99755-59-6
基本信息
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
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
物理化学性质
常见问题列表
Target | Value |
Dopamine receptor |
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.
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.