99755-59-6
99755-59-6 結(jié)構(gòu)式
基本信息
羅替戈汀堿
羅替戈汀雜質(zhì)
羅替哥汀雜質(zhì)
羅替戈汀 100MG
ROTIGOTINE(S構(gòu)型)
(S)-5,6,7,8-四氫-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
物理化學(xué)性質(zhì)
pharmaceutical small molecule
安全數(shù)據(jù)
常見問題列表
羅替戈汀為非麥角類多巴胺受體刺激藥，具有刺激腦部多巴胺受體的作用，用作柏金遜癥的單一治療或與左旋多巴共用。
羅替戈汀可能會(huì)引起敏感反應(yīng)。其他的副作用如頭暈，頭痛，突發(fā)性昏睡，失眠，腸胃不適，便秘，體位性低血壓等。
| 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.