Fabesetron

Modify Date: 2024-01-09 15:03:18

Fabesetron structure	Common Name	Fabesetron
	CAS Number	129300-27-2	Molecular Weight	293.36300
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₁₈H₁₉N₃O	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Fabesetron

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].

Name	(7R)-10-methyl-7-[(5-methyl-1H-imidazol-4-yl)methyl]-8,9-dihydro-7H-pyrido[1,2-a]indol-6-one
Synonym	More Synonyms

Description	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].
Related Catalog	Research Areas >> Cancer Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	5-HT3 Receptor 5-HT4 Receptor
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.
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.