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: 129722-12-9

Selleck's Aripiprazole has been cited by 12 Publications

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Purity & Quality Control

Batch: Purity: 99.96%
99.96

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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
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 Recruiting Schizophrenia|Myelin Degeneration|Cognition Disorder Fondazione IRCCS Ca'' Granda Ospedale Maggiore Policlinico January 1 2022 Phase 4
NCT04907279 Recruiting 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 lnformation & 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


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In vivo
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