| Description | Fabesetron (FK1052) is an orally active compound that acts as a dual antagonist, targeting both the 5-HT3 and 5-HT4 receptors. It exhibits efficacy in studying emesis induced by cancer chemotherapy, showing potential for managing both acute and delayed symptoms. |
| In vivo | Fabesetron (FK1052) (0.1 mg/kg p.o.) inhibits completely the increases in the colonic transit[1]. FK1052 (100 μg/kg) completely prevents emesis induced by cisplatin (18 mg/kg, i.p.) in Suncus murinus[2]. Animal Model: Male Sprague-Dawley rats weighing 220 to 330 g and male ddy mice weighing 25 to 35 g were used[1]. 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)[2]. 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. |
| Synonyms | 法贝司琼, FK1052 free base |
| molecular weight | 293.37 |
| Molecular formula | C18H19N3O |
| CAS | 129300-27-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. M Kadowaki, et al. Effect of FK1052, a potent 5-hydroxytryptamine3 and 5-hydroxytryptamine4 receptor dual antagonist, on colonic function in vivo. J Pharmacol Exp Ther. 1993 Jul;266(1):74-80. 2. Hiroe Nakayama, et al. Antiemetic activity of FK1052, a 5-HT3- and 5-HT4-receptor antagonist, in Suncus murinus and ferrets. J Pharmacol Sci. 2005 Aug;98(4):396-403. |