Aripiprazole

Catalog No.S1975 Synonyms: OPC-14597

For research use only.

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

CAS No. 129722-12-9

Selleck's Aripiprazole has been cited by 7 Publications

2 Customer Reviews

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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

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 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]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 90 mg/mL
(200.71 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 448.39
Formula

C23H27Cl2N3O2

CAS No. 129722-12-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(=O)NC2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl

In vivo Formulation Calculator (Clear solution)

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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.

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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04907279 Not yet recruiting Drug: Aripiprazole Once-Monthly (AOM) Schizophrenia|Schizo Affective Disorder|Bipolar I Disorder Otsuka Canada Pharmaceutical Inc.|Lundbeck Canada Inc. June 2021 --
NCT04030143 Completed Drug: Aripiprazole Schizophrenia|Bipolar I Disorder Otsuka Pharmaceutical Development & Commercialization Inc.|PRA Health Sciences July 31 2019 Phase 1|Phase 2
NCT03881449 Active not recruiting Combination Product: ABILIFY MYCITE 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 Drug: Aripiprazole Schizophrenia|Bipolar I Disorder Otsuka Pharmaceutical Development & Commercialization Inc.|PRA Health Sciences|H. Lundbeck A/S January 31 2019 Phase 1
NCT03342963 Completed Drug: ASC-01|Drug: Aripiprazole and sertraline Healthy Male Adults Otsuka Pharmaceutical Co. Ltd. November 21 2017 Phase 1
NCT03130478 Completed -- Schizophrenia Otsuka Pharmaceutical Europe Ltd July 18 2017 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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