- 英文名称
- rac-Rotigotine Hydrochloride
- 分子式
- C19H26ClNOS
- 分子量
- 351.93
- 中文别名
- 5,6,7,8-四氢-6-[丙基[2-(2-噻吩基)乙基]氨基]-1-萘酚盐酸盐; 消旋罗替戈汀; 罗替高汀消旋体; 罗替戈汀外消旋盐酸盐; 6-(丙基(2-(噻吩-2-基)乙基)氨基)-5,6,7,8-四氢萘-1-醇盐酸盐; 5,6,7,8-四氢-6-[丙基[2-(3-噻吩基)乙基]氨基]-1-羟基萘盐酸盐; Rotigotine Impurity 2(Rotigotine Racemate HCl); N 0437 hydrochloride; 5,6,7,8-Tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-1-naphthalenol Hydrochloride; 1-Naphthalenol, 5,6,7,8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-, (Hydrochloride) (1:1); (Rac) Rotigotine hydrochloride; (Rac)-Rotigotine (hydrochloride); 6-[propyl(2-thiophen-2-ylethyl)amino]-5,6,7,8-tetrahydronaphthalen-1-ol hydrochloride; rac-Rotigotine (Hydrochloride); Rotigotine Racemate HCl; Rotigotine hydrochloride, (+/-)-; (RS)-6-{Propyl[2-(thiophen-2-yl)ethyl]amino}-5,6,7,8-tetrahydronaphthalen-1-ol hydrochloride; 6-(Propyl(2-(thiophen-2-yl)ethyl)amino)-5,6,7,8-tetrahydronaphthalen-1-ol hydrochloride
- 用途
- - 生物活性:(Rac)-Rotigotine hydrochloride是Rotigotine的外消旋体,Rotigotine是dopamine receptor激动剂,5-HT1A receptor部分激动剂,α2B-adrenergic receptor拮抗剂,Ki值分别为0.71 nM(dopamine D3 receptor)、4-15 nM(D2、D5、D4 receptors)、83 nM(dopamine D1 receptor)、30 nM(5-HT1A receptor)、27 nM(5-HT2B receptor);体外研究显示其对D3受体选择性是D2、D4、D5的10倍(pKi=9.2 vs 8.5-8.0),对D1受体选择性是100倍(pKi=7.2),在功能研究中对所有多巴胺受体表现为完全激动剂,D1受体刺激效力与D2、D3受体相似(pEC50分别为9.0、9.4-8.6、9.7);10 μM时可使原代中脑细胞培养中THir神经元数量减少40%,0.01 μM时可轻微保护多巴胺能神经元免受MPP+毒性,显著保护免受鱼藤酮诱导的细胞死亡,并显著抑制鱼藤酮诱导的ROS产生。