Home Neuronal Signaling 5-HT Receptor agonist Aripiprazole For research use only.

Aripiprazole

Synonyms: OPC-14597

Aripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.

Aripiprazole Chemical Structure

Aripiprazole Chemical Structure

CAS No. 129722-12-9

Purity & Quality Control

Aripiprazole Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

Biological Activity

Description Aripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.
Targets
5-HT1A [1]
4.2 nM(Ki)
In vitro
In vitro Aripiprazole binds with high affinity to both the G protein-coupled and uncoupled states of receptors. Aripiprazole potently activates D2 receptor-mediated inhibition of cAMP accumulation. [1] Aripiprazole has highest affinity for h5-HT(2B)-, hD(2L)-, and hD(3)-dopamine receptors, but also has significant affinity (5-30 nM) for several other 5-HT receptors (5-HT(1A), 5-HT(2A), 5-HT(7)), as well as alpha(1A)-adrenergic and hH(1)-histamine receptors. Aripiprazole has less affinity (30-200 nM) for other G protein-coupled receptors, including the 5-HT(1D), 5-HT(2C), alpha(1B)-, alpha(2A)-, alpha(2B)-, alpha(2C)-, beta(1)-, and beta(2)-adrenergic, and H(3)-histamine receptors. Aripiprazole is an inverse agonist at 5-HT(2B) receptors and displays partial agonist actions at 5-HT(2A), 5-HT(2C), D(3), and D(4) receptors. [2]
In Vivo
In vivo Aripiprazole reduces extracellular 5-HIAA concentrations in the medial prefrontal cortex and striatum of drug-naive rats, but not in chronic Aripiprazole-pretreated rats. [3] Aripiprazole, 0.1 mg/kg and 0.3 mg/kg, significantly increases dopamine release in the hippocampus of rats. Aripiprazole, 0.3 mg/kg, slightly but significantly increases dopamine release in the medial prefrontal cortex but not in the nucleus accumbens. Aripiprazole, 3.0 mg/kg and 10 mg/kg, significantly decreases dopamine release in the nucleus accumbens but not the medical prefrontal cortex. Aripiprazole, 0.3 mg/kg, transiently potentiates haloperidol (0.1 mg/kg)-induced dopamine release in the medial prefrontal cortex but inhibited that in the nucleus accumbens. [4]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06060886 Not yet recruiting
Schizophrenia|Treatment-resistant Schizophrenia|Side Effect|Lipid Metabolism Disorders|Diabetes|NAFLD|Psychosis
Consorcio Centro de Investigación Biomédica en Red (CIBER)|Instituto de Salud Carlos III
 November 1 2023 Phase 4
NCT05322031 Unknown status
Schizophrenia|Myelin Degeneration|Cognition Disorder
Fondazione IRCCS Ca'' Granda Ospedale Maggiore Policlinico
 January 1 2022 Phase 4
NCT04907279 Unknown status
Schizophrenia|Schizo Affective Disorder|Bipolar I Disorder
Otsuka Canada Pharmaceutical Inc.|Lundbeck Canada Inc.
 November 1 2021 --
NCT04030143 Completed
Schizophrenia|Bipolar I Disorder
Otsuka Pharmaceutical Development & Commercialization Inc.
 August 1 2019 Phase 1|Phase 2
NCT03881449 Unknown status
Schizophrenia|Major Depressive Disorder|Bi-Polar Disorder|Schizo Affective Disorder
Durham VA Medical Center|Otsuka Pharmaceutical Development and Commercialization Inc.
 April 4 2019 Phase 4
NCT03854409 Completed
Schizophrenia|Bipolar I Disorder
Otsuka Pharmaceutical Development & Commercialization Inc.|PRA Health Sciences|H. Lundbeck A/S
 January 31 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 448.39 Formula

C23H27Cl2N3O2
CAS No. 129722-12-9 SDF Download Aripiprazole SDF
Smiles C1CC(=O)NC2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 90 mg/mL ( (200.71 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : 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 Aripiprazole | Aripiprazole ic50 | Aripiprazole price | Aripiprazole cost | Aripiprazole solubility dmso | Aripiprazole purchase | Aripiprazole manufacturer | Aripiprazole research buy | Aripiprazole order | Aripiprazole mouse | Aripiprazole chemical structure | Aripiprazole mw | Aripiprazole molecular weight | Aripiprazole datasheet | Aripiprazole supplier | Aripiprazole in vitro | Aripiprazole cell line | Aripiprazole concentration | Aripiprazole nmr