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Aripiprazole

Catalog No. T1566   CAS 129722-12-9
Synonyms: OPC-14597

Aripiprazole (OPC-14597) is an antipsychotic agent that is structurally related to piperazines and quinolones. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A.

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Aripiprazole Chemical Structure
Aripiprazole, CAS 129722-12-9
Pack Size Availability Price/USD Quantity
100 mg In stock $ 58.00
200 mg In stock $ 76.00
500 mg In stock $ 103.00
1 g In stock $ 135.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.53%
Purity: 99.43%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Aripiprazole (OPC-14597) is an antipsychotic agent that is structurally related to piperazines and quinolones. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A.
Targets&IC50 5-HT1A:4.2 nM(Ki)
In vitro Aripiprazole administration at doses of 0.1 mg/kg and 0.3 mg/kg significantly increased dopamine release in the hippocampus of rats. A dose of 0.3 mg/kg slightly, yet significantly, enhanced dopamine release in the medial prefrontal cortex, without affecting dopamine levels in the nucleus accumbens. Additionally, 0.3 mg/kg of Aripiprazole transiently amplified dopamine release in the medial prefrontal cortex induced by 0.1 mg/kg of Haloperidol, but it inhibited dopamine release in the nucleus accumbens. Higher doses of 3.0 mg/kg and 10 mg/kg distinctly decreased dopamine release in the nucleus accumbens, without impacting the medial prefrontal cortex. Aripiprazole reduced the extracellular concentration of 5-HIAA in the medial prefrontal cortex and striatum of drug-naïve rats, but this effect was not observed in rats with chronic Aripiprazole pretreatment.
In vivo Aripiprazole exhibits the highest affinity for h5-HT(2B), hD(2L), and hD(3) dopamine receptors but also demonstrates significant affinity (5-30 nM) for various other 5-HT receptors (5-HT(1A), 5-HT(2A), 5-HT(7)), as well as α(1A)-adrenergic and hH(1)-histamine receptors. Aripiprazole acts as an inverse agonist at the 5-HT(2B) receptor and displays partial agonist activity at 5-HT(2A), 5-HT(2C), D(3), and D(4) receptors. It binds with high affinity to both G protein-coupled and uncoupled states of these receptors. Additionally, Aripiprazole effectively activates D2 receptor-mediated inhibition of cAMP accumulation.
Synonyms OPC-14597
Molecular Weight 448.39
Formula C23H27Cl2N3O2
CAS No. 129722-12-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 44.8 mg/mL (100 mM)

TargetMolReferences and Literature

1. Burris KD, et al. J Pharmacol Exp Ther, 2002, 302(1), 381-389. 2. Shapiro DA, et al. Neuropsychopharmacology, 2003, 28(8), 1400-1411. 3. Keller RK, et al. Biochem Biophys Res Commun, 1999, 266(2), 560-563. 4. Li Z, et al. Eur J Pharmacol, 2004, 493(1-3), 75-83. 5. Xu P, Huang S, Zhang H, et al. Structural insights into the lipid and ligand regulation of serotonin receptors[J]. Nature. 2021, 592(7854): 469-473.

TargetMolCitations

1. Sharma K, Dev K K.The Effects of Antipsychotics in Experimental Models of Krabbe Disease.Biomedicines.2023, 11(5): 1313. 2. Xu Z, Guo L, Yu J, et al.Ligand recognition and G protein coupling of trace amine receptor TAAR1.Nature.2023: 1-3.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library FDA-Approved & Pharmacopeia Drug Library ReFRAME Related Library Neurotransmitter Receptor Compound Library Angiogenesis related Compound Library Drug-induced Liver Injury (DILI) Compound Library Inhibitor Library

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Keywords

Aripiprazole 129722-12-9 GPCR/G Protein Neuroscience 5-HT Receptor Inhibitor 5-hydroxytryptamine Receptor inhibit Antipsychotic Serotonin OPC14597 Prefrontal cortex OPC-14597 Dopamine Hippocampus OPC 14597 CHO-D2L cells COVID19 Serotonin Receptor inhibitor

 

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