Paliperidone

Paliperidone is an atypical antipsychotic.¹ It is an inverse agonist of dopamine D₂ and D₃ receptors (IC₅₀s = 1 and 0.9 nM, respectively), as well as an antagonist at these receptors (K_is = 0.4 and 0.1 nM, respectively).² Paliperidone also binds to α₁- and α₂-adrenergic receptors, histamine H₁ receptors, and the serotonin (5-HT) receptor subtypes 5-HT_1A, 5-HT_1D, 5-HT_2A, and 5-HT_2C (K_ds = 10.1, 80, 3.4, 480, 19, 1.21, and 48 nM, respectively).³ It improves spatial working memory in a T-maze alternation task in a maternal immune activation mouse model of schizophrenia when administered at a dose of 0.05 mg/kg per day.¹ Paliperidone is also an active metabolite of the atypical antipsychotic risperidone (Item No. 13629).³ Formulations containing paliperidone have been used in the treatment of schizophrenia and schizoaffective disorder.

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1. MacDowell, K.S., Munarriz-Cuezva, E., Caso, J.R., et al. Paliperidone reverts Toll-like receptor 3 signaling pathway activation and cognitive deficits in a maternal immune activation mouse model of schizophrenia. Neuropharmacology 116, 196-207 (2017).

2. Burstein, E.S., Ma, J., Wong, S., et al. Intrinsic efficacy of antipsychotics at human D₂, D₃, and D₄ dopamine receptors: Identification of the clozapine metabolite N-desmethylclozapine as a D₂/D₃ partial agonist. J. Pharmacol. Exp. Ther. 315(3), 1278-1287 (2005).

3. Richelson, E., and Souder, T. Binding of antipsychotic drugs to human brain receptors: Focus on newer generation compounds. Life Sci. 68(1), 29-39 (2000).