Description
A dual ETA and ETB receptor antagonist and an active metabolite of macitentan; inhibits ET-1- induced increases in intracellular calcium in HPASMCs (IC50 = 14 nM), ET-1-induced contractions in isolated rat aortic rings (pA2 = 6.7 for ETA), and sarafotoxin S6c-induced contractions of isolated rat tracheal rings (pKB = 5.5 for ETB); reduces ET-1-induced increases in proliferation of isolated human skin fibroblasts at 10 and 100 µM; increases plasma ET-1 concentrations in normotensive rats and decreases MAP in DOCA-salt hypertensive rats at 10-300 mg/kg