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KI0874Paliperidone100 mg$154

Chemical Characteristic

Product NamePaliperidone
SynonymsInvega
CAS No.144598-75-4
Molecular Weight 426.48
FormulaC23H27FN4O3
Chemical Structure

Biological activities

Paliperidone is an atypical antipsychotic agent. Paliperidone is used in the treatment of the acute and maintenance treatment of schizophrenia. Paliperidone is the major active metabolite of risperidone and acts at dopamine D2 and serotonin 5HT2A receptors. Paliperidone also has binding activity as an antagonist at α1- and α2 adrenergic receptors and H1 histaminergic receptors. Paliperidone has been shown to be effective in reducing positive and negative syndrome scale total scores in four short-term trials in acute schizophrenia.[1] The IC50 of paliperidone for inhibiting P-gp-mediated transport of Rh123 and DOX are >100 µM. The Ki for binding to the dopamine D2 and 5HT2A receptor subtype for paliperidone are 0.16 and 0.25 nM, respectively. [2] In vivo, cytochrome P450 (CYP)2D6 and CYP3A4 play a limited role in the metabolism of paliperidone. [1]

References

[1] Delia Bishara, et al. Once-monthly paliperidone injection for the treatment of schizophrenia. Neuropsychiatr Dis Treat. 2010, 6: 561閳?72. 閵嗏偓閵嗏偓
[2] Zhu HJ, et al. Risperidone and paliperidone inhibit p-glycoprotein activity in vitro. Neuropsychopharmacology. 2007, 32(4): 757-764. 閵嗏偓閵嗏偓

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