Aripiprazole

Identification

Summary

Aripiprazole is an atypical antipsychotic used in the treatment of a wide variety of mood and psychotic disorders, such as schizophrenia, bipolar I, major depressive disorder, irritability associated with autism, and Tourette's syndrome.

Brand Names
Abilify
Generic Name
Aripiprazole
DrugBank Accession Number
DB01238
Background

Aripiprazole is an atypical antipsychotic orally indicated for treatment of schizophrenia, bipolar I, major depressive disorder, irritability associated with autism, and Tourette'sLabel. It is also indicated as an injection for agitation associated with schizophrenia or bipolar maniaLabel. Aripiprazole exerts its effects through agonism of dopaminic and 5-HT1A receptors and antagonism of alpha adrenergic and 5-HT2A receptorsLabel,1. Aripiprazole was given FDA approval on November 15, 20025.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 448.385
Monoisotopic: 447.148032537
Chemical Formula
C23H27Cl2N3O2
Synonyms
  • Aripiprazol
  • Aripiprazole
  • Aripiprazolum
External IDs
  • OPC 31
  • OPC-14597
  • OPC-31

Pharmacology

Indication

Aripiprazole is indicated for manic and mixed episodes associated with bipolar I disorder, irritability associated with autism spectrum disorder, treatment of schizophrenia, treatment of Tourette's disorder, and as an adjunctive treatment of major depressive disorderLabel. An injectable formulation of aripiprazole is indicated for agitation associated with schizophrenia or bipolar maniaLabel.

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Aripiprazole has high affinity for serotonin type 2 (5HT2), dopamine type 2 (D2), alpha1 and 2 adrenergic, and H1 histaminergic receptorsLabel,1. It also acts on a number of other receptors with lower affinityLabel,1. The exact method by which aripiprazole's action on these receptors translates to a clinically relevant effect is not yet knownLabel.

Mechanism of action

The antipsychotic action of aripiprazole is likely due to the agonism of D2 and 5-HT1A receptors though the exact mechanism has not been definedLabel,1. Some adverse effects may be due to action on other receptorsLabel. For example, orthostatic hypotension may be explained by antagonism of the adrenergic alpha1 receptorsLabel,1.

TargetActionsOrganism
ADopamine D2 receptor
antagonist
partial agonist
Humans
A5-hydroxytryptamine receptor 2A
antagonist
partial agonist
Humans
U5-hydroxytryptamine receptor 1A
partial agonist
Humans
NAlpha-1A adrenergic receptor
antagonist
Humans
NAlpha-1B adrenergic receptor
antagonist
Humans
UDopamine D3 receptor
antagonist
partial agonist
Humans
U5-hydroxytryptamine receptor 1D
antagonist
ligand
Humans
U5-hydroxytryptamine receptor 7
antagonist
partial agonist
Humans
NAlpha-2A adrenergic receptor
antagonist
Humans
NAlpha-2C adrenergic receptor
antagonist
other/unknown
Humans
NHistamine H1 receptor
antagonist
Humans
U5-hydroxytryptamine receptor 1B
antagonist
ligand
Humans
U5-hydroxytryptamine receptor 2C
antagonist
partial agonist
Humans
U5-hydroxytryptamine receptor 3A
antagonist
Humans
U5-hydroxytryptamine receptor 6
antagonist
Humans
UDopamine D1 receptor
antagonist
partial agonist
ligand
Humans
UDopamine D4 receptor
antagonist
partial agonist
Humans
NAlpha-2B adrenergic receptor
antagonist
ligand
Humans
U5-hydroxytryptamine receptor 1E
antagonist
ligand
Humans
UDopamine D5 receptor
antagonist
partial agonist
ligand
Humans
U5-hydroxytryptamine receptor 2B
inverse agonist
Humans
U5-hydroxytryptamine receptor 5A
ligand
Humans
UBeta-1 adrenergic receptor
ligand
Humans
UBeta-2 adrenergic receptor
ligand
Humans
UHistamine H2 receptor
ligand
Humans
UHistamine H3 receptor
ligand
Humans
UHistamine H4 receptor
ligand
Humans
UMuscarinic acetylcholine receptor M1
ligand
Humans
UMuscarinic acetylcholine receptor M2
ligand
Humans
UMuscarinic acetylcholine receptor M3
ligand
Humans
UMuscarinic acetylcholine receptor M4
ligand
Humans
UMuscarinic acetylcholine receptor M5
ligand
Humans
UKappa-type opioid receptor
ligand
Humans
UMu-type opioid receptor
ligand
Humans
UDelta-type opioid receptor
ligand
Humans
UGlutamate (NMDA) receptor
ligand
Humans
USodium-dependent dopamine transporter
modulator
Humans
USodium-dependent serotonin transporter
modulator
Humans
Absorption

