129300-27-2
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
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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 |
| 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 |