罗替戈汀
- CAS号:99755-59-6
- 英文名:ROTIGOTINE
- 中文名:罗替戈汀
- CBNumber:CB81001679
- 分子式:C19H25NOS
- 分子量:315.47
- MOL File:99755-59-6.mol
- 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
- 水溶解性 :Insoluble in water
- 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
- 酸度系数(pKa) :10.49±0.40(Predicted)
- 形态 :powder to crystal
- 颜色 :White to Almost white
- 危险品标志 :Xn
- 危险类别码 :22
- 海关编码 :2934990002
- 毒害物质数据 :99755-59-6(Hazardous Substances Data)
罗替戈汀性质、用途与生产工艺
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功效作用
罗替戈汀为非麦角类多巴胺受体刺激药,具有刺激脑部多巴胺受体的作用,用作柏金逊症的单一治疗或与左旋多巴共用。
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副作用
罗替戈汀可能会引起敏感反应。其他的副作用如头晕,头痛,突发性昏睡,失眠,肠胃不适,便秘,体位性低血压等。
- 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。
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靶点
Target Value 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.
- 更新日期:2024/11/08
- 产品编号:46654
- 产品名称:罗替高汀 Rotigotine
- CAS编号:99755-59-6
- 包装:100mg
- 价格:3392元
- 更新日期:2024/11/08
- 产品编号:46654
- 产品名称:罗替高汀 Rotigotine
- CAS编号:99755-59-6
- 包装:500mg
- 价格:10881元
- 公司名称:UBV Corporation FZC
- 联系电话:--
- 电子邮件:info@ubvcorporation.com
- 国家:阿拉伯联合酋长国
- 产品数:281
- 优势度:58