DGIdb - ARIPIPRAZOLE Drug Record

ARIPIPRAZOLE chembl:CHEMBL1112 Approved

Alternate Names:

OPC-31
OPC-14597
ARIPIPRAZOLE
ABILIFY MAINTENA
ABILIFY MYCITE KIT
ABILIFY MAINTENA KIT
ABILIFY
ARIPIPREX
OPC 14597
ABILITAT
OPC 31
ARIPIPRAZOL
ARIPIPRAZOLUM
pubchem.compound:60795
chembl:CHEMBL1112
rxcui:89013
drugbank:01238
chemidplus:129722-12-9

Drug Info:

Drug Class	antipsychotic agents
Year of Approval	2002
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antipsychotic agent
Drug Categories	adrenergic alpha-1 receptor antagonists
Drug Categories	adrenergic alpha-antagonists
Drug Categories	adrenergic antagonists
Drug Categories	agents producing tachycardia
Drug Categories	agents that produce hypertension
Drug Categories	anticholinergic agents
Drug Categories	antidepressive agents
Drug Categories	aripiprazole and prodrugs
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a5 substrates
Drug Categories	cytochrome p-450 cyp3a7 substrates
Drug Categories	cytochrome p-450 substrates
Drug Categories	dopamine agents
Drug Categories	dopamine agonists
Drug Categories	dopamine antagonists
Drug Categories	dopamine d2 receptor antagonists
Drug Categories	heterocyclic compounds, fused-ring
Drug Categories	histamine antagonists
Drug Categories	histamine h1 antagonists
Drug Categories	muscarinic antagonists
Drug Categories	neurotoxic agents
Drug Categories	neurotransmitter agents
Drug Categories	potential qtc-prolonging agents
Drug Categories	qtc prolonging agents
Drug Categories	qtc shortening agents
Drug Categories	serotonergic drugs shown to increase risk of serotonin syndrome
Drug Categories	serotonin 5-ht1 receptor agonists
Drug Categories	serotonin 5-ht1 receptor antagonists
Drug Categories	serotonin 5-ht2 receptor antagonists
Drug Categories	serotonin agents
Drug Categories	serotonin receptor agonists
Drug Categories	serotonin receptor antagonists

(5 More Sources)

