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FK1052 hydrochloride

    
98%

Pyrido[1,2-a]indol-6(7H)-one, 8,9-dihydro-10-methyl-7-[(5-methyl-1H-imidazol-4-yl)methyl]-, monohydrochloride

源叶(MedMol)
T20723 一键复制产品信息
129299-81-6
C18H20ClN3O
329.8239
;Pyrido[1,2-a]indol-6(7H)-one, 8,9-dihydro-10-methyl-7-[(5-methyl-1H-imidazol-4-yl)methyl]-, monohydrochloride
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
T20723-5mg
98%

¥56100.00

货期:2-4周 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
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.
参考文献: 1. Kadowaki M, 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. Yamakuni H, et al. Probable involvement of the 5-hydroxytryptamine(4) receptor in methotrexate-induced delayed emesis in dogs. J Pharmacol Exp Ther. 2000 Mar;292(3):1002-7.
溶解性: DMSO
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 3.032 ml 15.16 ml 30.319 ml
5 mM 0.606 ml 3.032 ml 6.064 ml
10 mM 0.303 ml 1.516 ml 3.032 ml
50 mM 0.061 ml 0.303 ml 0.606 ml
注意: 部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

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