产品说明书
Paliperidone
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同义名 : | 9-羟基利培酮 ;9-Hydroxyrisperidone;RO76477 |
| CAS号 : | 144598-75-4 | |
| 货号 : | A267994 | |
| 分子式 : | C23H27FN4O3 | |
| 纯度 : | 98% | |
| 分子量 : | 426.484 | |
| MDL号 : | MFCD00871802 | |
| 存储条件： |
粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 4 mg/mL(9.38 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 |
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| 动物实验配方： |
IP 5% DMSO+water 1 mg/mL clear PO 0.5% CMC-Na 65 mg/mL suspension |
| 生物活性 | |||
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| 靶点 |
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| 描述 | Paliperidone is a second-generation antipsychotic drug belonging to the class of benzisoxasole derivatives. Paliperidone is the major active metabolite of risperidone (9-OH-risperidone) and, as such, is comparable to the latter in terms of pharmacodynamic properties[3]. Paliperidone has demonstrated efficacy in the reduction of acute schizophrenia symptoms and clinical benefits were maintained also in the long-term treatments. Paliperidone ER (extended-release) and PP (paliperidone palmitate) are generally well tolerated with a predictable adverse event profile[4]. Paliperidone inhibited MK-801 induced neurotoxicity both in MTT metabolism assay and in lactate dehydrogenase (LDH) activity assay. Time course studies revealed that paliperidone effectively attenuated the elevation of intracellular free calcium concentration ([Ca(2+)]i) induced by exposure to MK-801. Moreover, paliperidone could significantly retard MK-801-mediated inhibition of neurite outgrowth and reverse MK-801-induced decreases of gene expression and phosphorylation of Akt1 and GSK3β[5]. Moreover, paliperidone works finely at low concentrations (10 and 50 μM) against Aβ(25-35) and MPP(+) and solely protected SH-SY5Y from hydrogen peroxide. At 100 μM, paliperidone completely diminished cell reduction induced by different stressors, regardless of their dosages. Paliperidone was demonstrated with a higher oxidative stress-scavenging properties than other APDs (Antipsychotic drugs) in several aspects, such as generated bulk glutathione, low HNE, and protein carbonyl productions[6]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01742390 | Sexual Dysfunction ... 展开 >> Hyperprolactinemia 收起 << | Phase 4 | Unknown | June 2014 | China, Beijing ... 展开 >> Institute of mental health, Peking University Not yet recruiting Beijing, Beijing, China, 100191 Contact: Tianmei Si, MD. 8610-82801948 si.tian-mei@163.cm Principal Investigator: Tianmei Si, MD. China, Hebei The first hospital of Hebei Province University Recruiting Shijiazhuang, Hebei, China, 050000 Contact: Xueyi Wang, Professor 0311-85917290 Sub-Investigator: Xueyi Wang 收起 << |
| NCT00589914 | Schizophrenia | Phase 3 | Completed | - | - |
| NCT02532842 | - | Completed | - | Croatia ... 展开 >> Rijeka, Croatia Split, Croatia Zagreb, Croatia Russian Federation Moscow, Russian Federation St Petersburg N/A, Russian Federation St-Petersburg, Russian Federation Turkey Ankara, Turkey Denizli, Turkey 收起 << | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.34mL 0.47mL 0.23mL |
11.72mL 2.34mL 1.17mL |
23.45mL 4.69mL 2.34mL |
| 参考文献 |
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