马来酸替加色罗
| 中文名称 | 马来酸替加色罗 |
|---|---|
| 中文同义词 | 马来酸替加色罗;2-[(5-甲氧基-1H-吲哚-3-基)亚甲基]-N-戊基卡巴肼马来酸盐;马来酸替加色罗杂质 |
| 英文名称 | Tegaserod maleate |
| 英文同义词 | SDZ-HTF-919;TEGASEROD MALEATE;ZELMAC;2-[(5-METHOXY-1H-INDOL-3-YL)METHYLENE]-N-PENTYLHYDRAZINECARBOXIMIDAMIDE, MALEATE;2-[(5-methoxy-1h-indole-3-yl)methylene]-n-pentylcarbazimidamide hydrogen maleate;TegaserodMalate;TegastrodMaleate;SDZ-HTF-919, Zelmac, 2-[(5-Methoxy-1H-indol-3-yl)methylene]-N-pentylhydrazinecarboximidamide, Maleate |
| CAS号 | 189188-57-6 |
| 分子式 | C20H27N5O5 |
| 分子量 | 417.46 |
| EINECS号 | 630-469-2 |
| 相关类别 | 医药原料;小分子抑制剂;原料药;医药 吲哚类选择性5-HT4受体部分激动剂;医药原料药-科研原料;Active Pharmaceutical Ingredients;Chiral Compound;Intermediates & Fine Chemicals;Pharmaceuticals;Tegaserod;医药原料药;原料 |
| Mol文件 | 189188-57-6.mol |
| 结构式 |  |
马来酸替加色罗 性质
| 熔点 | 180-183°C |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | 乙腈（微溶、加热）、DMSO（微溶）、甲醇（微溶） |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| CAS 数据库 | 189188-57-6(CAS DataBase Reference) |
| Target | Value |
|
5-HT4 receptor
() |
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.
Tegaserod increases the amplitude of excitatory postsynaptic currents mediated by nicotinic acetylcholine receptors which may contribute to the prokinetic effects by facilitating excitatory neurotransmission in mice.
Tegaserod (0.1 mg/kg) significantly accelerates the gastric emptying rate of glucose in db/db mice, reducing the fraction of the meal remaining in the stomach at 30 min by 80%.
Tegaserod (5, 10, 50, 100 μg/mL) promotes hindlimb motor function at 6 weeks after spinal cord injury compared to the control group receiving vehicle only.
| Animal Model: | Female C57BLKS/J db/db mice. |
| Dosage: | 0.1, 0.5, 1.0, 2.0 mg/kg. |
| Administration: | IP 15 min prior to gastric loading. |
| Result: |
Produced a dramatic decrease in the fraction of the meal remaining in the stomach for doses as low as 0.1 mg/kg (0.1 mg/kg).
Accelerated gastric emptying, with a reduction of nearly 80% in the fraction remaining at 30 min (P < 0.0001) (0.1 mg/kg). Induced a significant decrease in the gastric emptying rate as the amount of the meal remaining at 30 min was significantly greater (2.0 mg/kg). Resulted in inhibition of tegaserod-induced increased gastric emptying (0.1 mg/kg). |
| Animal Model: | Three- to four-month-old female C57BL/6J mice. |
| Dosage: | 5, 10, 50, 100 μg/mL. |
| Administration: | Alzet pumps into non-injured spinal cords. |
| Result: |
Showed a less intense astrogliosis within and in the vicinity of the compression lesion site when compared to vehicle-only-treated mice.
Showed a smaller lesion area when compared to vehicle-onlytreated mice. Showed a higher staining intensity of 5-HT-immunoreactive axons 1 mm rostral, but not caudal to the lesion center as determined in cross-sections and quantification by ImageJ analysis. |