Home Neuronal Signaling 5-HT Receptor inhibitor Iloperidone For research use only.

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

Purity & Quality Control

Iloperidone Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

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NCT05344365 Withdrawn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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Iloperidone | Iloperidone supplier | purchase Iloperidone | Iloperidone cost | Iloperidone manufacturer | order Iloperidone | Iloperidone distributor