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P0099

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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:
144598-75-4
Molecular Weight:
426.48
MDL number:
MFCD00871802
UNSPSC Code:
12352200
PubChem Substance ID:
329820012
NACRES:
NA.77

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

human ... DRD2(1813) , HTR2A(3356)

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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
GHS06

Signal Word

Danger

Hazard Statements

H301

Hazard Classifications

Acute Tox. 3 Oral

Storage Class Code

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

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Mehrul Hasnain et al.
CNS drugs, 28(10), 887-920 (2014-08-30)
We comprehensively reviewed published literature to determine whether it supported the link between corrected QT (QTc) interval prolongation and torsade de pointes (TdP) for the 11 second-generation antipsychotics and seven second-generation antidepressants commonly implicated in these complications. Using PubMed and
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
Richard Newton et al.
Current medical research and opinion, 28(4), 559-567 (2012-02-11)
Paliperidone palmitate is an atypical long-acting injectable (LAI) antipsychotic that has been approved for use in the US, EU, Australia and numerous other countries for acute and maintenance therapy of schizophrenia. LAI antipsychotics are often viewed as a 'last-resort' treatment
Saeko Ikai et al.
The Journal of clinical psychiatry, 73(8), 1147-1152 (2012-09-13)
While 65%-80% occupancy of dopamine D2 receptors with antipsychotics has been proposed to achieve optimal therapeutic response during acute treatment of schizophrenia, it remains unclear as to whether it is also necessary to maintain D2 receptor occupancy within this "safe"
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