Paliperidone-d4

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 (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 .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)