Aripiprazole
For research use only.
Catalog No.S1975 Synonyms: OPC-14597
4 publications
CAS No. 129722-12-9
Aripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.
Selleck's Aripiprazole has been cited by 4 publications
2 Customer Reviews
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Olanzapine and aripiprazole differentially regulate cellular glucose uptake of PBMC. Bar graphs depict cellular glucose uptake assessed by 18F-FDG in PBMC after 72 h of stimulation with the indicated concentrations of olanzapine (Olan, A) or aripiprazole (Arip, B) relative to corresponding DMSO controls (Ctrl) and normalized to protein content. Data are depicted as mean ± SD. P-values were computed by one-way ANOVA followed by Dunnett's Multiple Comparison Test. ***P < 0.001, **P < 0.01, *P < 0.05 versus control; results were obtained from n = 4e-6 independent cell isolations measured in duplicate
J Psychiatr Res, 2017, 88:18-27 . Aripiprazole purchased from Selleck.
Olanzapine or aripiprazole stimulation of PBMC reduces mRNA expression of pro-inflammatory cytokines ex vivo. Bar graphs summarizing mRNA expression of pro-inflammatory cytokines IL-1β, IL-6 and TNF-α in PBMC after 72 h of olanzapine (Olan, 10−4 M; A) or aripiprazole (Arip; 10−5 M; B) stimulation and graphs showing mRNA levels of anti-inflammatory IL-10 and TGF-β1 after stimulation with Olan (C) or Arip (D) compared to corresponding control (Ctrl) cells. Values for controls were set as 100% in each cell preparation. Numbers of independent cell preparations for were as follows: n=4 for IL-6; n=5 for IL-10; n=6 for IL-1β, TNF-α and TGF-β1. Results are depicted as mean ± SEM. P-values were assessed by two-tailed one sample ttest; ****P < 0.0001, ***P < 0.001, **P < 0.01, *P < 0.05 versus respective control group.
J Psychiatr Res, 2018, 105:95-102. Aripiprazole purchased from Selleck.
Purity & Quality Control
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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. | ||
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| Targets |
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| 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] |
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| 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
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 |
powder in solvent |
| Synonyms | OPC-14597 |
| Smiles | C1CC(=O)NC2=C1C=CC(=C2)OCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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.
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
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Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT04030143 | Completed | Drug: Aripiprazole | Schizophrenia|Bipolar I Disorder | Otsuka Pharmaceutical Development & Commercialization Inc.|PRA Health Sciences | July 31 2019 | Phase 1 |
| 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 | -- |
| NCT02697045 | Completed | Drug: Aripiprazole 400mg LAI | Schizophrenia | Abdi İbrahim Otsuka | January 4 2017 | Phase 4 |
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.
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