- 英文名称
- Rotigotine Hydrochloride
- 分子式
- C19H26ClNOS
- 分子量
- 351.93
- 中文别名
- (S)-5,6,7,8-四氢-6-[丙基[2-(2-噻吩)乙基]氨基]-1-萘酚盐酸盐; (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; 罗替戈汀盐酸盐; (6S)-5,6,7,8-四氢-6-[丙基[2-(2-噻吩基)乙基]氨基]-1-萘醇盐酸盐; (6S)-6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol 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; rotigotine HCl; (6S)-6-{propyl[2-(thiophen-2-yl)ethyl]amino}-5,6,7,8-tetrahydronaphthalen-1-ol hydrochloride (1:1); (6S)-5,6,7,8-Tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-1-naphthalenol Hydrochloride Salt; (6S)-6-{Propyl[2-(2-thienyl)ethyl]amino}-5,6,7,8-tetrahydronaphthalen-1-ol hydrochloride (1:1); (2S)-5-HYDROXY-N-PROPYL-N-[2-(THIOPHEN-2-YL)ETHYL]-1,2,3,4-TETRAHYDRONAPHTHALEN-2-AMINIUM CHLORIDE; Hydrogen chloride - (6S)-6-{propyl[2-(2-thienyl)ethyl]amino}-5,6,7,8-tetrahydro-1-naphthalenol (1:1:1); (S)-Rotigotine hydrochloride; (-)-Rotigotine hydrochloride; (-)-5,6,7,8-Tetrahydro-6-(propyl(2-(2-thienyl)ethyl)amino)-1-naphthol hydrochloride; (6S)-6-[propyl(2-thiophen-2-ylethyl)amino]-5,6,7,8-tetrahydronaphthalen-1-ol,hydrochloride; 1-Naphthalenol, 5,6,7,8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-, chloride, hydrogen salt, (6S)- (1:1)
- 用途
- - 生物活性
Rotigotine Hydrochloride (N-0923 Hydrochloride) 是 dopamine receptor 纯激动剂，是 5-HT1A receptor 的部分激动剂，以及 α2B-adrenergic receptor 的拮抗剂，Ki 值分别为 0.71 nM (dopamine D3 receptor)，4-15 nM (D2，D5，D4 receptors)，83 nM (dopamine D1 receptor)。
- 靶点
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)
- 体外研究
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.
- 体内研究
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.
- It is a non-ergot dopamine agonist drug and is indicated for the treatment of Parkinson鈥檚 disease.
