Molecular Weight(MW): 426.48
Paliperidone, the main active metabolite of Risperidone, is a potent serotonin-2A and dopamine-2 receptor antagonist, used in the treatment of schizophrenia.
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Choose Selective Dopamine Receptor Inhibitors
|Description||Paliperidone, the main active metabolite of Risperidone, is a potent serotonin-2A and dopamine-2 receptor antagonist, used in the treatment of schizophrenia.|
Paliperidone significantly increases the intracellular accumulation of Rh123 and DOX in a concentration-dependent manner.  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.  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. 
|In vivo||Paliperidone normalizes prefrontal cortical basal extracellular glutamate in rats. Paliperidone also prevents the acute MK-801-induced increase in extracellular glutamate in rats.  Paliperidone coadministered with Escitalopram restores the suppression of the NE neuronal firing rate (n = 5 rats) and the percentage of neurons exhibiting burst firing.  Paliperidone results in a dose-dependent decrease in bite and attack behaviors with an effective dose. Paliperidone results in the maximal reduction in aggressive behavior. |
-  Zhu HJ, et al. Neuropsychopharmacology, 2007, 32(4), 757-764.
-  Yang MC, et al. Psychopharmacology (Berl), 2011, 217(3), 397-410.
-  Gass?P, et al. Prog Neuropsychopharmacol Biol Psychiatry, 2012, 36(1), 71-77.
|In vitro||DMSO||4 mg/mL warmed (9.37 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02918825||Recruiting||Schizophrenia||Beijing HuiLongGuan Hospital|WenZhou-Kangning Hospital||September 2016||--|
|NCT02713282||Recruiting||Schizophrenia||Janssen-Cilag Ltd.||April 2016||Phase 3|
|NCT02634463||Recruiting||Immunoassay|Antipsychotic||Janssen Research & Development, LLC||November 2015||Phase 1|
|NCT02431702||Recruiting||Schizophrenia|Psychotic Disorders||Janssen Scientific Affairs, LLC||July 2015||Phase 3|
|NCT02600741||Recruiting||Schizophrenia||Janssen Scientific Affairs, LLC||July 2015||Phase 4|
|NCT02462473||Completed||Schizophrenia|Schizoaffective Disorder||Janssen Research & Development, LLC||May 2015||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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