Aripiprazole

SKU: orb1308154

Description

Aripiprazole is a piperazine-quinolone derivative antipsychotic research compound. It acts as a partial agonist at 5-HT1A and D2 receptors, with post-synaptic D2 antagonism and 5-HT2A receptor antagonism. This pharmacological profile makes it a key tool for in vitro and in vivo studies of schizophrenia, bipolar disorder, and neurotransmitter systems.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	129722-12-9
MW	448.39
Purity	99.62%
Formula	C₂₃H₂₇Cl₂N₃O₂
SMILES	O(CCCCN1CCN(CC1)C2=C(Cl)C(Cl)=CC=C2)C=3C=C4C(=CC3)CCC(=O)N4
Target	Dopamine Receptor,5-HT Receptor
Solubility	DMSO:51 mg/mL (113.74 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.46 mM)

Bioactivity

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Target IC50	5-HT1A:4.2 nM(Ki)
In Vivo	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. Read more...
In Vitro	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. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Hippocampus, Inhibitor, inhibit, OPC 14597, OPC14597, OPC-14597, Dopamine, CHO-D2L cells, COVID19, 5HTReceptor, 5HT Receptor, 5-hydroxytryptamine Receptor, 5-HT1A, 5-HT Receptor, Aripiprazole, Antipsychotic, Prefrontal cortex, Serotonin Receptor, Serotonin

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Compound Identifiers

PubChem CID

60795 ↗

Key Properties

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No computed properties available.

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Aripiprazole (orb1308154)

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Aripiprazole

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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