ZD-1611

ZD-1611 is a potent, orally active, selective ETA receptor antagonist, used for the research of ischemic stroke. In Vitro: ZD1611 competitively inhibits ¹²⁵I-labeled ET-1 binding at human cloned ETA and ETB receptors with pIC₅₀ values of 8.6 and 5.6, respectively, showing 1000-fold selectivity for the ETA receptor^[1]. In Vivo: 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^[1]. 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^[2].