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(±)-Fabesetron hydrochloride  

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包装规格：100mg in glass bottle
产品描述：基本信息 产品编号： F10330 产品名称： (±)-Fabesetron hydrochloride CAS: 129299-81-6   储存条件 粉末 -20℃ 四年     分子式： C18H20ClN3O 溶于液体     分子量 329.82     化学名：  10-methyl-7-[(5-methyl-1H-imidazol-4-yl)methyl]-8,9-dihydro-7H-pyrido[1,2-a]indol-6-one;hydrochloride Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   生物活性 产品描述 Fabesetron hydrochloride 的消旋体。一种有效的 5-HT3 和 5-HT4 受体双重拮抗剂。 靶点 5-HT3 Receptor 5-HT4 Receptor 体内研究 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, (±)-Fabesetron, at 0.1 mg/kg p.o., inhibits completely the increases in the colonic transit. Furthermore, (±)-Fabesetron, 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 (±)-Fabesetron, Ondansetron and Granisetron, with ED50 values of 0.09, 2.3 and 0.88 mg/kg p.o., respectively. (±)-Fabesetron (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 (±)-Fabesetron also significantly inhibits the number of the emetic episodes induced by MTX, of which the action is more effective than the treatment with (±)-Fabesetron at 1 mg/kg.   推荐实验方法(仅供参考) Animal Administration Mice and Rats Male Sprague-Dawley rats weighing 220 to 330 g and male ddy mice weighing 25 to 35 g are used. (±)-Fabesetron, Ondansetron, Granisetron, Methysergide, Ketanserin and Atropine are dissolved in distilled water. 5-HT, 2-methyl-5-HT, 1- phenylbiguanide and 5-MeOT are dissolved in physiological saline. Diazepam is suspended with 0.5% methylcellulose solution. The drugs are administered to rats at a volume of 2mL/ kg and to mice at a volume of 5mL/kg. Dogs Beagle dogs of either sex weighting 8.0 to18.5 kg are used in the study. Dogs are injected i.v. with MTX (2.5 mg/kg/mL) at 7:30 AM. The animal behavior is recorded using a video camera with an automatic night photographing system for up to 72 h and analyzed at the end of the experiment. (±)-Fabesetron (1 and 3.2 mg/kg), Ondansetron (1 mg/kg), Tropisetron (1 mg/kg), CP122,721 (0.1 mg/kg), or vehicle (0.5mL/kg) is administered i.v. at 24, 36, 48, and 60 h after MTX treatment. Episodes of emesis occurring within a few minutes are defined as a single emetic episode. A 12 h artificial light cycle (lights on between 7:30 AM and 7:30 PM) is used throughout the study. Dogs are given a standard laboratory dog chow (300 g/day) and water ad libitum. The animals are retested with MTX at least 6 weeks later
保存条件：-20℃

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