法贝司琼
| 中文名称 | 法贝司琼 |
|---|---|
| 中文同义词 | 法贝司琼 |
| 英文名称 | Fabesetron |
| 英文同义词 | Fabesetron;Fabesetron [INN];Pyrido[1,2-a]indol-6(7H)-one, 8,9-dihydro-10-methyl-7-[(4-methyl-1H-imidazol-5-yl)methyl]-, (7R)-;FK1052 free base |
| CAS号 | 129300-27-2 |
| 分子式 | C18H19N3O |
| 分子量 | 293.36 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 129300-27-2.mol |
| 结构式 |  |
法贝司琼 性质
Fabesetron (FK1052) 是具有口服活性的 5-HT3 和 5-HT4 受体的拮抗剂。Fabesetron (FK1052) 可用于癌症化疗引起的急性和迟发性呕吐的研究。
|
5-HT 3 Receptor
|
5-HT 4 Receptor
|
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. |