Iloperidone - CAS 133454-47-4
Catalog number: 133454-47-4
Category: Inhibitor
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Molecular Formula:
C24H27FN2O4
Molecular Weight:
426.48
COA:
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Targets:
5-HT Receptor
Description:
Iloperidone displays high affinity (Ki < 10 nM) for norepinephrine alpha(1)-adrenoceptors, dopamine D(3) and serotonin 5-HT(2A) receptors.
Purity:
>98%
Synonyms:
HP873; HP 873; HP-873
MSDS:
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InChIKey:
XMXHEBAFVSFQEX-UHFFFAOYSA-N
InChI:
InChI=1S/C24H27FN2O4/c1-16(28)18-4-7-21(23(14-18)29-2)30-13-3-10-27-11-8-17(9-12-27)24-20-6-5-19(25)15-22(20)31-26-24/h4-7,14-15,17H,3,8-13H2,1-2H3
Canonical SMILES:
CC(=O)C1=CC(=C(C=C1)OCCCN2CCC(CC2)C3=NOC4=C3C=CC(=C4)F)OC
1.A placebo-controlled crossover study of iloperidone augmentation for residual anger and irritability in major depressive disorder.
Ionescu DF1, Fava M2, Kim DJ3, Baer L1, Shelton RC4, Cusin C1. Ther Adv Psychopharmacol. 2016 Feb;6(1):4-12. doi: 10.1177/2045125315618621.
BACKGROUND: Even when patients experience remission with antidepressants, many continue to report anger attacks and excessive irritability despite continued treatment. Iloperidone antagonizes 5-HT-2a, D2, and alpha-1 receptors, which can have anti-aggressive effects. We examined iloperidone's safety and efficacy as an augmentation agent in outpatients with partially remitted major depressive disorder (MDD) with residual symptoms of anger and irritability.
2.Effects of iloperidone, combined with desipramine, on alcohol drinking in the Syrian golden hamster.
Khokhar JY1, Green AI2. Neuropharmacology. 2016 Jan 12;105:25-34. doi: 10.1016/j.neuropharm.2016.01.017. [Epub ahead of print]
Alcohol use disorder in patients with schizophrenia dramatically worsens their clinical course, and few treatment options are available. Clozapine appears to reduce alcohol use in these patients, but its toxicity limits its use. To create a safer clozapine-like drug, we tested whether the antipsychotic iloperidone, a drug that combines a weak dopamine D2 receptor blockade and a potent norepinephrine alpha-2 receptor blockade would reduce alcohol drinking, and whether its effect on alcohol drinking could be increased if combined with an agent to facilitate norepinephrine activity. Syrian golden hamsters (useful animal model for screening drugs that reduce alcohol drinking in patients with schizophrenia) were given free access to water and alcohol (15% v/v) until stable drinking was established. Animals (n = 6-7/group), matched according to alcohol intake, were treated daily with each drug (iloperidone; clozapine; haloperidol; desipramine [norepinephrine reuptake inhibitor]; with idazoxan [norepinephrine alpha-2 receptor antagonist]) or with a two-drug (iloperidone + desipramine; iloperidone + idazoxan) combination for 14 days.
3.Flow Synthesis in Hot Water: Synthesis of the Atypical Antipsychotic Iloperidone.
Hartwig J1, Kirschning A2. Chemistry. 2016 Feb;22(9):3044-52. doi: 10.1002/chem.201504409. Epub 2016 Jan 25.
Inductively heated steel reactors continuously perform organic transformations in water under high temperature conditions, utilizing the unique physiochemical properties of water at subcritical conditions. We demonstrated the power of this set-up in the continuous synthesis of the atypical antipsychotic drug iloperidone, in which we performed four out of five steps under aqueous conditions.
4.Iloperidone-induced ejaculatory dysfunction: A case series.
Ravani NN1, Katke PH2. Indian J Psychiatry. 2016 Jan-Mar;58(1):87-9. doi: 10.4103/0019-5545.174392.
Disorders of ejaculation are the consequences of surgical procedures and with the use of various drugs. Until date, most drugs reported to induce ejaculatory dysfunctions such as retrograde ejaculation or dry orgasms share the capacity to significantly antagonize alpha 1-adrenergic receptor. Iloperidone, a new dopamine Type 2 and serotonin Type 2A antagonist similar to risperidone, provides better efficacy with lesser extra-pyramidal side effects. In addition, it also antagonize alpha 1-adrenergic receptor and alpha-2C receptors. Limited data is available for iloperidone-induced ejaculation dysfunction. This article features five schizophrenic patients which developed retrograde ejaculation during treatment with iloperidone. The ejaculatory dysfunction following treatment with iloperidone could be postulated due to blocking of alpha 1-adrenergic receptor.
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CAS 133454-47-4 Iloperidone

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