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Paliperidone Dopamine Receptor antagonist

Cat.No.S1724

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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Quality Control

Batch: Purity: 99.94%
99.94

Solubility

In vitro
Batch:

5%TFA : 15 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 426.48 Formula

C23H27FN4O3

Storage (From the date of receipt)
CAS No. 144598-75-4 Download SDF Storage of Stock Solutions

Synonyms N/A SMILES CC1=C(C(=O)N2CCCC(C2=N1)O)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F

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Mechanism of Action

Targets/IC50/Ki
Dopamine receptor
In vitro
Paliperidone significantly increases the intracellular accumulation of Rh123 and DOX in a concentration-dependent manner. 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. 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.
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. 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. 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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/21699956/
  • [5] https://pubmed.ncbi.nlm.nih.gov/17530476/
  • [6] https://pubmed.ncbi.nlm.nih.gov/19066856/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-05-01)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07047651 ACTIVE_NOT_RECRUITING
Treatment Resistant Schizophrenia; Treatment Resistant Bipolar Disorder
Dr. Stavroula Rakitzi
2025-06-04 PHASE4
NCT04478838 RECRUITING
Schizophrenia and Related Disorders; Drug Administration Schedule; Drug Therapy; Antipsychotic Agents
Centre for Addiction and Mental Health
2022-06-06 PHASE4
NCT07493551 RECRUITING
Schizophrenia
CSPC Zhongnuo Pharmaceutical (Shijiazhuang) Co., Ltd.
2024-10-09
NCT07075237 NOT_YET_RECRUITING
Schizophrenia
Jiangsu Province Nanjing Brain Hospital
2025-10 PHASE4
NCT07153835 NOT_YET_RECRUITING
Schizophrenia
Sher-E-Bangla Medical College
2025-09-01 PHASE4
NCT06060886 UNKNOWN
Schizophrenia; Treatment-resistant Schizophrenia; Side Effect; Lipid Metabolism Disorders; Diabetes; NAFLD; Psychosis
Consorcio Centro de Investigación Biomédica en Red (CIBER)
2023-11-01 PHASE4

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