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Aripiprazole 5-HT Receptor agonist

Cat.No.S1975

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

Batch: Purity: 99.96%
99.96

Solubility

In vitro
Batch:

DMSO : 90 mg/mL (200.71 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 448.39 Formula

C23H27Cl2N3O2

Storage (From the date of receipt)
CAS No. 129722-12-9 Download SDF Storage of Stock Solutions

Synonyms OPC-14597 SMILES C1CC(=O)NC2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl

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Mechanism of Action

Targets/IC50/Ki
5-HT1A
4.2 nM(Ki)
In vitro
Aripiprazole binds with high affinity to both the G protein-coupled and uncoupled states of receptors. This compound potently activates D2 receptor-mediated inhibition of cAMP accumulation. It 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. This chemical 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. It 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.
In vivo
Aripiprazole reduces extracellular 5-HIAA concentrations in the medial prefrontal cortex and striatum of drug-naive rats, but not in chronic this compound-pretreated rats. This compound, 0.1 mg/kg and 0.3 mg/kg, significantly increases dopamine release in the hippocampus of rats. This chemical, 0.3 mg/kg, slightly but significantly increases dopamine release in the medial prefrontal cortex but not in the nucleus accumbens. This compound, 3.0 mg/kg and 10 mg/kg, significantly decreases dopamine release in the nucleus accumbens but not the medical prefrontal cortex. This chemical, 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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/15189766/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-07-31)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06969755 RECRUITING
Schizophenia Disorder
Northwell Health
2024-09-04 PHASE4
NCT06433635 ACTIVE_NOT_RECRUITING
Bipolar I Disorder; Depression
Massachusetts General Hospital
2024-10-01 PHASE4
NCT07483294 RECRUITING
Psychosis; Acute
Northwell Health
2025-11-01 PHASE4
NCT07714213 NOT_YET_RECRUITING
Post-acute Infectious Syndrome (PAIS); Post-COVID-19 Condition (PCC or Long COVID)
Christiana Franke
2026-10-01 PHASE2
NCT07047651 ACTIVE_NOT_RECRUITING
Treatment Resistant Schizophrenia; Treatment Resistant Bipolar Disorder
Dr. Stavroula Rakitzi
2025-06-04 PHASE4
NCT07565428 RECRUITING
Negative Symptoms of Schizophrenia
Minerva Neurosciences
2026-04-23 PHASE3

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