REVIEW An atypical antipsychotic for the treatment of schizophrenia. Iloperidone has been shown to act as an antagonist at all tested receptors. It exhibits high (nM) affinity to serotonin 5HT2A (Ki value of 5,2 nM), dopamine D2 (6,3 nM) and D3 (7,1 nM), moderate affinity for dopamine D4 (25 nM), serotonin 5HT6 (43 nM), 5HT7 (22 nM) and noradrenaline a1 receptors (36 nM), and low affinity for the serotonin 5HT1A (168 nM), dopamine D1 and histamine H1 receptors.
REFERENCES
[1]
Vigneault P, Pilote S, Patoine D, Simard C, Drolet B (2012). Iloperidone (Fanapt®), a novel atypical antipsychotic, is a potent HERG blocker and delays cardiac ventricular repolarization at clinically relevant concentration. Pharmacol Res. 66(1):60-5. PMID 22465688.
[2]
Citrome L, Meng X, Hochfeld M, Stahl SM (2012). Efficacy of iloperidone in the short-term treatment of schizophrenia: a post hoc analysis of pooled patient data from four phase III, placebo- and active-controlled trials. Hum Psychopharmacol. 27(1):24-32. PMID 22161738.
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