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Paliperidone

Paliperidone is an antipsychotic compound that inhibits D2 receptors and 5-HT2A receptors and is used to treat schizophrenia. Paliperidone also attenuates epinephrine- and serotonin-induced platelet aggregation.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18952469

Cas No.

144598-75-4

Purity

≥97%

Formula

C23H27FN4O3

Formula Wt.

426.48

IUPAC Name

3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one

Synonym

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-OH-risperidone

Melting Point

158-160°C

Solubility

DMSO: >5 mg/mL

Appearance

An offwhite or pale yellow powder

Kozielska M, Johnson M, Pilla Reddy V, et al. Pharmacokinetic-pharmacodynamic modeling of the D2 and 5-HT (2A) receptor occupancy of risperidone and paliperidone in rats. Pharm Res. 2012 Jul;29(7):1932-48. PMID: 22437487.

Gilday E, Nasrallah HA. Clinical pharmacology of paliperidone palmitate a parenteral long-acting formulation for the treatment of schizophrenia. Rev Recent Clin Trials. 2012 Feb;7(1):2-9. PMID: 22023179.

De Clerck F, Somers Y, Mannaert E, et al. In vitro effects of risperidone and 9-hydroxy-risperidone on human platelet function, plasma coagulation, and fibrinolysis. Clin Ther. 2004 Aug;26(8):1261-73. PMID: 15476907.

ABT-628