鹽酸羅替戈汀
| 中文名稱 | 鹽酸羅替戈汀 |
|---|---|
| 中文同義詞 | 鹽酸羅替戈汀;(S)-5,6,7,8-四氫-6-[丙基[2-(2-噻吩)乙基]氨基]-1-萘酚鹽酸鹽;鹽酸羅替戈汀中文同義詞:鹽酸羅替戈汀;[2H3]-RAC ROTIGOTINE HYDROCHLORIDE SALT;(S)-6-(丙基(2-(噻吩-2-基)乙基)氨基)-5,6,7,8-四氫萘-1-醇鹽酸鹽 |
| 英文名稱 | (6S)-6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol hydrochloride |
| 英文同義詞 | (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號(hào) | 125572-93-2 |
| 分子式 | C19H26ClNOS |
| 分子量 | 351.93 |
| EINECS號(hào) | 603-080-0 |
| 相關(guān)類(lèi)別 | 原料藥;醫(yī)藥中間體;醫(yī)藥對(duì)照品;醫(yī)藥原料藥-科研原料;中間體;醫(yī)藥原料;APIs;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds |
| Mol文件 | 125572-93-2.mol |
| 結(jié)構(gòu)式 |  |
鹽酸羅替戈汀 性質(zhì)
| 熔點(diǎn) | 114-117°C |
|---|---|
| 密度 | 1.2g/cm3 at 20℃ |
| 蒸氣壓 | 0-0Pa at 20-25℃ |
| 儲(chǔ)存條件 | room temp |
| 溶解度 | 可溶于丙酮（輕微、加熱、超聲處理）、DMSO（輕微）、甲醇（輕微） |
| 形態(tài) | 固體 |
| 顏色 | 白色至類(lèi)白色 |
| 穩(wěn)定性 | 吸濕性 |
| LogP | 3.1 at 20℃ and pH7 |
| 表面張力 | 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 |
|---|---|
| 海關(guān)編碼 | 2934990002 |
| 更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
|---|---|---|---|---|---|
| 2024/11/08 | HY-A0007 | 鹽酸羅替戈汀 Rotigotine Hydrochloride | 5 mg | 354元 | |
| 2024/11/08 | HY-A0007 | 鹽酸羅替戈汀 Rotigotine Hydrochloride | 125572-93-2 | 10mM * 1mLin DMSO | 389元 |