Paliperidone-d4 is intended for use as an internal standard for the quantification of paliperidone by GC- or LC-MS. 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 (Kis = 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-HT1A, 5-HT1D, 5-HT2A, and 5-HT2C (Kds = 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 .3 Formulations containing paliperidone have been used in the treatment of schizophrenia and schizoaffective disorder.
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 schizophreniaNeuropharmacology116196-207(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 agonistJ. 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 compoundsLife Sci.68(1)29-39(2000)