102120-99-0
102120-99-0 結(jié)構(gòu)式
基本信息
消旋羅替戈汀
羅替高汀-D7鹽酸
5,6,7,8-四氫-6-[丙基[2-(2-噻吩基)乙基]氨基]-1-萘酚鹽酸鹽
N 0437 hydrochloride
rac-Rotigotine Hydrochloride
Rotigotine Impurity 2（Rotigotine Racemate HCl）
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-Naphthalenol, 5,6,7,8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]aMino]-, (Hydrochloride) (1:1)
常見問題列表
|
D 3 Receptor 0.71 nM (Ki) |
D 2 Receptor 13.5 nM (Ki) |
D 4 Receptor 3.9-15 nM (Ki) |
D 5 Receptor 5.4 nM (Ki) |
D 1 Receptor 83 nM (Ki) |
5-HT 1A Receptor 30 nM (Ki) |
5-HT 2B Receptor 27 nM (Ki) |
Rotigotine 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. .