Iloperidone
Iloperidone structure
|
Common Name | Iloperidone | ||
|---|---|---|---|---|
| CAS Number | 133454-47-4 | Molecular Weight | 426.481 | |
| Density | 1.2±0.1 g/cm3 | Boiling Point | 593.7±50.0 °C at 760 mmHg | |
| Molecular Formula | C24H27FN2O4 | Melting Point | 118-120°C | |
| MSDS | Chinese USA | Flash Point | 312.8±30.1 °C | |
| Symbol |
GHS02, GHS06, GHS08 |
Signal Word | Danger | |
|
A thorough QTc study of 3 doses of iloperidone including metabolic inhibition via CYP2D6 and/or CYP3A4 and a comparison to quetiapine and ziprasidone.
J. Clin. Psychopharmacol. 33(1) , 3-10, (2013) The potential for iloperidone, a D2/5-HT2A antipsychotic, to affect the heart rate-corrected QT interval (QTc) was assessed in the absence and presence of metabolic inhibitors in a randomized, open-label, multicenter study. QT interval prolongation by medicat... |
|
|
Long-term safety and tolerability of iloperidone: results from a 25-week, open-label extension trial.
CNS Spectr. 18(1) , 43-54, (2013) Long-term use of the atypical antipsychotic iloperidone has not been investigated at doses above 16 mg/d. This article describes safety and tolerability results from the 25-week open-label extension of a 4-week placebo- and ziprasidone-controlled clinical tri... |
|
|
Stable-isotope dilution LC-MS/MS assay for determination of iloperidone and its two major metabolites, P 88 and P 95, in human plasma: application to a bioequivalence study.
Bioanalysis 5(6) , 669-86, (2013) Iloperidone is a novel antipsychotic drug with high affinity for serotonin and D(2) dopamine receptors. A sensitive and rapid isotope dilution LC-MS/MS method has been developed for the simultaneous determination of iloperidone and its two major metabolites i... |
|
|
Role of α1 adrenergic antagonism in the mechanism of action of iloperidone: reducing extrapyramidal symptoms.
CNS Spectr. 18(6) , 285-8, (2013) The low incidence of extrapyramidal side effects associated with the atypical antipsychotic iloperidone may be linked to its unique binding profile of high affinity antagonism of both α1 adrenergic receptors and serotonin 2A receptors. |
|
|
Iloperidone: A new drug for the treatment of schizophrenia.
Am. J. Health Syst. Pharm. 68(4) , 301-8, (2011) The pharmacology, pharmacokinetics, pharmacogenomics, clinical efficacy, and safety and tolerability profile of iloperidone for the treatment of schizophrenia are reviewed.Iloperidone is an atypical antipsychotic that recently received marketing approval from... |
|
|
Iloperidone for the Management of Adults with Schizophrenia
Clin. Ther. 33(3) , 330-45, (2011) Background Iloperidone is a second-generation antipsychotic drug approved in May 2009 by the US Food and Drug Administration (FDA) for the acute treatment of schizophrenia in adults. It is a piperidinyl-benzisoxazole derivative with mixed serotonin (5HT2A) an... |
|
|
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. Clin. Exp. 27(1) , 24-32, (2012) The efficacy and tolerability characteristics of an antipsychotic are difficult to determine from a single registration study. We thus conducted an analysis that assessed key efficacy and tolerability outcomes post hoc from four pooled short-term (4-6 weeks) ... |
|
|
Scaffold hopping for identification of novel D(2) antagonist based on 3D pharmacophore modelling of illoperidone analogs.
Mol. Divers. 16(2) , 367-75, (2012) The dopamine D(2) receptor is involved in the etiology of a number of disorders, such as Parkinson's disease, Huntington's Chorea, tardive dyskinesia and schizophrenia. Antagonism of D(2) receptors is implicated in the treatment of various psychiatric disorde... |
|
|
Simultaneous determination of iloperidone and its two active metabolites in human plasma by liquid chromatography–tandem mass spectrometry: Application to a pharmacokinetic study
J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 928 , 52-7, (2013) • An LC/MS/MS method for simultaneous assay iloperidone and its metabolites in human plasma. • The method has an LLOQ of 10pg/mL for iloperidone and P88, and 50pg/mL for P95. • Liquid–liquid extraction is developed in sample preparation. • The validated metho... |
|
|
Angioedema occurring in patient prescribed iloperidone and haloperidol: a cross-sensitivity reaction to antipsychotics from different chemical classes.
J. Neuropsychiatry Clin. Neurosci. 24(2) , E40-1, (2012)
|