盐酸罗替戈汀
中文名称 | 盐酸罗替戈汀 |
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中文同义词 | 盐酸罗替戈汀;(S)-5,6,7,8-四氢-6-[丙基[2-(2-噻吩)乙基]氨基]-1-萘酚盐酸盐;盐酸罗替戈汀中文同义词:盐酸罗替戈汀;[2H3]-RAC ROTIGOTINE HYDROCHLORIDE SALT;(S)-6-(丙基(2-(噻吩-2-基)乙基)氨基)-5,6,7,8-四氢萘-1-醇盐酸盐 |
英文名称 | (6S)-6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol hydrochloride |
英文同义词 | (6S)-6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol hydrochloride;Rotigotine hydrochloride;(6S)-5,6,7,8-Tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-1-naphthalenolhydrochloride;(S)-6-(propyl(2-(thiophen-2-yl)ethyl)amino)-5,6,7,8-tetrahydronaphthalen-1-ol hydrochloride;(6S)-;8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]aMino]-;rotigotine HCl;(S)-6-(propyl(2-(thiophen-2-yl)ethyl)aMino)-5,6,7,8-tetrahydronaphthalen-1-ol |
CAS号 | 125572-93-2 |
分子式 | C19H26ClNOS |
分子量 | 351.93 |
EINECS号 | 603-080-0 |
相关类别 | 原料药;医药中间体;医药对照品;医药原料药-科研原料;中间体;医药原料;APIs;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds |
Mol文件 | 125572-93-2.mol |
结构式 |
盐酸罗替戈汀 性质
熔点 | 114-117°C |
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密度 | 1.2g/cm3 at 20℃ |
蒸气压 | 0-0Pa at 20-25℃ |
储存条件 | room temp |
溶解度 | 可溶于丙酮(轻微、加热、超声处理)、DMSO(轻微)、甲醇(轻微) |
形态 | 固体 |
颜色 | 白色至类白色 |
稳定性 | 吸湿性 |
LogP | 3.1 at 20℃ and pH7 |
表面张力 | 72.3mN/m at 1g/L and 20℃ |
D 3 Receptor 0.71 nM (Ki) |
D 2 Receptor 4-15 nM (Ki) |
D 5 Receptor 4-15 nM (Ki) |
D 4 Receptor 4-15 nM (Ki) |
D 1 Receptor 83 nM (Ki) |
α1A 176 nM (Ki) |
α1B 273 nM (Ki) |
α2A 338 nM (Ki) |
α2B 27 nM (Ki) |
5-HT 1A Receptor 30 nM (Ki) |
5-HT 7 Receptor 86 nM (Ki) |
Rotigotine (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 (N-0923) 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 (N-0923) (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-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
WGK Germany | 2 |
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海关编码 | 2934990002 |
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-A0007 | 盐酸罗替戈汀 Rotigotine Hydrochloride | 5 mg | 354元 | |
2024/08/19 | HY-A0007 | 盐酸罗替戈汀 Rotigotine Hydrochloride | 125572-93-2 | 10mM * 1mLin DMSO | 389元 |