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描述 | Bisacodyl is a stimulant laxative agent that works directly on the colon to produce a bowel movement. Bisacodyl increases the secretion of PGE2 (prostaglandin E(2)) by direct activation of colon macrophages. PGE2 acts as a paracrine factor and decreases the expression of AQP3 (aquaporin3) in the colon, which inhibits water transfer from the luminal to the vascular side and leads to a laxative effect[3]. Bisacodyl inhibited water absorption in rat jejunum, ileum, and colon. The degree of inhibition was linearly related to the logarithm of the bisacodyl concentration over the range of 0.05 to 2.0 mg per 100 ml. In human jejunal segments, bisacodyl, 1 mg per 100 ml, caused net water secretion[4]. Bisacodyl (10 mg/kg, intragastrically) induces a significant decrease in jejunal NOS activity in rats. Bisacodyl (10 mg/kg, intragastrically) increases the distance traveled by the marker in all time periods[5]. Bisacodyl (5.9 mg/kg) decreases significantly jejunal and colonic (Na + K) ATPase activity as compared to saline-treated rats. Bisacodyl (5.9 mg/kg) increases significantly jejunal and colonic PGE2 content and stimulates jejunal and colonic adenyl cyclase activity as compared to those in control rats without affecting cAMP content[6]. Bisacodyl (4.3 mg/kg) coupled with AOM increases the number of crypt per focus, but not the number of tumors in rats. Bisacodyl (43 mg/kg) significantly increases the number of crypt per focus and tumors in rats[7]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02213172 | Irritable Bowel Syndrome-Const... 展开 >>ipation 收起 << | Phase 2 | Completed | - | Canada, Ontario ... 展开 >> KGK Synergize Inc. London, Ontario, Canada, N6A 5R8 收起 << |
NCT00804167 | - | Completed | - | - | |
NCT01358708 | Diarrhea-predominant Irritable... 展开 >> Bowel Syndrome 收起 << | Phase 3 | Terminated(Administrative reas... 展开 >>ons) 收起 << | - | France ... 展开 >> Bordeaux, France Colombes, France Marseille, France Nice, France Rouen, France Germany Berlin, Germany Hamburg, Germany Mannheim, Germany 收起 << |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.77mL 0.55mL 0.28mL |
13.84mL 2.77mL 1.38mL |
27.67mL 5.53mL 2.77mL |
CAS号 | 603-50-9 |
分子式 | C22H19NO4 |
分子量 | 361.391 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解方案 |
DMSO: 50 mg/mL(138.35 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |