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| | Iloperidone (hydrochloride) Basic information |
| | Iloperidone (hydrochloride) Chemical Properties |
| storage temp. | Store at -20°C | | solubility | Soluble in DMSO | | form | Powder |
| | Iloperidone (hydrochloride) Usage And Synthesis |
| 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 | Iloperidone hydrochloride is eliminated slowly, with a mean t1/2 of 13.5 to 14.0 hours. Coadministration with food did not significantly affect AUC, tmax, or Cmax. These results indicate that the rate of iloperidone's absorption is decreased, but the overall bioavailability is unchanged, when the drug is taken with food. Orthostatic hypotension, dizziness, and somnolence were the most commonly reported adverse events[2].
| | IC 50 | Rat D2 Receptor: 54 nM (Ki); Rat 5-HT2 Receptor: 3.1 nM (Ki); Rat D1 Receptor: 546 nM (Ki); Rat 5-HT1A 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-HT2A Receptor: 5.6 nM (Ki); Human 5-HT2C 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 |
| | Iloperidone (hydrochloride) Preparation Products And Raw materials |
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