产品说明书
Rizatriptan benzoate
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同义名 : | MK 462;Rizatriptan (benzoate salt);Maxalt;2-(5-((1H-1,2,4-TRIAZOL-1-YL)METHYL)-1H-INDOL-3-YL)-N,N-DIMETHYLETHANAMINE BENZOATE;MK-0462;MK-462 Benzoate |
| CAS号 : | 145202-66-0 | |
| 货号 : | A343353 | |
| 分子式 : | C22H25N5O2 | |
| 纯度 : | 98% | |
| 分子量 : | 391.466 | |
| MDL号 : | MFCD00866224 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(127.72 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 100 mg/mL(255.45 mM)，配合低频超声助溶 |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Rizatriptan Benzoate is an orally active serotonin 5-HT(1) receptor agonist that potently and selectively binds to 5-HT(1B/1D) subtypes. Oral rizatriptan 5 and 10mg have shown greater efficacy than placebo in providing pain relief, an absence of pain, relief from associated symptoms, normal functional ability and an improvement in patient quality of life. Rizatriptan 10mg provides faster pain relief and a higher percentage of patients with an absence of pain and normal functional ability at 2 hours than naratriptan 2.5mg or zolmitriptan 2.5mg[3]. Rizatriptan Benzoate is a selective 5-hydroxy tryptamine receptor agonist with anti migraine property. The rizatriptan benzoate oral disintegrating strip is potentially a useful tool for an effective treatment of migraine with improved bioavailability, rapid onset of action and with increased patient compliance[4]. Rizatriptan benzoate significantly reduced expression of the mRNAs for proenkephalin and substance P. Rizatriptan benzoate may inhibit the analgesic effect of the endogenous pain modulatory system[5]. In addition, the brain uptake potential of optimized RB-SLNs (rizatriptan benzoate-loaded solid lipid nanoparticles) to be 18.43-folds higher with respect to the pure drug in its free form, post 2 h of oral drug administration. RB-SLNs have distinctly improved brain target ability[6]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.55mL 0.51mL 0.26mL |
12.77mL 2.55mL 1.28mL |
25.54mL 5.11mL 2.55mL |
| 参考文献 |
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