Iloperidone (hydrochloride)

Uses

Iloperidone hydrochloride (HP 873 hydrochloride) is a D2/5-HT2 receptor antagonist. Iloperidone hydrochloride is an atypical antipsychotic for the schizophrenia symptoms[1][2].

in vivo

IC 50

Rat D₂ Receptor: 54 nM (Ki); Rat 5-HT₂ Receptor: 3.1 nM (Ki); Rat D₁ Receptor: 546 nM (Ki); Rat 5-HT_1A Receptor: 168 nM (Ki); Rat 5-HT₆ Receptor: 42.7 nM (Ki); Rat 5-HT₇ Receptor: 21.6 nM (Ki); Human D₁ Receptor: 216 nM (Ki); Human D₃ Receptor: 7.1 nM (Ki); Human D₄ Receptor: 25 nM (Ki); Human D₅ Receptor: 319 nM (Ki); Human 5-HT_2A Receptor: 5.6 nM (Ki); Human 5-HT_2C Receptor: 42.8 nM (Ki)

References

[1] Kongsamut, S., et al., Iloperidone binding to human and rat dopamine and 5-HT receptors. Eur J Pharmacol, 1996. 317(2-3): p. 417-23. DOI:10.1016/s0014-2999(96)00840-0
[2] Sainati, S.M., et al., Safety, tolerability, and effect of food on the pharmacokinetics of iloperidone (HP 873), a potential atypical antipsychotic. J Clin Pharmacol, 1995. 35(7): p. 713-20. DOI:10.1002/j.1552-4604.1995.tb04112.x
[3] Albers, L.J., A. Musenga, and M.A. Raggi, Iloperidone: a new benzisoxazole atypical antipsychotic drug. Is it novel enough to impact the crowded atypical antipsychotic market Expert Opin Investig Drugs, 2008. 17(1): p. 61-75. DOI:10.1517/13543784.17.1.61