Aripiprazole tablets are 87% bioavailable and reach peak plasma concentrations in 3 to 5 hoursLabel. These tablets can be taken with or without food, but a high fat meal can delay the time to max concentration by 3 hours and up to 12 hours for the active metaboliteLabel.

Volume of distribution

404L or 4.9L/kgLabel,2.

Protein binding

>99%Label.

Metabolism

Metabolism of aripiprazole is predominantly hepatic, mediated mostly by cytochrome P450 (CYP)3A4 and CYP2D6Label,2. These enzymes perform dehydrogenation and hydroxylation while CYP3A4 alone performs N-dealkylationLabel,2. At any given time, the active metabolite dehydro-aripiprazole is approximately 40% of the drug available in plasmaLabel.

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Route of elimination

25% of a given dose will be eliminated in urine and 55% in the fecesLabel,4. <1% of a dose is eliminated in the urine as unmetabolized aripiprazole and approximately 18% of a dose will be eliminated in the feces unmetabolizedLabel,4.

Half-life

The half life of aripiprazole is 75 hours while the half life of the active metabolite is 94 hoursLabel. For populations that are poor CYP2D6 metabolizers, the half life of aripiprazole is 146 hours and these patients should be treated with half the normal doseLabel. Other studies have reported a half life of 61.03±19.59 hours for aripiprazole and 279±299 hours for the active metabolite3.

Clearance

0.8mL/min/kg2. Other studies have reported a clearance rate of 3297±1042mL/hr3.

Adverse Effects
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Toxicity

Studies on the safety and effectiveness of aripiprazole in pregnancy have not been performed, though there is currently a national pregnancy registry for mothers currently taking aripiprazole in pregnancyLabel,6. In other studies of antipsychotic medication in pregnancy, children are at risk of extrapyramidal or withdrawal symptomsLabel. In animal studies of pregnancy, aripiprazole was associated with a number of malformations and fetal death at doses higher than the maximum recommended human doseLabel. Aripiprazole should only be prescribed in pregnancy if the benefits outweigh the risksLabel. Neonates with third trimester exposure to aripiprazole may show extrapyramidal or withdrawal symptoms of varying severityLabel. These symptoms may resolve in hours or require extended hospital careLabel. Aripiprazole's effect on labor and delivery has not been investigatedLabel. Aripiprazole is present in human breast milk and so patients should either stop breastfeeding or stop taking aripiprazole depending on the risk and benefit to mother and childLabel. Pharmacokinetic properties in patients 10-17 years of age are similar to that of adults once body weight has been corrected forLabel. No dosage adjustment is necessary in elderly patients however aripiprazole is not approved for Alzheimer's associated psychosisLabel. Patients calssified as CYP2D6 poor metabolizers should be prescribed half the regular dose of aripiprazoleLabel. Hepatic and renal function as well as sex, race, and smoking status do not affect dosage requirements for aripiprazoleLabel,3.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Cytochrome P450 2D6CYP2D6*3Not AvailableC alleleEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*4Not AvailableC alleleEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*5Not AvailableWhole-gene deletionEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*6Not Available1707delTEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*7Not Available2935A>CEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*8Not Available1758G>TEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*11Not Available883G>CEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*12Not Available124G>AEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*13Not AvailableCYP2D7/2D6 hybrid gene structureEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*14ANot Available1758G>AEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*15Not Available137insT, 137_138insTEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*19Not Available2539_2542delAACTEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*20Not Available1973_1974insGEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*21Not Available2573insCEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*31Not Available-1770G>A / -1584C>G  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*36Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*38Not Available2587_2590delGACTEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*40Not Available1863_1864ins(TTT CGC CCC)2Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*42Not Available3259_3260insGTEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*44Not Available2950G>CEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*47Not Available100C>T / -1426C>T  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*51Not Available-1584C>G / -1235A>G  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*56Not Available3201C>TEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*57Not Available100C>T / 310G>T  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*62Not Available4044C>TEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*68ANot Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*68BNot AvailableSimilar but not identical switch region compared to CYP2D6*68A. Found in tandem arrangement with CYP2D6*4.Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*69Not Available2988G>A / -1426C>T  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*92Not Available1995delCEffect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*100Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details
Cytochrome P450 2D6CYP2D6*101Not Available-1426C>T / -1235A>G  … show all Effect InferredPoor drug metabolizer, lower dose requirement.Details

