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Iloperidone

Catalog No. T1539   CAS 133454-47-4
Synonyms: Inhibitor, 5-hydroxytryptamine Receptor, atypical, Dopamine Receptor, Serotonin Receptor, inhibit, Iloperidone, 5-HT Receptor, symptoms, HP873, HP-873, antipsychotic, schizophrenia, HP 873

Iloperidone is an atypical antipsychotic agent that is used for treatment of schizophrenia.

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Iloperidone, CAS 133454-47-4
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Purity: 98%
Biological Description
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Storage & Solubility Information
Description Iloperidone is an atypical antipsychotic agent that is used for treatment of schizophrenia.
Targets&IC50 dopamine D3 receptor:7.1 nM(ki), dopamine D4 receptor:25 nM(ki)
In vitro Iloperidone displays high affinity (Ki < 10 nM) for norepinephrine alpha(1)-adrenoceptors, dopamine D(3) and serotonin 5-HT(2A) receptors. [1] Iloperidone displays higher affinity for the dopamine D3 receptor (Ki = 7.1 nM) than for the dopamine D4 receptor (Ki = 25 nM). Iloperidone displays high affinity for the 5-HT6 and 5-HT7 receptors (Ki = 42.7 nM and 21.6 nM, respectively), and is found to have higher affinity for the 5-HT2A (Ki = 5.6 nM) than for the 5-HT2C receptor (Ki = 42.8 nM). [2] Iloperidone significantly increases dopa accumulation, an index of dopamine turnover in response to D2 receptor blockade, at doses from 0.3 mg/kg to 10 mg/kg i.p. in the striatum and from 1 mg/kg to 10 mg/kg in the nucleus accumbens. [3]
In vivo Iloperidone exerts behavioral effects in pharmacological rats models of disrupted sensorimotor gating consistent with "atypical" antipsychotics, mediated by antagonism of dopaminergic and noradrenergic receptors. Iloperidone (1 and 3 mg/kg) prevents the PPI-disruptive effects of treatment with 1 mg/kg PCP. Iloperidone (0.3 mg/kg) prevents cirazoline-induced PPI deficits, independent of its effects on startle magnitude. [4] Iloperidone (10 mg/kg) and Melperone (10 mg/kg) produce an equivalent or a smaller increase in DA release in the nucleus accumbens (NAC) of rats, respectively, compared to the mPFC, whereas none of them increase acetylcholine (ACh) release in the NAC. [5]
Kinase Assay Immunoblotting for the mTOR kinase assay: HEK293 cells are plated at 2-2.5&times;105 cells/well of a 12-well plate and serum-starved for 24 hours in DMEM. Cells are treated with increasing concentrations of Rapamycin (0.05-50 nM) for 15 minutes at 37 °C. Serum is added to a final concentration of 20% for 30 minutes at 37 °C. Cells are lysed, and cell lysates are separated by SDS-PAGE. Resolved proteins are transferred to a polyvinylidene difluoride membrane and immunoblotted with a phosphospecific primary antibody against Thr-389 of p70 S6 kinase. Data are analyzed using ImageQuant and KaleidaGr
Synonyms Inhibitor, 5-hydroxytryptamine Receptor, atypical, Dopamine Receptor, Serotonin Receptor, inhibit, Iloperidone, 5-HT Receptor, symptoms, HP873, HP-873, antipsychotic, schizophrenia, HP 873
Molecular Weight 426.488
Formula C24H27FN2O4
CAS No. 133454-47-4

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: 4 mg/mL (9.37 mM)

H2O: <1 mg/mL

DMSO: 26 mg/mL (61 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Danek P J, Kuban W, Daniel W A. The Effect of Chronic Iloperidone Treatment on Cytochrome P450 Expression and Activity in the Rat Liver: Involvement of Neuroendocrine Mechanisms. International Journal of Molecular Sciences. 2021, 22(16): 8447. 1. Kalkman HO, et al. Neuropsychopharmacology, 2001, 25(6), 904-914. 2. Qian H Y, Zhou F, Wu R, et al. Metformin Attenuates Bone Cancer Pain by Reducing TRPV1 and ASIC3 Expression. Frontiers in Pharmacology. 2021: 1924. 2. Kongsamut S, et al. Eur J Pharmacol, 1996, 317(2-3), 417-423. 3. Danek P J, Wójcikowski J, Daniel W A. Asenapine and iloperidone decrease the expression of major cytochrome P450 enzymes CYP1A2 and CYP3A4 in human hepatocytes. A significance for drug-drug interactions during combined therapy. Toxicology and Applied Pharmacology. 2020, 406: 115239 3. Szczepanik AM, et al. J Pharmacol Exp Ther, 1996, 278(2), 913-920. 4. Barr AM, et al. Neuropharmacology, 2006, 51(3), 457-465. 5. Ichikawa J, et al. Brain Res, 2002, 956(2), 349-357. 6. Danek P J, Wójcikowski J, Daniel W A. Asenapine and iloperidone decrease the expression of major cytochrome P450 enzymes CYP1A2 and CYP3A4 in human hepatocytes. A significance for drug-drug interactions during combined therapy[J]. Toxicology and Applied Pharmacology. 2020, 406: 115239.

Related compound libraries

This product is contained In the following compound libraries:
GPCR Compound Library Anti-Cardiovascular Disease Compound Library Coagulation and Anticoagulation Compound Library Neurotransmitter Receptor Compound Library Endocrinology-Hormone Compound Library Anti-Parkinson's Disease Compound Library Inhibitor Library Drug-induced Liver Injury (DILI) Compound Library Anti-Alzheimer's Disease Compound Library Fluorochemical Library

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