Catalog No.S1483 Synonyms: HP873
Molecular Weight(MW): 426.48
Iloperidone is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.
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|Description||Iloperidone is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.|
Iloperidone displays high affinity (Ki < 10 nM) for norepinephrine alpha(1)-adrenoceptors, dopamine D(3) and serotonin 5-HT(2A) receptors.  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).  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. 
|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.  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. |
-  Kalkman HO, et al. Neuropsychopharmacology, 2001, 25(6), 904-914.
-  Kongsamut S, et al. Eur J Pharmacol, 1996, 317(2-3), 417-423.
-  Szczepanik AM, et al. J Pharmacol Exp Ther, 1996, 278(2), 913-920.
|In vitro||DMSO||27 mg/mL (63.3 mM)|
|Ethanol||4 mg/mL (9.37 mM)|
|In vivo||Add solvents individually and in order:
2% DMSO+40% PEG 300+dd H2O
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02600741||Recruiting||Schizophrenia||Janssen Scientific Affairs, LLC||July 2015||Phase 4|
|NCT02453893||Recruiting||Schizophrenia||CSPC ZhongQi Pharmaceutical Technology Co., Ltd.||November 2013||Phase 3|
|NCT01917318||Completed||Post Traumatic Stress Disorder||University of Colorado, Denver|Novartis Pharmaceuticals||July 2013||Phase 2|
|NCT01498770||Recruiting||Bipolar Disorder||Merck Sharp & Dohme Corp.||April 2013||--|
|NCT01920802||Completed||Healthy||New York State Psychiatric Institute|Novartis Pharmaceuticals||November 2012||Phase 4|
|NCT01623713||Completed||Schizophrenia|Iloperidone|Efficacy||Jiangsu Hansoh Pharmaceutical Co., Ltd.||June 2012||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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