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编 号:F233617
分子式:C22H24N4O5S
分子量:456.51
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生物活性:
ZD-1611 is a potent, orally active, selective ETA receptor antagonist, used for the research of ischemic stroke.

体内研究:
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.

体外研究:
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.
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