Iloperidone

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.

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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).