化合物 T11293 T11293

Product Introduction
Bioactivity


英文名: (±)-Fabesetron hydrochloride

描述: FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist.

体内活性: FK1052 (1 mg/kg i.v. ×4) apparently reduces delayed emesis caused by Methotrexate (MTX) and increases, but not significantly, the time for onset of emesis.?Furthermore, increasing the dose to 3.2 mg/kg of FK1052 also significantly inhibits the number of the emetic episodes induced by MTX, of which the action is more effective than the treatment with FK1052 at 1 mg/kg.In conscious rats, both 5-HT and 5-methoxytryptamine significantly increase fecal pellet output and accelerate colonic transit.?In contrast, the effect of 2-methyl-5-HT is slight.?Although Ondansetron and Granisetron slightly reduce 5-HT (1 mg/kg s.c.) stimulated colonic transit, FK1052, at 0.1 mg/kg p.o., inhibits completely the increases in the colonic transit.?Furthermore, FK1052, Ondansetron and Granisetron significantly depress the increase in fecal pellet output caused by wrap-restraint stress, with ED50 values of 0.21, 3.0 and 1.1 mg/kg p.o., respectively.?Intraperitoneal administration of 5-HT and 5-methoxytryptamine, but not 2-methyl-5-HT, produces a dose-related increase in the incidence of diarrhea in fasted mice.?5-HT (0.32 mg/kg i.p.)-induced diarrhea is also inhibited by FK1052, Ondansetron and Granisetron, with ED50 values of 0.09, 2.3 and 0.88 mg/kg p.o., respectively.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: Fabesetron Hydrochloride | (±) Fabesetron hydrochloride | FK-1052 Hydrochloride | FK1052 Hydrochloride | (±)Fabesetron hydrochloride | FK 1052 Hydrochloride

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途