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99755-59-6

中文名称 罗替戈汀
英文名称 ROTIGOTINE
CAS 99755-59-6
分子式 C19H25NOS
分子量 315.47
MOL 文件 99755-59-6.mol
更新日期 2024/05/28 11:53:14
99755-59-6 结构式 99755-59-6 结构式

基本信息

中文别名
罗替戈汀
罗替戈汀碱
罗替戈汀杂质
罗替哥汀杂质
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
英文别名
CS-110
Neupro
N 0923
SPM 962
Rotigotine
S(-)-N-0437
Rotigotine (Base)
ROTIGOTINE USP/EP/BP
(S)-2-[Propyl[2-(2-thienyl)ethyl]amino]tetralin-5-ol
[S,(-)]-2-[Propyl[2-(2-thienyl)ethyl]amino]tetralin-5-ol
所属类别
生物化工:Dopamine Receptor 激动剂

物理化学性质

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: 30 mg/ml; DMF:PBS(pH7.2) (1:2): 0.33 mg/ml; DMSO: 20 mg/ml; Ethanol: 1 mg/ml
水溶解性不溶于水
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

安全数据

危险性符号(GHS)
GHS07,GHS08
警示词警告
危险性描述H336-H362-H361
危险品标志Xn
危险类别码22
海关编码2934990002

常见问题列表

生物活性
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。
靶点
TargetValue
Dopamine receptor
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.

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