Fabesetron (FK1052) 是具有口服活性的5-HT3和5-HT4受体的拮抗剂。Fabesetron (FK1052) 可用于癌症化疗引起的急性和迟发性呕吐的研究。
| 生物活性 | Fabesetron (FK1052) is an orally active5-HT3receptorantagonist with5-HT4receptorantagonistic activity. Fabesetron (FK1052) can be used in the study for both acute and delayed emesis induced bycancerchemotherapy[1][2]. |
| IC50& Target[1] | 5-HT3Receptor | 5-HT4Receptor |
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体内研究
(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.) inSuncus 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 murinusof 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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