Iloperidone-d3 is intended for use as an internal standard for the quantification of iloperidone by GC- or LC-MS. Iloperidone is an atypical antipsychotic and adrenergic, dopamine, and serotonin (5-HT) receptor antagonist.1 It binds to several receptors, including the α1-adrenergic receptor (α1-AR), α2-AR, and dopamine D2 receptor (Kis = 0.31, 3, and 3.3 nM, respectively), as well as the 5-HT1A, 5-HT1D, 5-HT2A, and 5-HT2C receptors (Kis = 33, 15, 0.2, and 14 nM, respectively) in radioligand binding assays using human post-mortem brain tissue.2 Iloperidone also binds to human D1, D3, D4, D5, and rat 5-HT2 receptors (Kis = 216, 7.1, 25, 319, and 3.1 nM, respectively, in CHO cells) and the histamine H1 receptor (Ki = 12.3 nM in human post-mortem brain tissue).3,2 Iloperidone (1-3 mg/kg) prevents the reduction in prepulse inhibition induced by apomorphine , phencyclidine (PCP), and cirazoline in rats.1 It also increases the time rats spend in the open arms of the elevated plus maze and the number of social interactions when administered at a dose of 0.5 mg/kg.4 Formulations containing iloperidone have been used in the treatment of schizophrenia.
1.Barr, A.M., Powell, S.B., Markou, A., et al.Iloperidone reduces sensorimotor gating deficits in pharmacological models, but not a developmental model, of disrupted prepulse inhibition in ratsNeuropharmacology51(3)457-465(2006) 2.Richelson, E., and Souder, T.Binding of antipsychotic drugs to human brain receptors: Focus on newer generation compoundsLife Sci.68(1)29-39(2000) 3.Kongsamut, S., Roehr, J.E., Cai, J., et al.Iloperidone binding to human and rat dopamine and 5-HT receptorsEur. J. Pharmacol.317(2-3)417-423(1996) 4.Szewczak, M.R., Corbett, R., Rush, D.K., et al.The pharmacological profile of iloperidone, a novel atypical antipsychotic agentJ. Pharmacol. Exp. Ther.274(3)1404-1413(1995)