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P0099

Sigma-Aldrich

Paliperidone

≥98% (HPLC)

Synonym(s):

3-[2-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one, 9-Hydroxyrisperidone

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About This Item

Empirical Formula (Hill Notation):
C23H27FN4O3
CAS Number:
Molecular Weight:
426.48
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to brown

solubility

DMSO: 2 mg/mL, clear (warmed)

originator

Johnson & Johnson

storage temp.

room temp

SMILES string

CC1=C(CCN2CCC(CC2)c3noc4cc(F)ccc34)C(=O)N5CCCC(O)C5=N1

InChI

1S/C23H27FN4O3/c1-14-17(23(30)28-9-2-3-19(29)22(28)25-14)8-12-27-10-6-15(7-11-27)21-18-5-4-16(24)13-20(18)31-26-21/h4-5,13,15,19,29H,2-3,6-12H2,1H3

InChI key

PMXMIIMHBWHSKN-UHFFFAOYSA-N

Gene Information

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Application

Paliperidone has been used as an atypical antipsychotic drug (AAPD) to study its efficacy in preventing psychopathology of mice prenatally immune challenged with lipopolysaccharide (LPS). It has also been used as an atypical antipsychotic drug (AAPD) to explain the modulation of hypothalamic-pituitary-adrenal (HPA) axis in female mice prenatally treated with bacterial endotoxin lipopolysaccharide (LPS).

Biochem/physiol Actions

Paliperidone is an atypical antipsychotic; active metabolite of risperidone.

Features and Benefits

This compound is featured on the Dopamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Johnson & Johnson. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

pictograms

Skull and crossbones

signalword

Danger

hcodes

Hazard Classifications

Acute Tox. 3 Oral

Storage Class

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges


Certificates of Analysis (COA)

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Umesh Kumar et al.
European journal of pharmacology, 747, 181-189 (2014-09-23)
Studies on animal models provide enough evidences that old age appearance of psychosis on exposures to various insults during critical period of brain development could be prevented by antipsychotic drug treatment. Presently, gestational intervention of the atypical antipsychotic paliperidone (PAL)
Eliyahu Dremencov et al.
Psychopharmacology, 194(1), 63-72 (2007-05-29)
Paliperidone (9-OH-risperidone) is the main metabolite of the atypical antipsychotic risperidone. While both drugs are potent dopamine (D)2 antagonists, they have quantitative differential affinities for serotonin (5-HT) and norepinephrine (NE) receptor binding sites. The present study aimed to determine if
Pierre S Chue et al.
Expert review of neurotherapeutics, 12(12), 1399-1410 (2012-12-15)
Paliperidone, or 9-hydroxyrisperidone (Invega(®), Janssen, Antwerp, Belgium) is the major active metabolite of the atypical antipsychotic risperidone (Risperdal(®), Janssen). It possesses a similar, though not identical, receptor pharmacology to the parent molecule. There are additional differences in terms of its
Danielle M Butzbach et al.
Journal of forensic sciences, 58(1), 90-100 (2012-09-22)
The stability of two benzisoxazole antipsychotics was determined in vitro in decomposing porcine blood inoculated with bacteria, utilizing a high-performance liquid chromatography with ultraviolet and fluorescence detection method for drug quantitation. Stability experiments for risperidone and paliperidone were conducted at
Angela C Doran et al.
Drug metabolism and disposition: the biological fate of chemicals, 40(11), 2162-2173 (2012-08-18)
Previous publications suggest that interstitial fluid compound concentrations (C(ISF)) best determine quantitative neurotherapeutic pharmacology relationships, although confirming large animal C(ISF) remains elusive. Therefore, this work primarily evaluated using respective acute dose, rat-derived unbound brain compound concentration-to-unbound plasma compound concentration ratios

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