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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

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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

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Molarity Calculator

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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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