中文名 | 罗替戈汀 |
英文名 | Rotigotine |
别名 | 罗替高汀 罗替戈汀 罗替戈汀碱 罗替哥汀杂质 罗替戈汀杂质 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 (-)-(S)-5,6,7,8-四氢-6-(丙基(2-(2-噻吩基)乙基)氨基)-1-萘酚 |
英文别名 | Neupro N 0923 SPM 962 Rotigotine (S)-2-[Propyl[2-(2-thienyl)ethyl]amino]tetralin-5-ol [S,(-)]-2-[Propyl[2-(2-thienyl)ethyl]amino]tetralin-5-ol ()-(S)-5,6,7,8-Tetrahydro-6-(propyl(2-(2-thienyl)ethyl)amino)-1-napht hol (-)-(S)-5,6,7,8-Tetrahydro-6-(propyl(2-(2-thienyl)ethyl)amino)-1-naphthol (6S)-5,6,7,8-Tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-1-naphthalenol (6S)-6-{propyl[2-(thiophen-2-yl)ethyl]amino}-5,6,7,8-tetrahydronaphthalen-1-ol [2S,(-)]-N-Propyl-N-[2-(2-thienyl)ethyl]-5-hydroxy-1,2,3,4-tetrahydro-2β-naphthalenamine |
CAS | 99755-59-6 |
化学式 | C19H25NOS |
分子量 | 315.47 |
InChI | InChI=1/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 |
密度 | 1.15±0.1 g/cm3(Predicted) |
熔点 | 78 °C |
沸点 | 470.1±45.0 °C(Predicted) |
闪点 | 238.1°C |
水溶性 | Insoluble in water |
蒸汽压 | 1.84E-09mmHg at 25°C |
折射率 | 1.611 |
酸度系数 | 10.49±0.40(Predicted) |
存储条件 | room temp |
外观 | 粉末或结晶 |
颜色 | White to Almost white |
MDL号 | MFCD00906149 |
体外研究 | 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. |
体内研究 | 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. |
危险品标志 | Xn - 有害物品 |
风险术语 | 22 - 吞食有害。 |
海关编号 | 2934990002 |
上游原料 | 2-(噻吩-2-基)乙基对甲苯磺酸酯 5-甲氧基-2-萘满酮 Rotigotine Impurity 7 盐酸罗替戈汀 (S)-5-甲氧基-N-丙基-N-(2-(噻吩-2-基)乙基)-1,2,3,4-四氢萘-2-胺 101470-23-9 2-噻吩乙酸 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.17 ml | 15.849 ml | 31.699 ml |
5 mM | 0.634 ml | 3.17 ml | 6.34 ml |
10 mM | 0.317 ml | 1.585 ml | 3.17 ml |
5 mM | 0.063 ml | 0.317 ml | 0.634 ml |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!