Iloperidone-d₃

Iloperidone-d₃ is intended for use as an internal standard for the quantification of iloperidone (Item No. 22957) 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 (Item No. 16094), phencyclidine (PCP), and cirazoline (Item No. 21791) 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.

WARNING This product is not for human or veterinary use.

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 rats. Neuropharmacology 51(3), 457-465 (2006).

2. 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).

3. Kongsamut, S., Roehr, J.E., Cai, J., et al. Iloperidone binding to human and rat dopamine and 5-HT receptors. Eur. 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 agent. J. Pharmacol. Exp. Ther. 274(3), 1404-1413 (1995).