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry
de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
Inoue et al., 1997, Aripiprazole, a novel antipsychotic drug, inhibits quinpirole-evoked GTPase activity but does not up-regulate dopamine D2 receptor following repeated treatment in the rat striatum., Eur. J. Pharmacol.
Wood et al., 2007, Aripiprazole acts as a selective dopamine D2 receptor partial agonist., Expert Opin Investig Drugs
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Hirose et al., 2005, Aripiprazole, a novel antipsychotic agent: dopamine D2 receptor partial agonist., J. Med. Invest.
Wood et al., 2006, Aripiprazole and its human metabolite are partial agonists at the human dopamine D2 receptor, but the rodent metabolite displays antagonist properties., Eur. J. Pharmacol.
Kim et al., 2006, Effects of DRD2 and CYP2D6 genotypes on delta EEG power response to aripiprazole in healthy male volunteers: a preliminary study., Hum Psychopharmacol
Arranz MJ et al., 1998, Lack of association between a polymorphism in the promoter region of the dopamine-2 receptor gene and clozapine response., Pharmacogenetics
Eum S et al., 2017, Pharmacogenetic evaluation to assess breakthrough psychosis with aripiprazole long-acting injection: a case report., BMC Psychiatry
Zhang JP et al., 2010, D2 receptor genetic variation and clinical response to antipsychotic drug treatment: a meta-analysis., Am J Psychiatry
Lawler CP et al., 1999, Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes., Neuropsychopharmacology
Batra S, 1976, Unconjugated estradiol in the myometrium of pregnancy., Endocrinology
Ohara K et al., 1998, Functional polymorphism of -141C Ins/Del in the dopamine D2 receptor gene promoter and schizophrenia., Psychiatry Res
Li T et al., 1998, Case-control, haplotype relative risk and transmission disequilibrium analysis of a dopamine D2 receptor functional promoter polymorphism in schizophrenia., Schizophr Res
Huertas E et al., 2010, The D2 dopamine receptor gene variant C957T affects human fear conditioning and aversive priming., Genes Brain Behav
Hirvonen MM et al., 2009, C957T polymorphism of dopamine D2 receptor gene affects striatal DRD2 in vivo availability by changing the receptor affinity., Synapse
Betcheva ET et al., 2009, Case-control association study of 59 candidate genes reveals the DRD2 SNP rs6277 (C957T) as the only susceptibility factor for schizophrenia in the Bulgarian population., J Hum Genet
Shen YC et al., 2009, Effects of DRD2/ANKK1 gene variations and clinical factors on aripiprazole efficacy in schizophrenic patients., J Psychiatr Res
Crettol S et al., 2008, Association of dopamine and opioid receptor genetic polymorphisms with response to methadone maintenance treatment., Prog Neuropsychopharmacol Biol Psychiatry
Allen NC et al., 2008, Systematic meta-analyses and field synopsis of genetic association studies in schizophrenia: the SzGene database., Nat Genet
Xing Q et al., 2007, The relationship between the therapeutic response to risperidone and the dopamine D2 receptor polymorphism in Chinese schizophrenia patients., Int J Neuropsychopharmacol
Hoenicka J et al., 2006, C957T DRD2 polymorphism is associated with schizophrenia in Spanish patients., Acta Psychiatr Scand
Hänninen K et al., 2006, Association between the C957T polymorphism of the dopamine D2 receptor gene and schizophrenia., Neurosci Lett
Lencz et al., 2006, DRD2 promoter region variation as a predictor of sustained response to antipsychotic medication in first-episode schizophrenia patients., Am J Psychiatry
Lerman C et al., 2006, Role of functional genetic variation in the dopamine D2 receptor (DRD2) in response to bupropion and nicotine replacement therapy for tobacco dependence: results of two randomized clinical trials., Neuropsychopharmacology
Hwang R et al., 2005, Association study of 12 polymorphisms spanning the dopamine D(2) receptor gene and clozapine treatment response in two treatment refractory/intolerant populations., Psychopharmacology (Berl)
Wu et al., 2005, Response to chlorpromazine treatment may be associated with polymorphisms of the DRD2 gene in Chinese schizophrenic patients., Neurosci. Lett.
Lawford BR et al., 2005, The C/C genotype of the C957T polymorphism of the dopamine D2 receptor is associated with schizophrenia., Schizophr Res
Yamanouchi Y et al., 2003, Effect of DRD2, 5-HT2A, and COMT genes on antipsychotic response to risperidone., Pharmacogenomics J
Li T et al., 2002, Allelic association analysis of the dopamine D2, D3, 5-HT2A, and GABA(A)gamma2 receptors and serotonin transporter genes with heroin abuse in Chinese subjects., Am J Med Genet
Suzuki A et al., 2001, The -141C Ins/Del polymorphism in the dopamine D2 receptor gene promoter region is associated with anxiolytic and antidepressive effects during treatment with dopamine antagonists in schizophrenic patients., Pharmacogenetics
Marona-Lewicka et al., 2004, Aripiprazole (OPC-14597) fully substitutes for the 5-HT1A receptor agonist LY293284 in the drug discrimination assay in rats., Psychopharmacology (Berl.)
Cosi et al., 2005, Clozapine, ziprasidone and aripiprazole but not haloperidol protect against kainic acid-induced lesion of the striatum in mice, in vivo: role of 5-HT1A receptor activation., Brain Res.
Jordan et al., 2002, The antipsychotic aripiprazole is a potent, partial agonist at the human 5-HT1A receptor., Eur. J. Pharmacol.
Jordan et al., 2004, In vivo effects of aripiprazole on cortical and striatal dopaminergic and serotonergic function., Eur. J. Pharmacol.
Swainston Harrison et al., 2004, Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder., Drugs
Stark et al., 2007, Interaction of the novel antipsychotic aripiprazole with 5-HT1A and 5-HT 2A receptors: functional receptor-binding and in vivo electrophysiological studies., Psychopharmacology (Berl.)
Bortolozzi et al., 2007, In vivo actions of aripiprazole on serotonergic and dopaminergic systems in rodent brain., Psychopharmacology (Berl.)
Meltzer et al., 2003, Serotonin receptors: their key role in drugs to treat schizophrenia., Prog. Neuropsychopharmacol. Biol. Psychiatry
Serretti A et al., 2009, Influence of TAAR6 polymorphisms on response to aripiprazole., Prog Neuropsychopharmacol Biol Psychiatry
Zhang JP et al., 2016, Pharmacogenetic Associations of Antipsychotic Drug-Related Weight Gain: A Systematic Review and Meta-analysis., Schizophr Bull
Czerwensky F et al., 2013, MC4R rs489693: a clinical risk factor for second generation antipsychotic-related weight gain?, Int J Neuropsychopharmacol
Nurmi EL et al., 2013, Moderation of antipsychotic-induced weight gain by energy balance gene variants in the RUPP autism network risperidone studies., Transl Psychiatry
Malhotra AK et al., 2012, Association between common variants near the melanocortin 4 receptor gene and severe antipsychotic drug-induced weight gain., Arch Gen Psychiatry
Wang R et al., 2018, ABCB1 1199G > A Polymorphism Impacts Transport Ability of P-gp-Mediated Antipsychotics., DNA Cell Biol
Monteleone P et al., 2010, Endocannabinoid Pro129Thr FAAH functional polymorphism but not 1359G/A CNR1 polymorphism is associated with antipsychotic-induced weight gain., J Clin Psychopharmacol
Tiwari AK et al., 2010, A common polymorphism in the cannabinoid receptor 1 (CNR1) gene is associated with antipsychotic-induced weight gain in Schizophrenia., Neuropsychopharmacology
Delacrétaz A et al., 2017, Association of variants in SH2B1 and RABEP1 with worsening of low-density lipoprotein and glucose parameters in patients treated with psychotropic drugs., Gene
Ikeda M et al., 2008, Variants of dopamine and serotonin candidate genes as predictors of response to risperidone treatment in first-episode schizophrenia., Pharmacogenomics

