Paliperidone

Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia[1].

Product Specifications

CAS Number

[144598-75-4]

Product Name Alternative

9-Hydroxyrisperidone

UNSPSC

12352005

Hazard Statement

H301

Target

5-HT Receptor; Adrenergic Receptor; Dopamine Receptor; Drug Metabolite

Type

Natural Products

Related Pathways

GPCR/G Protein; Metabolic Enzyme/Protease; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Paliperidone.html

Purity

99.69

Solubility

DMSO : 5 mg/mL (ultrasonic)

Smiles

CC1=C(C(N2CCCC(C2=N1)O)=O)CCN3CCC(CC3)C4=NOC5=C4C=CC(F)=C5

Molecular Formula

C23H27FN4O3

Molecular Weight

426.48

Precautions

H301

References & Citations

[1]Peng L, et al. Paliperidone protects prefrontal cortical neurons from damages caused by MK-801 via Akt1/GSK3β signaling pathway. Schizophr Res. 2013 Jun;147 (1) :14-23.|[2]Yang MC, et al. Neuroprotection of paliperidone on SH-SY5Y cells against β-amyloid peptide (25-35), N-methyl-4-phenylpyridinium ion, and hydrogen peroxide-induced cell death. Psychopharmacology (Berl) . 2011 Oct;217 (3) :397-410.|[3]Kalman S, et al. 9-hydroxy-risperidone (9OHRIS) prevents stress-induced β-actin overexpression in rat hippocampus. Neuropsychopharmacol Hung. 2010 Sep;12 (3) :425-31.|[4]Mauri MC, Paletta S, Maffini M, et al. Clinical pharmacology of atypical antipsychotics: an update. EXCLI J. 2014;13:1163-1191. Published 2014 Oct 13.|[5]Peng L, et al. Paliperidone protects SK-N-SH cells against glutamate toxicity via Akt1/GSK3β signaling pathway. Schizophr Res. 2014 Aug;157 (1-3) :120-7. |[6]Gassó P, et al. Neurotoxic/neuroprotective activity of haloperidol, risperidone and paliperidone in neuroblastoma cells. Prog Neuropsychopharmacol Biol Psychiatry. 2012 Jan 10;36 (1) :71-7.|[7]Boyda HN, et al. A comparison of the metabolic side-effects of the second-generation antipsychotic drugs risperidone and paliperidone in animal models. PLoS One. 2021 Jan 28;16 (1) :e0246211.