Iloperidone

Synonyms: HP873

Iloperidone (HP873) is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.

Iloperidone Chemical Structure

Iloperidone Chemical Structure

CAS No. 133454-47-4

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Iloperidone Related Products

Biological Activity

Description Iloperidone (HP873) is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.
Targets
5-HT [1]
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05344365 Withdrawn
Parkinson Disease Psychosis
Vanda Pharmaceuticals
June 2022 Phase 2
NCT04969211 Completed
Healthy
Vanda Pharmaceuticals
June 30 2021 Phase 1
NCT04712734 Completed
Schizophrenia
Vanda Pharmaceuticals
January 13 2021 Phase 1
NCT01495169 Completed
Safety and Tolerability of Iloperidone
Vanda Pharmaceuticals
October 2011 Phase 1
NCT01529294 Completed
Hepatic Impairment
Novartis Pharmaceuticals|Novartis
August 2010 Phase 1

Chemical Information & Solubility

Molecular Weight 426.48 Formula

C24H27FN2O4

CAS No. 133454-47-4 SDF Download Iloperidone SDF
Smiles CC(=O)C1=CC(=C(C=C1)OCCCN2CCC(CC2)C3=NOC4=C3C=CC(=C4)F)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 27 mg/mL ( (63.3 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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