福沙吡坦
| 中文名称 | 福沙吡坦 |
|---|---|
| 中文同义词 | [3-[[(2R,3S)-2-[(1R)-1-[3,5-双(三氟甲基)苯基]乙氧基]-3-(4-氟苯基)-4-吗啉基]甲基]-2,5-二氢-5-氧代-1H-1,2,4-三唑-1-基]膦酸;福沙匹坦二甲基葡胺;福沙吡坦;福沙匹坦 /福沙匹坦二葡甲胺;福沙吡坦二葡甲胺;福沙匹坦异构体;福沙吡坦-D4;(3-(((2R,3S)-2-((R)-1-(3,5-双(三氟甲基)苯基)乙氧基)-3-(4-氟苯基)吗啉基)甲基)-5-氧代-2,5-二氢-1H-1,2,4-三唑-1-基)膦酸 |
| 英文名称 | Fosaprepitant |
| 英文同义词 | [3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-5-oxo-2H-1,2,4-triazol-1-yl]phosphonic acid;[3-[[(2R,3S)-2-[(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl]phosphonic acid;L 758298;P-[3-[[(2R,3S)-2-[(1R)-1-[3,5-Bis(trifluoroMethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-Morpholinyl]Methyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl]phosphonic Acid;MK-0517 (Fosaprepitant);D-Glucitol, 1-deoxy-1-(MethylaMino)-, (3-(((2R,3S)-2-((1R)-1-(3,5-bis(trifluoroMethyl)phenyl)ethoxy)-3-(4-fluorophenyl)-4- Morpholinyl)Methyl)-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl)phosphonate (2:1);Fosaprepitant;Fosaprepitant (See also F727305) |
| CAS号 | 172673-20-0 |
| 分子式 | C23H22F7N4O6P |
| 分子量 | 614.41 |
| EINECS号 | |
| 相关类别 | 原料药;化工原料;Aromatics;Chiral Reagents;Intermediates & Fine Chemicals;Pharmaceuticals |
| Mol文件 | 172673-20-0.mol |
| 结构式 |  |
福沙吡坦 性质
| 熔点 | >74°C (dec.) |
|---|---|
| 密度 | 1.65 |
| 储存条件 | Inert atmosphere,Store in freezer, under -20°C |
| 溶解度 | 可溶于二甲基亚砜、甲醇 |
| 酸度系数(pKa) | 2.45±0.20(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色 |
| InChIKey | BARDROPHSZEBKC-OITMNORJSA-N |
| SMILES | P(N1C(=O)N=C(CN2CCO[C@H](O[C@@H](C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)C)[C@@H]2C2=CC=C(F)C=C2)N1)(=O)(O)O |
Fosaprepitant (L-758298) 是 Aprepitant (HY-10052) 的前药。Fosaprepitant 是一种神经激肽-1 受体 (neurokinin-1 receptor) 拮抗剂，被开发用于预防化疗引起的恶心呕吐 (CINV)。
Neurokinin-1 receptor
Fosaprepitant (30 mg/kg; i.p.; daily; for 7 days) attenuates tolerance to morphine and increases the antinociceptive effect in in rats.
| Animal Model: | Sprague-Dawley rats |
| Dosage: | 30 mg/kg |
| Administration: | Intraperitoneal injection, daily, for 7 days |
| Result: | Increased the antinociceptive effect of morphine compared to control group. |