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

Key Properties

• CAS Number: 129722-12-9
• MW: 448.40
• Purity: >98%
• Formula: C₂₃H₂₇Cl₂N₃O₂
• SMILES: O(CCCCN1CCN(CC1)C2=C(Cl)C(Cl)=CC=C2)C=3C=C4C(=CC3)CCC(=O)N4
• Target: Monoamine receptor
• Solubility: Soluble in DMSO (up to 30 mg/ml) or in Ethanol (up to 5 mg/ml with warming).

Bioactivity

• 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.
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• 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.
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Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

OPC-14597

Compound Identifiers

PubChem CID

60795