Paliperidone

Catalog No.S1724

Paliperidone  Chemical Structure

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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Biological Activity

Description Paliperidone, the main active metabolite of Risperidone, is a potent serotonin-2A and dopamine-2 receptor antagonist, used in the treatment of schizophrenia.
Targets
Dopamine receptor [1]
In vitro

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]

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. [4] Paliperidone coadministered with Escitalopram restores the suppression of the NE neuronal firing rate (n = 5 rats) and the percentage of neurons exhibiting burst firing. [5] 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. [6]

Protocol

Solubility (25°C)

In vitro DMSO 4 mg/mL warmed (9.37 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 426.48
Formula

C23H27FN4O3

CAS No. 144598-75-4
Storage powder
Synonyms N/A

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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

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Dopamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID