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产品描述： Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor. |
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靶点：
D3 Receptor:0.71 nM (Ki);D2 Receptor:4-15 nM (Ki);D5 Receptor:4-15 nM (Ki);D4 Receptor:4-15 nM (Ki);D1 Receptor:83 nM (Ki);α1A:176 nM (Ki);α1B:273 nM (Ki);α2A:338 nM (Ki);α2B:27 nM (Ki);5-HT1A Receptor:30 nM (Ki);5-HT7 Receptor:86 nM (Ki);DopamineReceptor;5-HTReceptor;AdrenergicReceptor |
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 |
参考文献：
1. Wood M, et al. Rotigotine is a potent agonist at dopamine D1 receptors as well as at dopamine D2 and D3 receptors. Br J Pharmacol. 2015 Feb;172(4):1124-35. 2. Scheller D, et al. The in vitro receptor profile of rotigotine: a new agent for the treatment of Parkinson's disease. Naunyn Schmiedebergs Arch Pharmacol. 2009 Jan;379(1):73-86. 3. Fenu S, et al. In vivo dopamine agonist properties of rotigotine: Role of D1 and D2 receptors. Eur J Pharmacol. 2016 Oct 5;788:183-91. 4. Radad K, et al. Neuroprotective effect of rotigotine against complex I inhibitors, MPP? and rotenone, in primary mesencephalic cell culture. Folia Neuropathol. 2014;52(2):179-86. |
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溶解性：
DMSO : ≥ 50 mg/mL (142.07 mM) H2O : 4.76 mg/mL (13.53 mM; ultrasonic and warming and heat to 60°C) |
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保存条件：
2-8℃ |
配置溶液浓度参考：
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1mg |
5mg |
10mg |
| 1 mM |
2.841 ml |
14.207 ml |
28.414 ml |
| 5 mM |
0.568 ml |
2.841 ml |
5.683 ml |
| 10 mM |
0.284 ml |
1.421 ml |
2.841 ml |
| 50 mM |
0.057 ml |
0.284 ml |
0.568 ml |
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| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京