102120-99-0
102120-99-0 结构式
基本信息
消旋罗替戈汀
罗替高汀-D7盐酸
5,6,7,8-四氢-6-[丙基[2-(2-噻吩基)乙基]氨基]-1-萘酚盐酸盐
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)
常见问题列表
|
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. .