Paliperidone

Catalog No.S1724

For research use only.

Paliperidone, the main active metabolite of Risperidone, is a potent serotonin-2A and dopamine-2 receptor antagonist, used in the treatment of schizophrenia.

Paliperidone  Chemical Structure

CAS No. 144598-75-4

Selleck's Paliperidone has been cited by 1 Publication

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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 (from reference)

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 426.48
Formula

C23H27FN4O3

CAS No. 144598-75-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C(=O)N2CCCC(C2=N1)O)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04072575 Active not 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 Baltimore January 2014 Not Applicable
NCT01926912 Completed Drug: No intervention Schizophrenia Janssen-Cilag International NV May 2013 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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.

Handling Instructions

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