| Identification | Back Directory | [Name]
Fabesetron | [CAS]
129300-27-2 | [Synonyms]
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)- | [Molecular Formula]
C18H19N3O | [MDL Number]
MFCD00891468 | [MOL File]
129300-27-2.mol | [Molecular Weight]
293.36 |
| Hazard Information | Back Directory | [Uses]
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[1][2]. | [Definition]
ChEBI: Fabesetron is an organic heterotricyclic compound that is 8,9-dihydropyrido[1,2-a]indol-6(7H)-one substituted by a (5-methyl-1H-imidazol-4-yl)methyl group at position 7R and a methyl group at position 10. It is a dual 5-HT3 and 5-HT4 receptors antagonist whose clinical development was terminated in phase II. It was being developed for the treatment of chemotherapy-induced emesis and irritable bowel syndrome. It has a role as an antiemetic and a serotonergic antagonist. It is a member of imidazoles and an organic heterotricyclic compound. | [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. |
| [IC 50]
5-HT3 Receptor; 5-HT4 Receptor | [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. PMID:8331576
[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. DOI:10.1254/jphs.fpj05001x |
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