125572-93-2
125572-93-2 結(jié)構(gòu)式
基本信息
鹽酸羅替戈汀中文同義詞:鹽酸羅替戈汀
[2H3]-RAC ROTIGOTINE HYDROCHLORIDE SALT
(S)-5,6,7,8-四氫-6-[丙基[2-(2-噻吩)乙基]氨基]-1-萘酚鹽酸鹽
CS-1395
rotigotine HCl
Rotigotine hydrochloride
hydrochloride hcl powder
CEXBONHIOKGWNU-NUDVEOEASA-N
[2H3]-Rac Rotigotine Hydrochloride Salt
8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]aMino]-
(6S)-6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol hydrochloride
(S)-6-(propyl(2-(thiophen-2-yl)ethyl)aMino)-5,6,7,8-tetrahydronaphthalen-1-ol
物理化學(xué)性質(zhì)
應(yīng)用領(lǐng)域
常見問題列表
|
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) |
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.
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.