129300-27-2
129300-27-2 結(jié)構(gòu)式
基本信息
中文別名
法貝司瓊 英文別名
FabesetronFabesetron [INN]
Pyrido[1,2-a]indol-6(7H)-one, 8,9-dihydro-10-methyl-7-[(4-methyl-1H-imidazol-5-yl)methyl]-, (7R)-
常見問題列表
生物活性
Fabesetron (FK1052) 是具有口服活性的 5-HT3 和 5-HT4 受體的拮抗劑。Fabesetron (FK1052) 可用于癌癥化療引起的急性和遲發(fā)性嘔吐的研究。靶點(diǎn)
|
5-HT 3 Receptor
|
5-HT 4 Receptor
|
體內(nèi)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. |