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
1,2-BenzodiazepineThe risk or severity of adverse effects can be increased when Aripiprazole is combined with 1,2-Benzodiazepine.
AbaloparatideAripiprazole may increase the hypotensive activities of Abaloparatide.
AbametapirThe serum concentration of Aripiprazole can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Aripiprazole can be increased when combined with Abatacept.
AbirateroneThe metabolism of Aripiprazole can be decreased when combined with Abiraterone.
AcalabrutinibThe metabolism of Aripiprazole can be decreased when combined with Acalabrutinib.
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Aripiprazole.
AcebutololThe risk or severity of hypotension can be increased when Aripiprazole is combined with Acebutolol.
AceclofenacThe risk or severity of hypertension can be increased when Aripiprazole is combined with Aceclofenac.
AcemetacinThe risk or severity of hypertension can be increased when Aripiprazole is combined with Acemetacin.
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Food Interactions
  • Avoid alcohol. Alcohol may increase CNS effects.
  • Drink plenty of fluids. Drink water to avoid dehydration while taking aripiprazole.
  • Take with or without food. Food does not affect absorption.

Products

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Product Images
International/Other Brands
Abilitat
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AbilifyTablet30 mgOralOtsuka Pharmaceutical Netherlands B.V.2021-01-12Not applicableEU flag
AbilifyTablet15 mg/1OralRebel Distributors2002-11-15Not applicableUS flag
AbilifyTablet30 mg/1OralRemedy Repack2010-12-132014-06-21US flag
AbilifyTablet5 mg/1OralCardinal Health2002-11-152017-09-30US flag
AbilifyTablet15 mg/1OralOtsuka America Pharmaceutical, Inc.2002-11-15Not applicableUS flag
AbilifyTablet5 mgOralOtsuka Pharmaceutical Netherlands B.V.2021-01-12Not applicableEU flag
AbilifyTablet, orally disintegrating30 mgOralOtsuka Pharmaceutical Netherlands B.V.2021-01-12Not applicableEU flag
AbilifyTablet10 mg/1OralAphena Pharma Solutions Tennessee, Inc.2002-11-15Not applicableUS flag
AbilifyTablet2 mg/1OralOtsuka America Pharmaceutical, Inc.2002-11-15Not applicableUS flag
AbilifyTablet15 mgOralOtsuka Pharmaceutical Co., Ltd.2009-09-30Not applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-aripiprazoleTablet15 mgOralApotex Corporation2018-04-10Not applicableCanada flag
Apo-aripiprazoleTablet2 mgOralApotex Corporation2018-04-10Not applicableCanada flag
Apo-aripiprazoleTablet30 mgOralApotex Corporation2018-04-10Not applicableCanada flag
Apo-aripiprazoleTablet10 mgOralApotex Corporation2018-04-10Not applicableCanada flag
Apo-aripiprazoleTablet20 mgOralApotex Corporation2018-04-10Not applicableCanada flag
Apo-aripiprazoleTablet5 mgOralApotex Corporation2018-04-10Not applicableCanada flag
AripiprazoleTablet30 mg/1OralMajor Pharmaceuticals2015-08-25Not applicableUS flag
AripiprazoleTablet2 mg/1OralMajor Pharmaceuticals2015-04-282015-04-28US flag
AripiprazoleTablet20 mg/1OralCamber Pharmaceuticals, Inc.2015-04-28Not applicableUS flag
AripiprazoleSolution1 mg/1mLOralAurobindo Pharma Limited2019-01-29Not applicableUS flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
AbilifyAripiprazole (15 mg/1)TabletOralRemedy Repack2010-12-142014-08-27US flag
AbilifyAripiprazole (20 mg/1)TabletOralRemedy Repack2013-04-092014-08-12US flag
AbilifyAripiprazole (10 mg/1)TabletOralRemedy Repack2010-12-142015-05-20US flag
AbilifyAripiprazole (30 mg/1)TabletOralRemedy Repack2010-12-132014-06-21US flag
CUREXOL 5 MG TABLET, 28 ADETAripiprazole (5 mg)TabletOralACTAVİS İLAÇLARI A.Ş.2020-08-14Not applicableTurkey flag

