Iloperidone-d3

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 (K_is = 0.31, 3, and 3.3 nM, respectively), as well as the 5-HT_1A, 5-HT_1D, 5-HT_2A, and 5-HT_2C receptors (K_is = 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 (K_is = 216, 7.1, 25, 319, and 3.1 nM, respectively, in CHO cells) and the histamine H₁ receptor (K_i = 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)