硝替卡朋
| 中文名称 | 硝替卡朋 |
|---|---|
| 中文同义词 | 硝替卡朋;3-(3,4-二羟基-5-硝基亚苄基)戊烷-2,4-二酮 |
| 英文名称 | Nitecapone |
| 英文同义词 | 3-[(3,4-Dihydroxy-5-nitrophenyl)methylene]-2,4-pentanedione;Nitecapone;OR 462;3-(3,4-Dihydroxy-5-nitrobenzylidene)pentane-2,4-dione;3-(3,4-dihydroxy-5-nitrobenzylidene)pentane-2,5-dione;GSH,Nitecapone,glutathione,OR-462,Inhibitor,ROS,Parkinson,COMT,OR 462,inhibit,OR462,allodynia;2,4-Pentanedione, 3-[(3,4-dihydroxy-5-nitrophenyl)methylene]- |
| CAS号 | 116313-94-1 |
| 分子式 | C12H11NO6 |
| 分子量 | 265.22 |
| EINECS号 | |
| 相关类别 | Intermediates & Fine Chemicals;Pharmaceuticals;Aromatics |
| Mol文件 | 116313-94-1.mol |
| 结构式 |  |
硝替卡朋 性质
| 熔点 | 171-173°C |
|---|---|
| 沸点 | 495.3±45.0 °C(Predicted) |
| 密度 | 1.451±0.06 g/cm3(Predicted) |
| 储存条件 | Sealed in dry,Store in freezer, under -20°C |
| 溶解度 | DMSO：可溶15mg/mL，澄清 |
| 形态 | 粉末 |
| 酸度系数(pKa) | 5.60±0.50(Predicted) |
| 颜色 | 白色至米色 |
硝替卡朋(OR-462) 是一种药物，可作为儿茶酚 O-甲基转移酶 (COMT) 的选择性抑制剂。它已获得抗帕金森药物专利。
硝替卡朋可用作儿茶酚-O-甲基转移酶(COMT)抑制剂。
Nitecapone (OR-462) 是一个短效的、具有口服活性的、儿茶酚-O-甲基转移酶 (COMT) 的抑制剂，具有胃肠道保护和抗氧化活性。Nitecapone (OR-462) 可清除活性氧和一氧化氮，防止脂质过氧化。Nitecapone (1-100 μM) reducesd GSH (reduced glutathione) depletion induced by ROO - by 11-38% and oxidation to oxidized glutathione (GSSG) by 32-45%.
Nitecapone (30 mg/kg, ip daily for 13 days) reduces development and symptoms of neuropathic pain after spinal nerve ligation in rats.
| Animal Model: | Eighty-six male Wistar rats, weighing 140-350 g. |
| Dosage: | 30 mg/kg (3.3 mL/kg). |
| Administration: | IP, once daily for 13 days. |
| Result: |
Selectively and specifically inhibits COMT in the peripheral tissues, and to some extent in the CNS for ca. 3 h.
Increased the thresholds for the mechanical stimuli and thus reduced mechanical allodynia. Reduced the number of positive reactions of the ipsilateral paws when compared with the baselines in the nitecapone-pretreated rats. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/11/08 | HY-106842 | 硝替卡朋 Nitecapone | 116313-94-1 | 5mg | 800元 |
| 2024/11/08 | HY-106842 | Nitecapone | 10 mM * 1 mLin DMSO | 880元 |