Solriamfetol hydrochloride
目录号 : GC39443
Solriamfetol hydrochloride (JZP-110 hydrochloride) 是一种口服有效的，选择性的多巴胺和去甲肾上腺素再摄取抑制剂，对多巴胺和去甲肾上腺素转运蛋白的 IC50 分别为 2.9 μM 和 4.4 μM。Solriamfetol hydrochloride 具有强大的促唤醒作用。
Cas No.:178429-65-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Solriamfetol hydrochloride (JZP-110 hydrochloride) is an orally active and selective dopamine and norepinephrine reuptake inhibitor with IC50s of 2.9 μM and 4.4 μM for dopamine and norepinephrine transporters, respectively. Solriamfetol hydrochloride has robust wake-promoting effects[1][2].
[1]. Baladi MG, et al. Characterization of the Neurochemical and Behavioral Effects of Solriamfetol (JZP-110), a Selective Dopamine and Norepinephrine Reuptake Inhibitor. J Pharmacol Exp Ther. 2018 Aug;366(2):367-376. [2]. Yang J, et al. Solriamfetol for the treatment of excessive daytime sleepiness associated with narcolepsy. Expert Rev Clin Pharmacol. 2019 Aug;12(8):723-728.
| 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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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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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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1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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A randomized study of Solriamfetol for excessive sleepiness in narcolepsy
Ann Neurol 2019 Mar;85(3):359-370.PMID:30694576DOI:10.1002/ana.25423.
Objective: Solriamfetol (JZP-110) is a selective dopamine and norepinephrine reuptake inhibitor with wake-promoting effects. This phase 3 study (NCT02348593) evaluated the safety and efficacy of Solriamfetol in narcolepsy. Methods: Patients with narcolepsy with mean sleep latency <25 minutes on the Maintenance of Wakefulness Test (MWT), Epworth Sleepiness Scale (ESS) score ≥10, and usual nightly sleep ≥6 hours were randomized to Solriamfetol 75, 150, or 300 mg, or placebo for 12 weeks. Coprimary endpoints were change from baseline to week 12 in MWT and ESS. Improvement on the Patient Global Impression of Change (PGI-C) was the key secondary endpoint. Results: Safety and modified intention-to-treat populations included 236 and 231 patients, respectively. Solriamfetol 300 and 150 mg were positive on both coprimary endpoints. Least squares mean (standard error [SE]) changes from baseline were 12.3 (SE = 1.4) and 9.8 (SE = 1.3) minutes for Solriamfetol 300 and 150 mg on the MWT, respectively, versus 2.1 (SE = 1.3) minutes for placebo, and -6.4 (SE = 0.7) for 300 mg and -5.4 (SE = 0.7) for 150 mg on the ESS versus -1.6 (SE = 0.7) for placebo (all p < 0.0001). At week 12, higher percentages of patients treated with Solriamfetol 150 mg (78.2%) and 300 mg (84.7%) reported PGI-C improvement relative to placebo (39.7%; both p < 0.0001). Adverse events ≥5% across all Solriamfetol doses included headache (21.5%), nausea (10.7%), decreased appetite (10.7%), nasopharyngitis (9.0%), dry mouth (7.3%), and anxiety (5.1%). Interpretation: Solriamfetol has the potential to be an important therapeutic option for the treatment of impaired wakefulness and excessive sleepiness in patients with narcolepsy. ANN NEUROL 2019;85:359-370.
Idiopathic Hypersomnia and Other Hypersomnia Syndromes
Neurotherapeutics 2021 Jan;18(1):20-31.PMID:32901432DOI:10.1007/s13311-020-00919-1.
There are numerous disorders of known or presumed neurologic origin that result in excessive daytime sleepiness, collectively known as the central disorders of hypersomnolence. These include narcolepsy types 1 and 2, idiopathic hypersomnia, Kleine-Levin syndrome, and hypersomnia due to or associated with medical disease, neurologic disease, psychiatric disease, medications or substances, and insufficient sleep durations. This chapter focuses on the treatment of nonnarcoleptic hypersomnia syndromes, from those that are commonly encountered in neurologic practice, such as hypersomnia due to Parkinson's disease, to those that are exceedingly rare but present with dramatic manifestations, such as Kleine-Levin syndrome. The level of evidence for the treatment of sleepiness in these disorders is generally lower than in the well-characterized syndrome of narcolepsy, but available clinical and randomized, controlled trial data can provide guidance for the management of each of these disorders. Treatments vary by diagnosis but may include modafinil/armodafinil, traditional psychostimulants, Solriamfetol, pitolisant, clarithromycin, flumazenil, sodium oxybate, melatonin, methylprednisolone, and lithium.
Recently Approved and Upcoming Treatments for Narcolepsy
CNS Drugs 2020 Jan;34(1):9-27.PMID:31953791DOI:10.1007/s40263-019-00689-1.
Narcolepsy is a chronic, disabling neurologic disorder characterised by excessive daytime sleepiness (EDS) and, in up to 60% of patients, cataplexy. Treatments for narcolepsy are aimed at improving wakefulness (e.g. modafinil, armodafinil, stimulants), reducing cataplexy attacks (e.g. sodium oxybate, venlafaxine), and treating the symptoms of disturbed nocturnal sleep, sleep paralysis and sleep-related hallucinations (e.g. sodium oxybate). In general, medications that increase the release, or inhibit the reuptake, of norepinephrine or dopamine have wake-promoting effects and are useful in managing EDS, whereas medications that inhibit serotonin or norepinephrine reuptake have anticataplectic effects. Modulation of γ-aminobutyric acid B (GABAB) receptors or histamine H3 receptors (H3Rs) has effects on both EDS and cataplexy. Pitolisant, an H3R antagonist, and Solriamfetol, a dopamine and norepinephrine reuptake inhibitor, are the most recently approved treatments for EDS associated with narcolepsy in the European Union (pitolisant) and the USA (pitolisant and Solriamfetol). Several new agents are being developed and tested as potential treatments for EDS and cataplexy associated with narcolepsy; these agents include novel oxybate formulations (once-nightly [FT218]; low sodium [JZP-258]), a selective norepinephrine reuptake inhibitor (AXS-12), and a product combining modafinil and an astroglial connexin inhibitor (THN102). This review summarises the mechanisms of action, pharmacokinetics, efficacy, and safety/tolerability of recently approved and emerging treatments for narcolepsy.
Solriamfetol for the Use of Narcolepsy: A Systematic Review
Cureus 2022 May 12;14(5):e24937.PMID:35706734DOI:10.7759/cureus.24937.
Narcolepsy is a chronic and disabling neurological disorder characterized by excessive daytime sleepiness (EDS) and cataplexy. Historically, some medications have demonstrated efficacy in managing EDS and cataplexy symptoms. However, some patients cannot tolerate them, become refractory, or may use concomitant medications that preclude the use due to drug-drug interaction. Therefore, there is a necessity to explore the efficacy of new treatments, such as Solriamfetol (JZP-110), a 2019 FDA-approved drug indicated to improve wakefulness in adults with EDS associated with narcolepsy. We conducted this systematic review to investigate the effectiveness of Solriamfetol in EDS and cataplexy, and the drug's overall safety. For this study, we used the PRISMA (Preferred Reporting Items for Systematic Reviews and Meta-Analyses) guidelines and MOOSE protocol. After an initial search of 119 papers, we included four clinical trials to investigate and analyze the use of Solriamfetol for the treatment of narcolepsy. Solriamfetol was proven to improve objective measures of EDS in all clinical trials. We conducted this systematic review using objective measures such as the Epworth Sleepiness Scale and the Maintenance of Wakefulness Test. Overall, cataplexy was not formally evaluated in the four clinical trials; however, it demonstrated that EDS improved in patients with and without cataplexy. More clinical trials are needed to analyze the efficacy of Solriamfetol on cataplexy. The effect of Solriamfetol in EDS seems to be conclusive.
Solriamfetol for the Management of Excessive Daytime Sleepiness
J Pharm Pract 2022 Dec;35(6):963-970.PMID:33882756DOI:10.1177/08971900211009080.
Objective: To review efficacy, safety, and place in therapy of Solriamfetol for management of excessive daytime sleepiness (EDS) in patients with narcolepsy and obstructive sleep apnea (OSA). Methods: PubMed (1966 to January 2021) was searched using the terms Solriamfetol, JZP-110, ADX-N05 and Sunosi. Human studies published in peer-reviewed medical journals in English language were reviewed. Results: The efficacy and safety of Solriamfetol has been reported in 2 phase II trials and 4 phase III trials (TONES 2, TONES 3, TONES 4, and TONES 5). Statistically significant improvements in the maintenance of wakefulness test were reported with Solriamfetol 150 mg and 300 mg vs placebo in participants with narcolepsy (7.65- to 10.14-minute difference from placebo). In subjects with OSA, statistically significant improvements in maintenance of wakefulness test difference from placebo were also observed in those taking Solriamfetol 75 mg, 150 mg, or 300 mg vs placebo (4.5- to 12.8-minute difference from placebo). Statistically significant reductions in Epworth Sleepiness Scale scores were also reported in phase III trials in subjects with narcolepsy or OSA taking Solriamfetol vs placebo (ranging from - 4.7 to - 1.9 difference from placebo). Common adverse events in reported in phase III trials were headache, nausea, decreased appetite, anxiety, dry mouth, and diarrhea. Solriamfetol appears to have a reduced risk for drug interactions and fewer adverse effects compared to other agents available for management of EDS in patients with narcolepsy and OSA. Conclusions: Solriamfetol is an effective option for management of EDS in patients with narcolepsy and OSA.