Solriamfetol hydrochloride
目录号 : GC39443
Solriamfetol hydrochloride是一种多巴胺和去甲肾上腺素再摄取抑制剂。Solriamfetol hydrochloride能阻断突触前神经元对多巴胺和去甲肾上腺素的再摄取。Solriamfetol hydrochloride可用于治疗与发作性睡病或阻塞性睡眠呼吸暂停相关的日间嗜睡。
Cas No.:178429-65-7
Sample solution is provided at 25 µL, 10mM.
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Solriamfetol hydrochloride is a dopamine and norepinephrine reuptake inhibitor. Solriamfetol hydrochloride blocks the reuptake of dopamine and norepinephrine by presynaptic neurons. Solriamfetol hydrochloride is used to treat daytime sleepiness associated with narcolepsy or obstructive sleep apnea [1-4].
In CHO cells, Solriamfetol hydrochloride (2500 and 4100nM, 3h) inhibits DA and NE transporters, thereby enhancing neurotransmission [5]. In HEK293 cells, Solriamfetol hydrochloride (1nM-100μM, 1.5h) has dual reuptake inhibition activity at dopamine (DA; IC50 = 2.9μM) and norepinephrine (NE; IC50 = 4.4μM) transporters, and this activity is associated in vivo with increased extracellular concentration of DA and NE as measured by microdialysis [6].
In C57BL/6J mice, Solriamfetol hydrochloride (30 and 100mg/kg, po, 9h) significantly increased locomotor activity in a dose-dependent manner, indicating its wake-promoting and psychostimulant-like effects [5]. In rats, Solriamfetol hydrochloride (30mg/kg, sc, 10h) increased DA and NE levels in the striatum and prefrontal cortex [6]. In TetO-DTA mice model, Solriamfetol hydrochloride (50, 100, and 150mg/kg, po, 9h) effectively promotes wakefulness in WT and narcolepsy DTA mice in a dose-dependent manner [7]. In a murine model of OSA, Solriamfetol hydrochloride (200mg/kg, ip, 9d) enhances wakefulness and improves cognition and anxiety [8].
References:
[1]. Markham A. Solriamfetol: first global approval. Drugs. 2019 May 1; 79: 785-790.
[2]. Yang J, Gao J. Solriamfetol for the treatment of excessive daytime sleepiness associated with narcolepsy. Expert Review of Clinical Pharmacology. 2019 Aug 3; 12(8): 723-728.
[3]. Abad VC, Guilleminault C. Solriamfetol for the treatment of daytime sleepiness in obstructive sleep apnea. Expert Review of Respiratory Medicine. 2018 Dec 2; 12(12): 1007-1019.
[4]. Al-Rifai N, Alshishani A, Darras F, et al. Solriamfetol impurities: Synthesis, characterization, and analytical method (UPLC-UV) validation. Journal of pharmaceutical analysis. 2023 Apr 1; 13(4): 403-411.
[5]. Krief S, Berrebi‐Bertrand I, Nagmar I, et al. Pitolisant, a wake‐promoting agent devoid of psychostimulant properties: Preclinical comparison with amphetamine, modafinil, and solriamfetol. Pharmacology research & perspectives. 2021 Oct; 9(5): e00855.
[6]. Baladi MG, Forster MJ, Gatch MB, et al. Characterization of the neurochemical and behavioral effects of solriamfetol (JZP-110), a selective dopamine and norepinephrine reuptake inhibitor. The Journal of pharmacology and experimental therapeutics. 2018 Aug 1; 366(2): 367-376.
[7]. Sakai N, Nishino S. Comparison of Solriamfetol and Modafinil on Arousal and Anxiety-Related Behaviors in Narcoleptic Mice. Neurotherapeutics. 2023 Mar; 20(2): 546-563.
[8]. Badran M, Puech C, Barrow MB, et al. Solriamfetol enhances wakefulness and improves cognition and anxiety in a murine model of OSA. Sleep medicine. 2023 Jul 1; 107: 89-99.
Solriamfetol hydrochloride是一种多巴胺和去甲肾上腺素再摄取抑制剂。Solriamfetol hydrochloride能阻断突触前神经元对多巴胺和去甲肾上腺素的再摄取。Solriamfetol hydrochloride可用于治疗与发作性睡病或阻塞性睡眠呼吸暂停相关的日间嗜睡 [1-4]。
在CHO细胞中，Solriamfetol hydrochloride（2500和4100nM，3h）可抑制DA和NE转运体，从而增强神经传递 [5]。在HEK293细胞中，Solriamfetol hydrochloride（1nM-100μM，1.5h）对多巴胺（DA；IC50 = 2.9μM）和去甲肾上腺素（NE；IC50 = 4.4μM）转运蛋白具有双重再摄取抑制活性，并且这种活性在体内与微透析测定的细胞外DA和NE浓度升高有关 [6]。
在C57BL/6J小鼠中，Solriamfetol hydrochloride（30和100mg/kg，po，9h）以剂量依赖性方式显著增加小鼠的运动活性，表明其具有促觉醒和类似精神兴奋剂的作用 [5]。在大鼠中，Solriamfetol hydrochloride（30mg/kg，sc，10h）可提高纹状体和前额叶皮质中的DA和NE水平 [6]。在TetO-DTA小鼠模型中，Solriamfetol hydrochloride（50、100和150mg/kg，po，9h）以剂量依赖性方式有效促进野生型和发作性睡病DTA小鼠的觉醒 [7]。在小鼠OSA模型中，Solriamfetol hydrochloride（200mg/kg，ip，9d）可增强觉醒，改善认知能力和焦虑 [8]。
| Cell experiment []: | |
Cell lines | CHO cells |
Preparation Method | DAT- and NET-expressing CHO cells were seeded in 96-well clear-bottom microplates at a seeding density of 200,000 cells/well. During the 3h incubation, cells were treated with various concentrations of Solriamfetol hydrochloride. |
Reaction Conditions | 2500 and 4100nM; 3h |
Applications | Solriamfetol hydrochloride inhibits DA and NE transporters, thereby enhancing neurotransmission. |
| Animal experiment []: | |
Animal models | TetO-DTA mice model |
Preparation Method | TetO-DTA mice were given Solriamfetol hydrochloride (50, 100, and 150mg/kg) by oral injection during ZT2 (resting) or ZT14 (active) for 9h. |
Dosage form | 50, 100, and 150mg/kg; po; 9h |
Applications | Solriamfetol hydrochloride improved the duration and number of wakefulness in DTA mice after 9h administration. |
References: | |
| Cas No. | 178429-65-7 | SDF | |
| Canonical SMILES | N[C@@H](COC(N)=O)CC1=CC=CC=C1.[H]Cl | ||
| 分子式 | C10H15ClN2O2 | 分子量 | 230.69 |
| 溶解度 | DMSO: 250 mg/mL (1083.71 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.3348 mL | 21.6741 mL | 43.3482 mL |
| 5 mM | 0.867 mL | 4.3348 mL | 8.6696 mL |
| 10 mM | 0.4335 mL | 2.1674 mL | 4.3348 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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Quality Control & SDS
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- Purity: >99.50%
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