ARIPIPRAZOLE CHRM3

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE HTR3A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

ARIPIPRAZOLE DRD2

Interaction Types & Directionality:

agonist (activating)

partial agonist (activating)

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction Measuring cAMP production via the Gi-coupled signaling pathway

Direct Interaction? True

Endogenous Drug? False

Publications:

Inoue et al., 1997, Aripiprazole, a novel antipsychotic drug, inhibits quinpirole-evoked GTPase activity but does not up-regulate dopamine D2 receptor following repeated treatment in the rat striatum., Eur. J. Pharmacol.

Wood et al., 2007, Aripiprazole acts as a selective dopamine D2 receptor partial agonist., Expert Opin Investig Drugs

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

ARIPIPRAZOLE HTR1A

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 1a (5-HT1a) receptor partial agonist

Trial Name Abilify

Publications:

Marona-Lewicka et al., 2004, Aripiprazole (OPC-14597) fully substitutes for the 5-HT1A receptor agonist LY293284 in the drug discrimination assay in rats., Psychopharmacology (Berl.)

Cosi et al., 2005, Clozapine, ziprasidone and aripiprazole but not haloperidol protect against kainic acid-induced lesion of the striatum in mice, in vivo: role of 5-HT1A receptor activation., Brain Res.

Jordan et al., 2002, The antipsychotic aripiprazole is a potent, partial agonist at the human 5-HT1A receptor., Eur. J. Pharmacol.

ARIPIPRAZOLE HTR1E

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE CHRM1

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE DRD4

Interaction Types & Directionality:

partial agonist (activating)

antagonist (inhibitory)

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE HTR2C

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

partial agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE HTR2A

Interaction Types & Directionality:

antagonist (inhibitory)

agonist (activating)

partial agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Specific Action of the Ligand Partial agonist

Publications:

Stark et al., 2007, Interaction of the novel antipsychotic aripiprazole with 5-HT1A and 5-HT 2A receptors: functional receptor-binding and in vivo electrophysiological studies., Psychopharmacology (Berl.)

