

生物活性
产品描述 |
Paliperidone(Invega) is used as an atypical antipsychotic. It applies to the acute and maintenance treatment of schizophrenia. Chemically, paliperidone is the primary active metabolite of the older atypical antipsychotic risperidone. |
靶点活性 |
5-HT, Dopamine, H1 receptor, β-adrenergic receptor, |
体外活性 |
Paliperidone significantly increases the intracellular accumulation of Rh123 and DOX in a concentration-dependent manner. [1] Paliperidone works finely at low concentrations (10 and 50 μM) against Aβ(25-35) and MPP(+) and solely protects SH-SY5Y from hydrogen peroxide. Paliperidone (100 μM) completely diminishes cell reduction induced by different stressors, regardless of their dosages. Paliperidone is demonstrated with higher oxidative stress-scavenging properties than other APDs in several aspects, such as generated bulk glutathione, low HNE, and protein carbonyl productions. [2] Paliperidone enhances dopamine toxicity at the highest dose and is the only AP that significantly increases cell viability (8.1%) compared with cells treated with dopamine alone. [3] |
体内活性 |
化学信息
分子量 |
426.48 |
分子式 |
C23H27FN4O3 |
CAS |
144598-75-4 |
溶解度 |
DMSO: 4.3 mg/mL (10 mM) ( < 1 mg/ml refers to the product slightly soluble or insoluble ) |
储存条件 |
store at -80°C |
备注 |
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
配制溶液
1 mg | 5 mg | 10 mg | |
1 mM | 2.345 ml | 11.724 ml | 23.448 ml |
5 mM | 0.469 ml | 2.345 ml | 4.69 ml |
10 mM | 0.234 ml | 1.172 ml | 2.345 ml |
50 mM | 0.047 ml | 0.234 ml | 0.469 ml |
参考文献
- 1. Zhu HJ, et al. Neuropsychopharmacology, 2007, 32(4), 757-764.
- 2. Yang MC, et al. Psychopharmacology (Berl), 2011, 217(3), 397-410.
- 3. Gassó P, et al. Prog Neuropsychopharmacol Biol Psychiatry, 2012, 36(1), 71-77.
- 4. Roenker NL, et al. Neurosci Lett, 2011, 500(3), 167-171.
- 5. Dremencov E, et al. Psychopharmacology (Berl), 2007, 194(1), 63-72.