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.
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Choose Selective 5-HT Receptor Inhibitors
|Description||Aripiprazole is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.|
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.  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. 
|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.  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. |
|In vitro||DMSO||90 mg/mL (200.71 mM)|
* 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.
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02977299||Not yet recruiting||Treatment Resistant Major Depressive Disorder||Massachusetts General Hospital|Patient-Centered Outcomes Research Institute||May 2017||Phase 2|
|NCT02960763||Not yet recruiting||Treatment Resistant Depression|Major Depressive Disorder||Washington University School of Medicine|Patient-Centered Outcomes Research Institute||February 2017||Phase 4|
|NCT02955654||Not yet recruiting||Obsessive-Compulsive Disorder||Shanghai Mental Health Center||December 2016||--|
|NCT02926976||Not yet recruiting||Schizophrenia||Shanghai Mental Health Center||November 2016||--|
|NCT02918370||Recruiting||Bipolar Disorder|Alcoholism|Alcohol Abuse||University of Texas Southwestern Medical Center||November 2016||Phase 3|
|NCT02893371||Not yet recruiting||Bipolar Disorder||University of New Mexico|Patient-Centered Outcomes Research Institute|Montana State University|National Alliance on Mental Illness|CGStat LLC|Risk Benefit Statistics LLC||September 2016||--|
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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