罗替戈汀
| 中文名称 | 罗替戈汀 |
|---|---|
| 中文同义词 | 罗替戈汀碱;罗替戈汀 100MG;ROTIGOTINE(S构型);(S)-5,6,7,8-四氢-6-(丙基(2-(2-噻吩基)乙基)氨基)-1-萘酚;罗替哥汀杂质;罗替戈汀杂质;罗替高汀;(6S)-6-{丙基[2-(2-噻吩基)乙基]氨基}-5,6,7,8-四氢-1-萘酚 |
| 英文名称 | ROTIGOTINE |
| 英文同义词 | ()-(S)-5,6,7,8-Tetrahydro-6-(propyl(2-(2-thienyl)ethyl)amino)-1-napht hol;(6S)-5,6,7,8-Tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-1-naphthalenol;N 0923;SPM 962;(S)-2-[Propyl[2-(2-thienyl)ethyl]amino]tetralin-5-ol;[2S,(-)]-N-Propyl-N-[2-(2-thienyl)ethyl]-5-hydroxy-1,2,3,4-tetrahydro-2β-naphthalenamine;[S,(-)]-2-[Propyl[2-(2-thienyl)ethyl]amino]tetralin-5-ol;S(-)-N-0437 |
| CAS号 | 99755-59-6 |
| 分子式 | C19H25NOS |
| 分子量 | 315.47 |
| EINECS号 | |
| 相关类别 | 对照品-杂质对照品;中间体;医药原料;G蛋白偶联受体&G蛋白;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;Inhibitors;小分子抑制剂，天然产物;化学原料药;化工原料 |
| Mol文件 | 99755-59-6.mol |
| 结构式 |  |
罗替戈汀 性质
| 熔点 | 78 °C |
|---|---|
| 沸点 | 470.1±45.0 °C(Predicted) |
| 密度 | 1.15±0.1 g/cm3(Predicted) |
| 储存条件 | room temp |
| 溶解度 | DMF：30mg/mL； DMF:PBS(pH7.2)(1:2)：0.33mg/ml； DMSO：20mg/mL；乙醇：1mg/mL |
| 水溶解性 | Insoluble in water |
| 酸度系数(pKa) | 10.49±0.40(Predicted) |
| 形态 | 粉末晶体 |
| 颜色 | 白色到近乎白色 |
| 主要应用 | 药物 药物小分子 |
| InChI | InChI=1S/C19H25NOS/c1-2-11-20(12-10-17-6-4-13-22-17)16-8-9-18-15(14-16)5-3-7-19(18)21/h3-7,13,16,21H,2,8-12,14H2,1H3/t16-/m0/s1 |
| InChIKey | KFQYTPMOWPVWEJ-INIZCTEOSA-N |
| SMILES | C1(O)=C2C(C[C@@H](N(CCC)CCC3SC=CC=3)CC2)=CC=C1 |
罗替戈汀为非麦角类多巴胺受体刺激药，具有刺激脑部多巴胺受体的作用，用作柏金逊症的单一治疗或与左旋多巴共用。
罗替戈汀可能会引起敏感反应。其他的副作用如头晕，头痛，突发性昏睡，失眠，肠胃不适，便秘，体位性低血压等。
Rotigotine是一种dopamine receptor的激动剂，用于帕金森氏症和不宁腿综合征的治疗。| Target | Value |
| Dopamine receptor |
Rotigotine (N-0437; N-0923) has a 10-fold selectivity for D3 (pK
i
9.2) receptors compared with D2, D4 and D5 (pK
i
8.5-8.0) and a 100-fold selectivity compared with D1 receptors (pK
i
7.2). In functional studies, Rotigotine behaves as full agonist at all dopamine receptors but notably the potency for stimulation of D1 receptors is similar to that for D2 and D3 receptors (pEC
50
respectively: 9.0, 9.4-8.6, 9.7).
Rotigotine (10 µM) decreases the number of THir neurons by 40% in primary mesencephalic cell culture. Rotigotine (0.01 µM) slightly protects dopaminergic neurons against MPP
+
toxicity, significantly protects dopaminergic neurons against rotenone-induced cell death, and significantly inhibits ROS production by rotenone.
In primed rats, Rotigotine (N-0437; N-0923; 0.035, 0.1 and 0.35 mg/kg) induces contralateral turning behavior in a dose dependent manner. In drug naive rats, the turning behavior induced by Rotigotine, either alone or in combination with SCH 39166, is reduced compared to primed rats.
安全信息
| 危险品标志 | Xn |
|---|---|
| 危险类别码 | 22 |
| WGK Germany | WGK 3 |
| 海关编码 | 2934990002 |
| 存储类别 | 11 - 可燃固体 |
| 毒害物质数据 | 99755-59-6(Hazardous Substances Data) |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026/06/06 | R0220 | 罗替戈汀 Rotigotine | 99755-59-6 | 10mg | 320元 |
| 2026/06/06 | R0220 | 罗替戈汀 Rotigotine | 99755-59-6 | 50mg | 1130元 |