比沙可啶
| 有效期 | 2年 |
| 描述 | 是一种刺激性缓泻化合物，主要作用于大肠。还可刺激局部轴突反射和节段反射，产生广泛的结肠蠕动。 |
| EC | EINECS 210-044-4 |
| MDL | MFCD00038039 |
| InChIKey | KHOITXIGCFIULA-UHFFFAOYSA-N |
| InChI | InChI=1S/C22H19NO4/c1-15(24)26-19-10-6-17(7-11-19)22(21-5-3-4-14-23-21)18-8-12-20(13-9-18)27-16(2)25/h3-14,22H,1-2H3 |
| PubChem CID | 2391 |
| 别名 | 4,4′-(2-吡啶亚甲基)双酚二乙酸酯 |
| 英文名称 | Bisacodyl |
| CAS | 603-50-9 |
| 分子式 | C22H19NO4 |
| 分子量 | 361.39 |
| 储存条件 | 2-8℃ |
| 纯度 | ≥98% |
| 外观（性状） | White to off-white crystalline Powder |
| 单位 | 瓶 |
| 生物活性 | Bisacodyl is a stimulant laxative agent that works directly on the colon to produce a bowel movement. Bisacodyl increases the secretion of PGE2 by direct activation of colon macrophages. PGE2 acts as a paracrine factor and decreases the expression of AQP3 in the colon, which inhibits water transfer from the luminal to the vascular side and leads to a laxative effect[1]. |
| In Vivo | Bisacodyl (20 mg/kg) results in a decrease in AQP3 protein expression and increased mRNA expression level of TNF-α in the colon of rats [1]. Bisacodyl inhibits water absorption in rat jejunum, ileum, and colon, the degree of inhibition is linearly related to the logarithm of the bisacodyl concentration over the range of 0.05 mg to 2.0 mg per 100 mL [2]. 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 [3]. 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 [4]. 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 [5]. |
| SMILES | CC(OC1=CC=C(C(C2=CC=C(OC(C)=O)C=C2)C3=NC=CC=C3)C=C1)=O |
| 靶点 | Others |
| 数据来源文献 | [1]. Ikarashi, N., 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. 301(5): p. G887-95.
[2]. Saunders, D.R., et al., Effect of bisacodyl on the structure and function of rodent and human intestine. Gastroenterology, 1977. 72(5 Pt 1): p. 849-56. [3]. Karmeli, F., R. Stalnikowicz, and D. Rachmilewitz, Effect of colchicine and bisacodyl on rat intestinal transit and nitric oxide synthase activity. Scand J Gastroenterol, 1997. 32(8): p. 791-6. [4]. Rachmilewitz, D., F. Karmeli, and E. Okon, Effects of bisacodyl on cAMP and prostaglandin E2 contents, (Na + K) ATPase, adenyl cyclase, and phosphodiesterase activities of rat intestine. Dig Dis Sci, 1980. 25(8): p. 602-8. [5]. Borrelli, F., et al., Effect of bisacodyl and cascara on growth of aberrant crypt foci and malignant tumors in the rat colon. Life Sci, 2001. 69(16): p. 1871-7. |
| 规格 | 500mg 1g |