S80231 |
Rotigotine Hydrochloride ( N-0923 Hydrochloride) |
源葉(MedMol) | 99% |
- 提示:詳情請下載說明書。
- 產(chǎn)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.
- 靶點: 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
- 體內(nèi)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
- 參考文獻:
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.
- 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)
- 保存條件: 2-8℃
- 配置溶液濃度參考:
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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