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Bisacodyl

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Chemical Structure| 603-50-9 同义名 : -
CAS号 : 603-50-9
货号 : A297750
分子式 : C22H19NO4
纯度 : 98%
分子量 : 361.391
MDL号 : MFCD00038039
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
生物活性
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].
临床研究
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 <<
实验方案
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
参考文献

[1]Ikarashi N, Baba K, et al. The laxative effect of bisacodyl is attributable to decreased aquaporin-3 expression in the colon induced by increased PGE2 secretion from macrophages. Am J Physiol Gastrointest Liver Physiol. 2011 Nov;301(5):G887-95.

[2]Saunders DR, Sillery J, Rachmilewitz D, Rubin CE, Tytgat GN. Effect of bisacodyl on the structure and function of rodent and human intestine. Gastroenterology. 1977 May;72(5 Pt 1):849-56.

[3]Ikarashi N, Baba K, Ushiki T, Kon R, Mimura A, Toda T, Ishii M, Ochiai W, Sugiyama K. The laxative effect of bisacodyl is attributable to decreased aquaporin-3 expression in the colon induced by increased PGE2 secretion from macrophages. Am J Physiol Gastrointest Liver Physiol. 2011 Nov;301(5):G887-95

[4]Saunders DR, Sillery J, Rachmilewitz D, Rubin CE, Tytgat GN. Effect of bisacodyl on the structure and function of rodent and human intestine. Gastroenterology. 1977 May;72(5 Pt 1):849-56

[5]Karmeli F, Stalnikowicz R, Rachmilewitz D. Effect of colchicine and bisacodyl on rat intestinal transit and nitric oxide synthase activity. Scand J Gastroenterol. 1997 Aug;32(8):791-6

[6]Rachmilewitz D, Karmeli F, Okon E. Effects of bisacodyl on cAMP and prostaglandin E2 contents, (Na + K) ATPase, adenyl cyclase, and phosphodiesterase activities of rat intestine. Dig Dis Sci. 1980 Aug;25(8):602-8

[7]Borrelli F, Mereto E, Capasso F, Orsi P, Sini D, Izzo AA, Massa B, Boggio M, Mascolo N. Effect of bisacodyl and cascara on growth of aberrant crypt foci and malignant tumors in the rat colon. Life Sci. 2001 Sep 7;69(16):1871-7