Aripiprazole monohydrate

Names

[ Name ]:
Aripiprazole monohydrate

[Synonym ]:
7-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydro-2(1H)-quinolinone hydrate
7-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydrocarbostyril monohydrate
Aripiprazole monohydrate
aripiprazole hydrate
Aripiprazole hydrate
7-(4-[4-(2,3-dichloropheny)-1-piperazinyl]-butoxy)-3,4-dihydrocarbostyril monohydrate
7-(4-[4-(2,3-dichloropheny)-1-piperazinyl]-butoxy)-3,4-dihydro-2(1H)-quinolone monohydrate

Biological Activity

[Description]:

Aripiprazole (OPC-14597) monohydrate, an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole monohydrate is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole monohydrate can be used for the research of schizophrenia and COVID19[1][2][3][4].

[Related Catalog]:

Research Areas >> Infection

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT1A Receptor

5-HT2A Receptor

5-HT2B Receptor

5-HT2C Receptor

D2 Receptor

D3 Receptor

D4 Receptor

[In Vitro]

Aripiprazole monohydrate potently activates D2 receptor-mediated inhibition of cAMP accumulation[1]. Aripiprazole monohydrate shows a greater anti-inflammatory effect on TNF-α, IL-13, IL-17α and fractalkine[3].

[In Vivo]

Aripiprazole monohydrate (0-3 mg/kg, IP, daily) shows some anxiolytic properties[4]. Animal Model: WAG/Rij rats (N = 6 per dose, 6 months, administration of a mixture of tiletamine/zolazepam)[4] Dosage: 0, 0.3, 1, 3 mg/kg Administration: IP, 1 mL/kg, every day at 5 p.m. until the end of the experiments Result: Showed some anxiolytic properties with the 1 mg/kg dose being the most active.

[References]

[1]. Burris KD, et al. Aripiprazole, a novel antipsychotic, is a high-affinity partial agonist at human dopamine D2 receptors. J Pharmacol Exp Ther. 2002 Jul;302(1):381-9.

[2]. Davies MA, et al. Aripiprazole: a novel atypical antipsychotic drug with a uniquely robust pharmacology. CNS Drug Rev. 2004 Winter;10(4):317-36.

[3]. Crespo-Facorro B, et al. Aripiprazole as a Candidate Treatment of COVID-19 Identified Through Genomic Analysis. Front Pharmacol. 2021 Mar 2;12:646701.

[4]. Russo E, et al. Ameliorating effects of aripiprazole on cognitive functions and depressive-like behavior in a genetic rat model of absence epilepsy and mild-depression comorbidity. Neuropharmacology. 2013 Jan;64:371-9.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₃H₂₉Cl₂N₃O₃

[ Molecular Weight ]:
466.40100

[ Exact Mass ]:
465.15900

[ PSA ]:
57.53000

[ LogP ]:
4.88300

Synthetic Route

Click to get detail synthetic route

Related Compounds

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