Name | Fabesetron |
Synonyms | Fabesetron FK1052 free base Fabesetron [INN] Pyrido[1,2-a]indol-6(7H)-one, 8,9-dihydro-10-methyl-7-[(4-methyl-1H-imidazol-5-yl)methyl]-, (7R)- |
CAS | 129300-27-2 |
Molecular Formula | C18H19N3O |
Molar Mass | 293.36 |
biological activity | Fabesetron (FK1052) is an orally active antagonist of 5-HT3 and 5-HT4 receptors. Fabesetron (FK1052) can be used in the study of acute and late-onset Vomit caused by cancer chemotherapy. |
Animal Model: | Male Sprague-Dawley rats weighing 220 to 330 g and male ddy mice weighing 25 to 35 g were used. Suncus murinus of either sex (>10-week-old; 30-70 g body weight). |
Dosage: | 0.1 mg/kg. 1, 10, and 100 µg/kg. |
Administration: | P.O. Orally administered 30 min before the injection of cisplatin. |
Result: | Significantly caused delay and its degree of inhibition was 33.8 ± 4.8% by 0.1 mg/kg p.o.. Inhibited cisplatininduced emesis in a dose-dependent manner, and no emesis was observed in three animals given the compound at 100 µg/kg. |