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Paliperidone Dopamine Receptor antagonist

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

Paliperidone Dopamine Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 426.48

Purity & Quality Control

Related Products

Signaling Pathway

Dopamine Receptor Signaling Pathways

Dopamine Receptor Signaling Pathway

Mechanism of Action

Targets
Dopamine receptor [1]

In vitro
In vitro Paliperidone significantly increases the intracellular accumulation of Rh123 and DOX in a concentration-dependent manner. [1] This compound works finely at low concentrations (10 and 50 μM) against Aβ(25-35) and MPP(+) and solely protects SH-SY5Y from hydrogen peroxide. It completely diminishes cell reduction induced by different stressors, regardless of their dosages. This chemical 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] It 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
In vivo Paliperidone normalizes prefrontal cortical basal extracellular glutamate in rats. This compound also prevents the acute MK-801-induced increase in extracellular glutamate in rats. [4] When coadministered with Escitalopram, it restores the suppression of the NE neuronal firing rate (n = 5 rats) and the percentage of neurons exhibiting burst firing. [5] It results in a dose-dependent decrease in bite and attack behaviors with an effective dose. This chemical results in the maximal reduction in aggressive behavior. [6]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06060886 Not yet recruiting
Schizophrenia|Treatment-resistant Schizophrenia|Side Effect|Lipid Metabolism Disorders|Diabetes|NAFLD|Psychosis
Consorcio Centro de Investigación Biomédica en Red (CIBER)|Instituto de Salud Carlos III
 November 1 2023 Phase 4
NCT02532842 Completed
Schizophrenia
Janssen Pharmaceutica N.V. Belgium
 July 2015 --
NCT01584466 Withdrawn
Schizophrenia
University of Maryland Baltimore
 January 2014 Not Applicable

References
  • https://pubmed.ncbi.nlm.nih.gov/16936711/
  • https://pubmed.ncbi.nlm.nih.gov/21523348/
  • https://pubmed.ncbi.nlm.nih.gov/21878360/
  • https://pubmed.ncbi.nlm.nih.gov/21699956/
  • https://pubmed.ncbi.nlm.nih.gov/17530476/
  • https://pubmed.ncbi.nlm.nih.gov/19066856/

Chemical Information

Molecular Weight 426.48 Formula

C23H27FN4O3
CAS No. 144598-75-4 SDF Download SDF
Synonyms N/A
Smiles CC1=C(C(=O)N2CCCC(C2=N1)O)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

5%TFA : 15 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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