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129300-27-2

129300-27-2 structure
129300-27-2 structure
  • Name: Fabesetron
  • Chemical Name: (7R)-10-methyl-7-[(5-methyl-1H-imidazol-4-yl)methyl]-8,9-dihydro-7H-pyrido[1,2-a]indol-6-one
  • CAS Number: 129300-27-2
  • Molecular Formula: C18H19N3O
  • Molecular Weight: 293.36300
  • Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
  • Create Date: 2017-12-18 14:48:42
  • Modify Date: 2024-01-09 15:03:18
  • 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
Synonyms (+)-(7r)-8,9-dihydro-10-methyl-7-[(5-methyl-1h-imidazol-4-yl)methyl]pyrido[1,2-a]indol-6(7h)-one
UNII-QU72HVX338
Fabesetron
Fabesetron [INN]
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
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.

Molecular Formula C18H19N3O
Molecular Weight 293.36300
Exact Mass 293.15300
PSA 50.68000
LogP 3.42650
Vapour Pressure 1.28E-12mmHg at 25°C