Aripiprazole
Catalog No.S1975 Synonyms: OPC-14597
Molecular Weight(MW): 448.39
Aripiprazole is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.
Cited by 3 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 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 |
Bio Calculators
Molarity Calculator
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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 | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03874494 | Not yet recruiting | Schizophrenia | Otsuka Beijing Research Institute | April 30 2019 | Phase 3 |
| NCT03874494 | Not yet recruiting | Schizophrenia | Otsuka Beijing Research Institute | April 30 2019 | Phase 3 |
| NCT03485417 | Not yet recruiting | Stimulant Use With Stimulant-Induced Psychotic Disorder (Diagnosis)|Schizophrenia and Related Disorders|Stimulant Dependence|Stimulant Abuse|Pharmacotherapy | The University of Hong Kong|Queen Mary Hospital Hong Kong|North District Hospital | April 1 2019 | Phase 2|Phase 3 |
| NCT03485417 | Not yet recruiting | Stimulant Use With Stimulant-Induced Psychotic Disorder (Diagnosis)|Schizophrenia and Related Disorders|Stimulant Dependence|Stimulant Abuse|Pharmacotherapy | The University of Hong Kong|Queen Mary Hospital Hong Kong|North District Hospital | April 1 2019 | Phase 2|Phase 3 |
| NCT03854409 | Recruiting | Schizophrenia|Bipolar I Disorder | Otsuka Pharmaceutical Development & Commercialization Inc.|PRA Health Sciences|H. Lundbeck A/S | January 31 2019 | Phase 1 |
| NCT03854409 | Recruiting | Schizophrenia|Bipolar I Disorder | Otsuka Pharmaceutical Development & Commercialization Inc.|PRA Health Sciences|H. Lundbeck A/S | January 31 2019 | Phase 1 |
Tech Support
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