186497-38-1

ZD1611 competitively inhibits ¹²⁵ I-labeled ET-1 binding at human cloned ETA and ETB receptors with pIC ₅₀ values of 8.6 and 5.6, respectively, showing 1000-fold selectivity for the ETA receptor.

ZD1611 (0.3 mg/kg, p.o.) has a duration of action of more than 7 h in rats. In the dog, ZD1611 is active for at least 6 h at dose of 0.6 mg/kg p.o. ZD1611 (0.15 mg/kg/day) in combination with candesartan decreases the brain damage and improves the neurological scores in rats. However, ZD1611 or candesartan alone does not significantly decrease the brain damage or improve neurological scores.