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编 号：F616763
分子式：C18H19N3O
分子量：293.36
分子式：C18H19N3O
分子量：293.36
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CAS No: 129300-27-2
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生物活性：
Fabesetron (FK1052) is an orally active 5-HT3 receptor antagonist with 5-HT4 receptor antagonistic activity. Fabesetron (FK1052) can be used in the study for both acute and delayed emesis induced by cancer chemotherapy.
体内研究：
Fabesetron (FK1052) (0.1 mg/kg p.o.) inhibits completely the increases in the colonic transit.FK1052 (100 μg/kg) completely prevents emesis induced by cisplatin (18 mg/kg, i.p.) in Suncus murinus.Animal Model:Male Sprague-Dawley rats weighing 220 to 330 g and male ddy mice weighing 25 to 35 g were used.
Dosage:0.1 mg/kg.
Administration:P.O.
Result:Significantly caused delay and its degree of inhibition was 33.8 ± 4.8% by 0.1 mg/kg p.o..
Animal Model:Suncus murinus of either sex (>10-week-old; 30-70 g body weight).
Dosage:1, 10, and 100 μg/kg.
Administration:Orally administered 30 min before the injection of cisplatin.
Result:Inhibited cisplatininduced emesis in a dose-dependent manner, and no emesis was observed in three animals given the compound at 100 μg/kg.
Fabesetron (FK1052) is an orally active 5-HT3 receptor antagonist with 5-HT4 receptor antagonistic activity. Fabesetron (FK1052) can be used in the study for both acute and delayed emesis induced by cancer chemotherapy.
体内研究：
Fabesetron (FK1052) (0.1 mg/kg p.o.) inhibits completely the increases in the colonic transit.FK1052 (100 μg/kg) completely prevents emesis induced by cisplatin (18 mg/kg, i.p.) in Suncus murinus.Animal Model:Male Sprague-Dawley rats weighing 220 to 330 g and male ddy mice weighing 25 to 35 g were used.
Dosage:0.1 mg/kg.
Administration:P.O.
Result:Significantly caused delay and its degree of inhibition was 33.8 ± 4.8% by 0.1 mg/kg p.o..
Animal Model:Suncus murinus of either sex (>10-week-old; 30-70 g body weight).
Dosage:1, 10, and 100 μg/kg.
Administration:Orally administered 30 min before the injection of cisplatin.
Result:Inhibited cisplatininduced emesis in a dose-dependent manner, and no emesis was observed in three animals given the compound at 100 μg/kg.
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