Categories

ATC Codes
N05AX12 — Aripiprazole
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as phenylpiperazines. These are compounds containing a phenylpiperazine skeleton, which consists of a piperazine bound to a phenyl group.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazinanes
Sub Class
Piperazines
Direct Parent
Phenylpiperazines
Alternative Parents
N-arylpiperazines / Hydroquinolones / Hydroquinolines / Dichlorobenzenes / Dialkylarylamines / Aniline and substituted anilines / N-alkylpiperazines / Alkyl aryl ethers / Aryl chlorides / Secondary carboxylic acid amides
show 9 more
Substituents
1,2-dichlorobenzene / Alkyl aryl ether / Amine / Amino acid or derivatives / Aniline or substituted anilines / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid
show 28 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
N-arylpiperazine, dichlorobenzene, N-alkylpiperazine, quinolone (CHEBI:31236)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
82VFR53I78
CAS number
129722-12-9
InChI Key
CEUORZQYGODEFX-UHFFFAOYSA-N
InChI
InChI=1S/C23H27Cl2N3O2/c24-19-4-3-5-21(23(19)25)28-13-11-27(12-14-28)10-1-2-15-30-18-8-6-17-7-9-22(29)26-20(17)16-18/h3-6,8,16H,1-2,7,9-15H2,(H,26,29)
IUPAC Name
7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-1,2,3,4-tetrahydroquinolin-2-one
SMILES
ClC1=CC=CC(N2CCN(CCCCOC3=CC4=C(CCC(=O)N4)C=C3)CC2)=C1Cl

