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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|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||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04072575||Recruiting||Drug: PP6M injection Dose 1|Drug: PP6M injection Dose 2||Schizophrenia||Janssen Research & Development LLC||September 19 2019||Phase 3|
|NCT02532842||Completed||--||Schizophrenia||Janssen Pharmaceutica N.V. Belgium||July 2015||--|
|NCT01584466||Withdrawn||Drug: Paliperidone||Schizophrenia||University of Maryland College Park|University of Maryland Baltimore||January 2014||Not Applicable|
|NCT01926912||Completed||Drug: No intervention||Schizophrenia||Janssen-Cilag International NV||May 2013||--|
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