Bortolozzi et al., 2007, In vivo actions of aripiprazole on serotonergic and dopaminergic systems in rodent brain., Psychopharmacology (Berl.)

Meltzer et al., 2003, Serotonin receptors: their key role in drugs to treat schizophrenia., Prog. Neuropsychopharmacol. Biol. Psychiatry

ARIPIPRAZOLE CHRM2

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE ADRA2B

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE HTR7

Interaction Types & Directionality:

antagonist (inhibitory)

partial agonist (activating)

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE HTR1B

Interaction Types & Directionality:

antagonist (inhibitory)

agonist (activating)

ligand

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE DRD3

Interaction Types & Directionality:

partial agonist (activating)

antagonist (inhibitory)

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE HTR6

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE ADRA2C

Interaction Types & Directionality:

antagonist (inhibitory)

other/unknown

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE ADRA1B

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE ADRA2A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE HRH1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE HTR1D

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

ligand

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE ADRA1A

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE DRD5

Interaction Types & Directionality:

partial agonist (activating)

antagonist (inhibitory)

ligand

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE CHRM4

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE CHRM5

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE DRD1

Interaction Types & Directionality:

partial agonist (activating)

antagonist (inhibitory)

ligand

Interaction Info:

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

ARIPIPRAZOLE HRH2

Interaction Types & Directionality:

ligand

Interaction Info:

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
ARIPIPRAZOLE SLC6A3

Interaction Types & Directionality:

modulator

Interaction Info:

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
ARIPIPRAZOLE OPRD1

Interaction Types & Directionality:

ligand

Interaction Info:

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
ARIPIPRAZOLE ADRB1

Interaction Types & Directionality:

ligand

Interaction Info:

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
ARIPIPRAZOLE GRIN1

Interaction Types & Directionality:

ligand

Interaction Info:

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
ARIPIPRAZOLE OPRK1

Interaction Types & Directionality:

ligand

Interaction Info:

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
ARIPIPRAZOLE OPRM1

Interaction Types & Directionality:

ligand

Interaction Info:

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
ARIPIPRAZOLE HRH4

Interaction Types & Directionality:

ligand

Interaction Info:

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
ARIPIPRAZOLE SLC6A4

Interaction Types & Directionality:

modulator

Interaction Info:

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
ARIPIPRAZOLE HRH3

Interaction Types & Directionality:

ligand

Interaction Info:

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
ARIPIPRAZOLE HTR2B

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
ARIPIPRAZOLE ADRB2

Interaction Types & Directionality:

ligand

Interaction Info:

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
ARIPIPRAZOLE HTR5A

Interaction Types & Directionality:

ligand

Interaction Info:

Publications:
ARIPIPRAZOLE TAAR6

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Serretti A et al., 2009, Influence of TAAR6 polymorphisms on response to aripiprazole., Prog Neuropsychopharmacol Biol Psychiatry

ARIPIPRAZOLE MC4R

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Zhang JP et al., 2016, Pharmacogenetic Associations of Antipsychotic Drug-Related Weight Gain: A Systematic Review and Meta-analysis., Schizophr Bull

Czerwensky F et al., 2013, MC4R rs489693: a clinical risk factor for second generation antipsychotic-related weight gain?, Int J Neuropsychopharmacol

Nurmi EL et al., 2013, Moderation of antipsychotic-induced weight gain by energy balance gene variants in the RUPP autism network risperidone studies., Transl Psychiatry

ARIPIPRAZOLE ABCB1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Wang R et al., 2018, ABCB1 1199G > A Polymorphism Impacts Transport Ability of P-gp-Mediated Antipsychotics., DNA Cell Biol

ARIPIPRAZOLE CNR1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Nurmi EL et al., 2013, Moderation of antipsychotic-induced weight gain by energy balance gene variants in the RUPP autism network risperidone studies., Transl Psychiatry

Monteleone P et al., 2010, Endocannabinoid Pro129Thr FAAH functional polymorphism but not 1359G/A CNR1 polymorphism is associated with antipsychotic-induced weight gain., J Clin Psychopharmacol