References

Synthesis Reference
US5006528
General References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. Bauman JN, Frederick KS, Sawant A, Walsky RL, Cox LM, Obach RS, Kalgutkar AS: Comparison of the bioactivation potential of the antidepressant and hepatotoxin nefazodone with aripiprazole, a structural analog and marketed drug. Drug Metab Dispos. 2008 Jun;36(6):1016-29. doi: 10.1124/dmd.108.020545. Epub 2008 Mar 10. [Article]
  3. Kubo M, Koue T, Maune H, Fukuda T, Azuma J: Pharmacokinetics of aripiprazole, a new antipsychotic, following oral dosing in healthy adult Japanese volunteers: influence of CYP2D6 polymorphism. Drug Metab Pharmacokinet. 2007 Oct;22(5):358-66. [Article]
  4. Prommer E: Aripiprazole. Am J Hosp Palliat Care. 2017 Mar;34(2):180-185. doi: 10.1177/1049909115612800. Epub 2016 Jul 10. [Article]
  5. FDA Drug Approval Package: Aripiprazole [Link]
  6. Clinicaltrails.gov: National Pregnancy Registry for Atypical Antipsychotics [Link]
Human Metabolome Database
HMDB0005042
KEGG Drug
D01164
KEGG Compound
C12564
PubChem Compound
60795
PubChem Substance
46505745
ChemSpider
54790
BindingDB
50130293
RxNav
89013
ChEBI
31236
ChEMBL
CHEMBL1112
ZINC
ZINC000001851149
Therapeutic Targets Database
DAP000076
PharmGKB
PA10026
Guide to Pharmacology
GtP Drug Page
PDBe Ligand
9SC
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Aripiprazole
PDB Entries
6a7p / 7e2z / 7voe / 7vr9 / 7wkz
FDA label
Download (1.35 MB)
MSDS
Download (24.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentDementia / Depression / Geriatric Depression / Late Life Depression (LLD) / Major Depressive Disorder (MDD) / Major depressive disorder, recurrent episode / Mild Cognitive Impairment (MCI) / Treatment-Refractory Depression1
4CompletedBasic ScienceCYP3A4 Protein, Human / Cytochrome P-450 CYP2D6 / Pharmacokinetics1
4CompletedBasic ScienceDiabetes2
4CompletedBasic SciencePsychosis / Schizophrenia1
4CompletedHealth Services ResearchFirst Episode Psychosis (FEP) / Schizoaffective Disorders / Schizophrenia1
4CompletedHealth Services ResearchSchizophrenia1
4CompletedPreventionSchizophrenia1
4CompletedSupportive CareAutism Disorder1
4CompletedTreatmentAdherence, Medication / Bipolar Disorder (BD) / Nonadherence, Medication1
4CompletedTreatmentAggression / Attention Deficit Hyperactivity Disorder (ADHD) / Bipolar Disorder (BD) / Defiant Disorder, Oppositional / Pervasive Development Disorder1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Bristol-Myers Squibb Co.
  • Bryant Ranch Prepack
  • Cardinal Health
  • Comprehensive Consultant Services Inc.
  • DispenseXpress Inc.
  • E.R. Squibb and Sons LLC
  • Murfreesboro Pharmaceutical Nursing Supply
  • Otsuka America
  • PD-Rx Pharmaceuticals Inc.
  • Physician Partners Ltd.
  • Physicians Total Care Inc.
  • Quality Care
  • Rebel Distributors Corp.
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Southwood Pharmaceuticals
  • Stat Rx Usa
Dosage Forms
FormRouteStrength
Injection
Injection, solutionIntramuscular7.5 MG/ML
Injection, solutionIntramuscular9.75 mg/1.3mL
SolutionOral
TabletOral10 mg/1
TabletOral15 mg/1
TabletOral2 mg/1
TabletOral20 mg/1
TabletOral30 mg/1
TabletOral5 mg/1
Tablet, orally disintegratingOral5 MG
Injection, solutionIntramuscular
Injection, powder, for suspension, extended releaseIntramuscular300 mg / syr
Injection, powder, for suspension, extended releaseIntramuscular300 mg
Injection, powder, for suspension, extended releaseIntramuscular400 mg / syr
Injection, powder, for suspension, extended releaseIntramuscular400 mg
Injection, powder, for suspension, extended releaseIntramuscular; Parenteral300 MG
Injection, powder, for suspension, extended releaseIntramuscular; Parenteral400 MG
Injection, powder, for suspension, extended release; kitIntramuscular300 mg / vial
Injection, powder, for suspension, extended release; kitIntramuscular400 mg / vial
Injection, powder, lyophilized, for suspension, extended releaseIntramuscular300 mg/1.5mL
Injection, powder, lyophilized, for suspension, extended releaseIntramuscular400 mg/2.0mL
Injection, suspension, extended release; kitIntramuscular300 mg/1.5mL
Injection, suspension, extended release; kitIntramuscular400 mg/1.9mL
Injection, powder, for suspensionIntramuscular300 mg/1vial
Injection, powder, for suspensionIntramuscular400 mg/1vial
Injection, suspension, extended releaseIntramuscular
Injection, powder, for suspensionIntramuscular
Injection, suspension, extended releaseIntramuscular400 mg
Injection, powder, for suspension, extended releaseIntramuscular400 mg/vial
SolutionOral1.0 mg/ml
TabletOral10.0 mg
TabletOral2 mg
TabletOral5.0 mg
TabletOral20 mg
TabletOral10 mg
TabletOral15 mg
Tablet, orally disintegratingOral10 mg
Tablet, orally disintegratingOral15 mg
TabletOral
TabletOral5 mg
Tablet, solubleBuccal
Tablet, orally disintegratingOral
SolutionOral1 mg/1mL
Tablet, orally disintegratingOral10 mg/1
Tablet, orally disintegratingOral15 mg/1
Tablet, orally disintegratingOral20 mg/1
Tablet, orally disintegratingOral30 mg/1
Tablet, solubleOral
SolutionOral1 MG/ML
Tablet, orally disintegratingOral30 MG
TabletOral30 mg
SolutionOral100 mg
SolutionOral1 mg
Tablet, solubleBuccal15 mg
Tablet, coatedOral10 mg
Tablet, coatedOral15 mg
Tablet, coatedOral5 mg
Prices
Unit descriptionCostUnit
Abilify Discmelt 30 10 mg Dispersible Tablet Box636.3USD box
Abilify 30 mg tablet32.12USD tablet
Abilify 15 mg tablet26.07USD tablet
Abilify 10 mg tablet23.53USD tablet
Abilify 5 mg tablet23.53USD tablet
Abilify 2 mg tablet22.25USD tablet
Abilify 20 mg tablet21.99USD tablet
Abilify discmelt 10 mg tablet20.39USD tablet
Abilify discmelt 15 mg tablet20.39USD tablet
Abilify 9.7 mg/1.3 ml vial16.04USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5006528No1991-04-092014-10-20US flag
US7053092No2006-05-302022-01-28US flag
US8642600Yes2014-02-042022-07-28US flag
US8759350No2014-06-242027-03-02US flag
US9125939No2015-09-082026-07-28US flag
US9089567No2015-07-282022-01-28US flag
US8017615Yes2011-09-132024-12-16US flag
US8580796Yes2013-11-122023-03-25US flag
US8642760Yes2014-02-042023-03-25US flag
US6977257Yes2005-12-202022-10-24US flag
US8518421Yes2013-08-272021-07-24US flag
US7115587Yes2006-10-032025-01-21US flag
US7550445Yes2009-06-232025-01-21US flag
US8030313No2011-10-042024-10-19US flag
US8338427No2012-12-252025-03-15US flag
US8338428No2012-12-252023-08-06US flag
US8759351No2014-06-242023-08-06US flag
US7807680No2010-10-052024-10-19US flag
US8993761No2015-03-312022-09-25US flag
US8722679No2014-05-132024-10-19US flag
US8399469No2013-03-192025-06-29US flag
US9193685No2015-11-242033-10-24US flag
US8796276No2014-08-052030-06-24US flag
US9034867No2015-05-192032-11-07US flag
US8431576No2013-04-302030-10-26US flag
US9387182No2016-07-122023-12-25US flag
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Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)137-140http://www.chemspider.com/Chemical-Structure.54790.html
water solubility0.00001%https://medsafe.govt.nz/profs/Datasheet/a/Abilifytab.pdf
pKa7.6https://medsafe.govt.nz/profs/Datasheet/a/Abilifytab.pdf
Predicted Properties
PropertyValueSource
Water Solubility0.00777 mg/mLALOGPS
logP5.21ALOGPS
logP4.9Chemaxon
logS-4.8ALOGPS
pKa (Strongest Acidic)13.51Chemaxon
pKa (Strongest Basic)7.46Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count4Chemaxon
Hydrogen Donor Count1Chemaxon
Polar Surface Area44.81 Ã…2Chemaxon
Rotatable Bond Count7Chemaxon
Refractivity124.34 m3·mol-1Chemaxon
Polarizability49.23 Ã…3Chemaxon
Number of Rings4Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9934
Blood Brain Barrier+0.992
Caco-2 permeable+0.5
P-glycoprotein substrateSubstrate0.7431
P-glycoprotein inhibitor IInhibitor0.9585
P-glycoprotein inhibitor IIInhibitor0.9321
Renal organic cation transporterInhibitor0.5175
CYP450 2C9 substrateNon-substrate0.8663
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.7408
CYP450 1A2 substrateInhibitor0.6581
CYP450 2C9 inhibitorInhibitor0.6682
CYP450 2D6 inhibitorInhibitor0.6633
CYP450 2C19 inhibitorInhibitor0.8934
CYP450 3A4 inhibitorInhibitor0.5256
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9104
Ames testNon AMES toxic0.6124
CarcinogenicityNon-carcinogens0.8765
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.8894 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.62
hERG inhibition (predictor II)Inhibitor0.8814
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0f72-0340900000-34d93478ad0d9f5cf2b0
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000i-3970100000-6b98b53e8175df39986e

