The pharmacological profile of iloperidone, a novel atypical antipsychotic agent.

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Szewczak MR, Corbett R, Rush DK, Wilmot CA, Conway PG, Strupczewski JT, Cornfeldt M

The pharmacological profile of iloperidone, a novel atypical antipsychotic agent.

J Pharmacol Exp Ther. 1995 Sep;274(3):1404-13.

PubMed ID

7562515 [ View in PubMed

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Abstract

Iloperidone (1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1- piperidinyl]propoxy]-3-methoxyphenyl]ethanone) demonstrated a potent antipsychotic profile in several in vitro and in vivo animal models. Iloperidone displaced ligand binding at D2 dopamine receptors (IC50 = 0.11 microM) and displayed a high affinity for serotonin (5-HT2) receptors (IC50 = 0.011 microM) and alpha-1 receptors (IC50 = 0.00037 microM). In vivo, iloperidone antagonized apomorphine-induced climbing behavior in mice at low doses with good oral bioavailability, prevented 5-HT-induced head twitch in rats at low doses, and inhibited self-stimulation behavior in rats, pole climb avoidance in rats and continuous Sidman avoidance responding in monkeys. The latter assay also demonstrated a good duration of action. Iloperidone was substantially less active in models of extrapyramidal side effect (EPS) liability, such as preventing apomorphine-induced stereotypy and causing catalepsy in rats. In single dopamine neuron sampling studies, iloperidone demonstrated clozapine-like effects on the number of active midbrain dopamine neurons. Based on the significant increase in the open arm time seen after iloperidone treatment in the elevated plus maze assay and increased interaction score in social interaction, iloperidone may also have favorable effects in the clinic on anxiety and, possibly, negative symptoms. Clinical trials are under way of the use of iloperidone for the treatment of schizophrenia.

DrugBank Data that Cites this Article

Drugs

Iloperidone

Drug Interactions

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drugs	Interaction
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Iloperidone Thioridazine	The metabolism of Iloperidone can be decreased when combined with Thioridazine.
Iloperidone Bupropion	The metabolism of Iloperidone can be decreased when combined with Bupropion.
Iloperidone Cisapride	The metabolism of Iloperidone can be decreased when combined with Cisapride.
Iloperidone Cinacalcet	The metabolism of Iloperidone can be decreased when combined with Cinacalcet.
Iloperidone Propafenone	The metabolism of Iloperidone can be decreased when combined with Propafenone.