Tiwari AK et al., 2010, A common polymorphism in the cannabinoid receptor 1 (CNR1) gene is associated with antipsychotic-induced weight gain in Schizophrenia., Neuropsychopharmacology

ARIPIPRAZOLE SH2B1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Delacrétaz A et al., 2017, Association of variants in SH2B1 and RABEP1 with worsening of low-density lipoprotein and glucose parameters in patients treated with psychotropic drugs., Gene

ARIPIPRAZOLE FAAH

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Monteleone P et al., 2010, Endocannabinoid Pro129Thr FAAH functional polymorphism but not 1359G/A CNR1 polymorphism is associated with antipsychotic-induced weight gain., J Clin Psychopharmacol

ARIPIPRAZOLE ANKK1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Shen YC et al., 2009, Effects of DRD2/ANKK1 gene variations and clinical factors on aripiprazole efficacy in schizophrenic patients., J Psychiatr Res

Ikeda M et al., 2008, Variants of dopamine and serotonin candidate genes as predictors of response to risperidone treatment in first-episode schizophrenia., Pharmacogenomics

ARIPIPRAZOLE RABEP1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Delacrétaz A et al., 2017, Association of variants in SH2B1 and RABEP1 with worsening of low-density lipoprotein and glucose parameters in patients treated with psychotropic drugs., Gene
ARIPIPRAZOLE CYP2D6

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

DrugBank: DB01238

Version: 5.1.7

Alternate Names:

ARIPIPRAZOLE DrugBank Drug Name

129722-12-9 CAS Number

Abilify Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Bortolozzi et al., 2007, In vivo actions of aripiprazole on serotonergic and dopaminergic systems in rodent brain., Psychopharmacology (Berl.)

TEND: ARIPIPRAZOLE
- Version: 01-August-2011
Alternate Names:

ARIPIPRAZOLE Primary Drug Name

Drug Info:

Year of Approval 2002

Drug Class antipsychotic agents

Publications:
TdgClinicalTrial: ARIPIPRAZOLE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antipsychotic agent

Drug Class Small Molecule

FDA Approval approved

Publications:

PharmGKB: aripiprazole

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Suzuki A et al., 2001, The -141C Ins/Del polymorphism in the dopamine D2 receptor gene promoter region is associated with anxiolytic and antidepressive effects during treatment with dopamine antagonists in schizophrenic patients., Pharmacogenetics

Li T et al., 2002, Allelic association analysis of the dopamine D2, D3, 5-HT2A, and GABA(A)gamma2 receptors and serotonin transporter genes with heroin abuse in Chinese subjects., Am J Med Genet

Yamanouchi Y et al., 2003, Effect of DRD2, 5-HT2A, and COMT genes on antipsychotic response to risperidone., Pharmacogenomics J

GuideToPharmacology: 135649956
- Version: 29-September-2020
Alternate Names:

ARIPIPRAZOLE GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: Aripiprazole
- Version: 2020.06.01
Alternate Names:

D0H3HM TTD Drug ID

Drug Info:

Publications:
ChemblInteractions: CHEMBL1112
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1112
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
FDA: Aripiprazole
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:

Details of the Assay for Interaction	Measuring cAMP production via the Gi-coupled signaling pathway
Direct Interaction?	True
Endogenous Drug?	False

Direct Interaction	yes
Mechanism of Interaction	Serotonin 1a (5-HT1a) receptor partial agonist
Trial Name	Abilify

Direct Interaction	yes
Mechanism of Interaction	Serotonin 2a (5-HT2a) receptor antagonist
Specific Action of the Ligand	Partial agonist

Specific Action of the Ligand	Full agonist
Endogenous Drug?	False

Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

ARIPIPRAZOLE	DrugBank Drug Name
129722-12-9	CAS Number
Abilify	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational

ARIPIPRAZOLE Drug Record

ARIPIPRAZOLE chembl:CHEMBL1112 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: antagonist (inhibitory) ligand

Interaction Info:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

Publications: Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

Interaction Types & Directionality: agonist (activating) partial agonist (activating) antagonist (inhibitory)

