中文名 | 马来酸替加色罗 |
英文名 | Tegaserod |
别名 | 马来酸替加色罗 马来酸替加色罗杂质 2-[(5-甲氧基-1H-吲哚-3-基)亚甲基]-N-戊基卡巴肼 2-[(5-甲氧基-1H-吲哚-3-基)亚甲基]-N-戊基卡巴肼马来酸盐 |
英文别名 | ZELMAC Tegaserod Tegaserode SDZ-HTF-919 TegaserodMalate TegastrodMaleate TEGASEROD MALEATE 2-[(5-METHOXY-1H-INDOL-3-YL)METHYLENE]-N-PENTYLHYDRAZINECARBOXIMIDAMIDE, MALEATE 2-[(5-methoxy-1h-indole-3-yl)methylene]-n-pentylcarbazimidamide hydrogen maleate 2-[(Z)-(5-methoxy-3H-indol-3-ylidene)methyl]-N'-pentylhydrazinecarboximidamide (2Z)-but-2-enedioate SDZ-HTF-919, Zelmac, 2-[(5-Methoxy-1H-indol-3-yl)methylene]-N-pentylhydrazinecarboximidamide, Maleate |
CAS | 189188-57-6 |
EINECS | 630-469-2 |
化学式 | C20H27N5O5 |
分子量 | 417.46 |
InChI | InChI=1/C16H23N5O.C4H4O4/c1-3-4-5-8-18-16(17)21-20-11-12-10-19-15-7-6-13(22-2)9-14(12)15;5-3(6)1-2-4(7)8/h6-7,9-11,19H,3-5,8H2,1-2H3,(H3,17,18,21);1-2H,(H,5,6)(H,7,8)/b20-11+;2-1- |
熔点 | 180-183°C |
沸点 | 661.4°C at 760 mmHg |
闪点 | 353.8°C |
蒸汽压 | 2.15E-18mmHg at 25°C |
溶解度 | 乙腈 (微溶加热) 、DMSO (微溶加热) 、甲醇 (微溶加热) |
存储条件 | 2-8°C |
外观 | 粉末 |
颜色 | white to beige |
物化性质 | 类白色结晶粉末。 |
体外研究 | Tegaserod was metabolized in human liver microsomes to O-desmethyl tegaserod at a low rate. Tegaserod had significant binding affinity for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors (pK i =7.5, 8.4 and 7.0, respectively). Tegaserod (0.1-3 μM) inhibits 5-HT-mediated contraction of the rat isolated stomach fundus potently (pA 2 =8.3), consistent with 5-HT2B receptor antagonist activity. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.395 ml | 11.977 ml | 23.954 ml |
5 mM | 0.479 ml | 2.395 ml | 4.791 ml |
10 mM | 0.24 ml | 1.198 ml | 2.395 ml |
5 mM | 0.048 ml | 0.24 ml | 0.479 ml |
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