PaliperIDOne 是 RisperIDOne 的主要活性代谢产物,是多巴胺 D2 拮抗剂和5-HT2A拮抗剂。它用作非典型抗精神病药,用于精神分裂症的急性及维持治疗。它对α1和α2肾上腺素能受体和H1组胺能受体也有拮抗作用。
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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.
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]
Cas No.
144598-75-4
分子式
C23H27FN4O3
分子量
426.492
别名
9-hydroxyrisperidone;9-羟基利培酮;帕潘立酮;Paliperidone
储存和溶解度
DMSO:4.3 mg/mL (10 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years