Interaction Info: Details of the Assay for Interaction Measuring cAMP production via the Gi-coupled signaling pathway Direct Interaction? True Endogenous Drug? False

Interaction Types & Directionality: partial agonist (activating) agonist (activating) antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Serotonin 1a (5-HT1a) receptor partial agonist Trial Name Abilify

Interaction Types & Directionality: antagonist (inhibitory) ligand

Interaction Info:

Interaction Types & Directionality: antagonist (inhibitory) ligand

Interaction Info:

Interaction Types & Directionality: partial agonist (activating) antagonist (inhibitory)

Interaction Info:

Interaction Types & Directionality: agonist (activating) antagonist (inhibitory) partial agonist (activating)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Partial agonist

Interaction Types & Directionality: antagonist (inhibitory) agonist (activating) partial agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist Specific Action of the Ligand Partial agonist

Interaction Types & Directionality: antagonist (inhibitory) ligand

Interaction Info:

Interaction Types & Directionality: antagonist (inhibitory) ligand

Interaction Info:

Interaction Types & Directionality: antagonist (inhibitory) partial agonist (activating)

Interaction Info:

Interaction Types & Directionality: antagonist (inhibitory) agonist (activating) ligand

Interaction Info: Specific Action of the Ligand Full agonist Endogenous Drug? False

Interaction Types & Directionality: partial agonist (activating) antagonist (inhibitory)

Interaction Info:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

Interaction Types & Directionality: antagonist (inhibitory) other/unknown

Interaction Info:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

Interaction Types & Directionality: agonist (activating) antagonist (inhibitory) ligand

Interaction Info: Specific Action of the Ligand Full agonist Endogenous Drug? False

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

Interaction Types & Directionality: partial agonist (activating) antagonist (inhibitory) ligand

Interaction Info:

Interaction Types & Directionality: antagonist (inhibitory) ligand

Interaction Info:

Interaction Types & Directionality: antagonist (inhibitory) ligand

Interaction Info:

Interaction Types & Directionality: partial agonist (activating) antagonist (inhibitory) ligand

Interaction Info:

Interaction Types & Directionality: ligand

Interaction Info:

Publications: de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality: modulator

Interaction Info:

Publications: de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality: ligand

Interaction Info:

Publications: de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality: ligand

Interaction Info:

Publications: de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality: ligand

Interaction Info:

Publications: de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality: ligand

Interaction Info:

Publications: de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality: ligand

Interaction Info:

Publications: de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality: ligand

Interaction Info:

Publications: de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

Interaction Types & Directionality:

antagonist (inhibitory)

Publications:

Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry

Interaction Types & Directionality:

agonist (activating)

partial agonist (activating)

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction Measuring cAMP production via the Gi-coupled signaling pathway

Direct Interaction? True

Endogenous Drug? False

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 1a (5-HT1a) receptor partial agonist

Trial Name Abilify

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

Interaction Types & Directionality:

partial agonist (activating)

antagonist (inhibitory)

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

partial agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

Interaction Types & Directionality:

antagonist (inhibitory)

agonist (activating)

partial agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2a (5-HT2a) receptor antagonist

Specific Action of the Ligand Partial agonist

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

Interaction Types & Directionality:

antagonist (inhibitory)

partial agonist (activating)

Interaction Types & Directionality:

antagonist (inhibitory)

agonist (activating)

ligand

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types & Directionality:

partial agonist (activating)

antagonist (inhibitory)

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Types & Directionality:

antagonist (inhibitory)

other/unknown

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

ligand

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Types & Directionality:

partial agonist (activating)

antagonist (inhibitory)

ligand

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

Interaction Types & Directionality:

partial agonist (activating)

antagonist (inhibitory)

ligand

Interaction Types & Directionality:

ligand

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality:

modulator

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality:

ligand

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality:

ligand

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality:

ligand

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality:

ligand

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality:

ligand

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality:

ligand

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality:

modulator

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality:

ligand

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs

Interaction Types & Directionality:

inverse agonist (inhibitory)

Publications:

de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs