Solriamfetol
目录号 : GC39184
Solriamfetol (JZP-110) 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 具有强大的促唤醒作用。
Cas No.:178429-62-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Solriamfetol (JZP-110) 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 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. | 178429-62-4 | SDF | |
| Canonical SMILES | N[C@@H](COC(N)=O)CC1=CC=CC=C1 | ||
| 分子式 | C10H14N2O2 | 分子量 | 194.23 |
| 溶解度 | DMSO: 250 mg/mL (1287.13 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 | 5.1485 mL | 25.7427 mL | 51.4854 mL |
| 5 mM | 1.0297 mL | 5.1485 mL | 10.2971 mL |
| 10 mM | 0.5149 mL | 2.5743 mL | 5.1485 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 | ||||||||||
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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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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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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.
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.
Solriamfetol for the treatment of excessive daytime sleepiness associated with narcolepsy
Expert Rev Clin Pharmacol 2019 Aug;12(8):723-728.PMID:31215815DOI:10.1080/17512433.2019.1632705.
Introduction: Narcolepsy is a chronic disabling condition, excessive daytime somnolence is the main symptoms of it. There is currently no cure for narcolepsy, and hence there is a great need for new treatment options. Solriamfetol is a new selective dopamine and norepinephrine reuptake inhibitor with robust wake-promoting effects. The purpose of this paper is to review Solriamfetol. Areas covered: The chemical property, mechanism of action, pharmacokinetics, clinical efficacy, and safety of Solriamfetol are introduced in this paper. Expert opinion: Solriamfetol can bind to dopamine and norepinephrine transporters and inhibit reuptake of dopamine and norepinephrine. Clinical trials showed that Solriamfetol could significantly improve the ability to stay awake and subjective symptoms of excessive sleepiness in adults with narcolepsy. Solriamfetol was well tolerated. Very common adverse reactions were headache, nausea, decreased appetite, insomnia, and anxiety.
Solriamfetol for Excessive Sleepiness in Narcolepsy and Obstructive Sleep Apnea
Ann Pharmacother 2020 Oct;54(10):1016-1020.PMID:32270686DOI:10.1177/1060028020915537.
Objective: The purpose of this article is to review the available clinical trial data that led to the Food and Drug Administration (FDA) approval of Solriamfetol as well as its role in clinical practice. Data sources: A MEDLINE/PubMed search was conducted (January 2000 to February 2020) using the keyword Solriamfetol to discover appropriate clinical trials. Study selection and data extraction: Articles were included that were published in the English language and related to the FDA approval of Solriamfetol or provided novel information regarding this drug entity. Data synthesis: The findings of the review show that Solriamfetol may be a safe and effective option for the treatment of excessive sleepiness (ES) related to narcolepsy and obstructive sleep apnea (OSA). Relevance to patient care and clinical practice: Solriamfetol is distinguished from other stimulants in that it has lower binding affinity to dopamine and norepinephrine transporters and does not have the monoamine-releasing effects of amphetamines at usual therapeutic doses. Because of Solriamfetol's unique mechanism of action, there may be a reduction in abuse potential compared with the other currently FDA-approved options. Conclusions: In clinical trials, Solriamfetol has shown dose-dependent improvement in wakefulness over placebo and adds another option for clinicians when treating ES in narcolepsy and OSA.