ChemicalBook CAS DataBase List 129300-27-2

129300-27-2

Name	Fabesetron
CAS	129300-27-2
Molecular Formula	C18H19N3O
MDL Number	MFCD00891468
Molecular Weight	293.36
MOL File	129300-27-2.mol

Chemical Properties

form	Solid
color	Off-white to light yellow

Hazard Information

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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