125572-93-2 盐酸罗替戈汀

WGK Germany:2 海关编码:2934990002 存储类别:11 - 可燃固体

• 生物活性 Rotigotine Hydrochloride (N-0923 Hydrochloride) 是 dopamine receptor 纯激动剂，是 5-HT1A receptor 的部分激动剂，以及 α2B-adrenergic receptor 的拮抗剂，Ki 值分别为 0.71 nM (dopamine D3 receptor)，4-15 nM (D2，D5，D4 receptors)，83 nM (dopamine D1 receptor)。
• 靶点 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)
• 体外研究 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.
• 体内研究 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.
• It is a non-ergot dopamine agonist drug and is indicated for the treatment of Parkinson鈥檚 disease.

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