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
in solvent
Synonyms N/A

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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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Dopamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID