ca2+ levels were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
- Sakai, S. et al. (2016) Life Sci. 159, 116.
- Wessale, J.L. et al. (2002) Clin. Sci. 103, 112S.
- Wu-Wong, J.R. et al. (2002) Clin. Sci. 103, 418S.
- Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286.
- Xie, C. and Wang, D.H. (2009) Hypertension 54, 1298.
A-192621 is a synthetic compound that acts as a selective antagonist of the endothelin B (ET-B) receptor, a member of the G-protein coupled receptor (GPCR) superfamily.
In vivo efficacy studies showed that A-192621 inhibits ET-1-induced dilatory and pressor responses that are mediated by ET-B. The compound can cause an increase in arterial blood pressure and plasma ET-1 levels1,2. It inhibits ET-B receptors with an IC50 value of 4.5 nM3.
ET-B receptors play an important role in regulating renal function and blood pressure and are expressed in sensory nerves. They are mainly present in medium- and large-sized cell bodies of human trigeminal ganglia4,5.
A-192621 (#A-360) is a highly pure, synthetic, and biologically active compound.