Targets

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Details
1. Dopamine D2 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
Partial agonist
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Hirose T, Kikuchi T: Aripiprazole, a novel antipsychotic agent: dopamine D2 receptor partial agonist. J Med Invest. 2005 Nov;52 Suppl:284-90. [Article]
  2. Inoue A, Miki S, Seto M, Kikuchi T, Morita S, Ueda H, Misu Y, Nakata Y: 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. 1997 Feb 19;321(1):105-11. [Article]
  3. Wood MD, Scott C, Clarke K, Westaway J, Davies CH, Reavill C, Hill M, Rourke C, Newson M, Jones DN, Forbes IT, Gribble A: Aripiprazole and its human metabolite are partial agonists at the human dopamine D2 receptor, but the rodent metabolite displays antagonist properties. Eur J Pharmacol. 2006 Sep 28;546(1-3):88-94. Epub 2006 Jul 21. [Article]
  4. Kim E, Yu KS, Cho JY, Shin YW, Yoo SY, Kim YY, Jang IJ, Shin SG, Kwon JS: Effects of DRD2 and CYP2D6 genotypes on delta EEG power response to aripiprazole in healthy male volunteers: a preliminary study. Hum Psychopharmacol. 2006 Dec;21(8):519-28. [Article]
  5. Wood M, Reavill C: Aripiprazole acts as a selective dopamine D2 receptor partial agonist. Expert Opin Investig Drugs. 2007 Jun;16(6):771-5. [Article]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  7. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
Partial agonist
General Function
Virus receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 Da
References
  1. Meltzer HY, Li Z, Kaneda Y, Ichikawa J: Serotonin receptors: their key role in drugs to treat schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry. 2003 Oct;27(7):1159-72. [Article]
  2. Stark AD, Jordan S, Allers KA, Bertekap RL, Chen R, Mistry Kannan T, Molski TF, Yocca FD, Sharp T, Kikuchi T, Burris KD: Interaction of the novel antipsychotic aripiprazole with 5-HT1A and 5-HT 2A receptors: functional receptor-binding and in vivo electrophysiological studies. Psychopharmacology (Berl). 2007 Feb;190(3):373-82. Epub 2006 Nov 25. [Article]
  3. Bortolozzi A, Diaz-Mataix L, Toth M, Celada P, Artigas F: In vivo actions of aripiprazole on serotonergic and dopaminergic systems in rodent brain. Psychopharmacology (Berl). 2007 Apr;191(3):745-58. Epub 2007 Jan 30. [Article]
  4. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Partial agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da
References
  1. Jordan S, Koprivica V, Chen R, Tottori K, Kikuchi T, Altar CA: The antipsychotic aripiprazole is a potent, partial agonist at the human 5-HT1A receptor. Eur J Pharmacol. 2002 Apr 26;441(3):137-40. [Article]
  2. Marona-Lewicka D, Nichols DE: Aripiprazole (OPC-14597) fully substitutes for the 5-HT1A receptor agonist LY293284 in the drug discrimination assay in rats. Psychopharmacology (Berl). 2004 Apr;172(4):415-21. Epub 2003 Nov 28. [Article]
  3. Jordan S, Koprivica V, Dunn R, Tottori K, Kikuchi T, Altar CA: In vivo effects of aripiprazole on cortical and striatal dopaminergic and serotonergic function. Eur J Pharmacol. 2004 Jan 1;483(1):45-53. [Article]
  4. Swainston Harrison T, Perry CM: Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder. Drugs. 2004;64(15):1715-36. [Article]
  5. Cosi C, Waget A, Rollet K, Tesori V, Newman-Tancredi A: 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. 2005 May 10;1043(1-2):32-41. [Article]
  6. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
Molecular Weight
51486.005 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1B
Uniprot ID
P35368
Uniprot Name
Alpha-1B adrenergic receptor
Molecular Weight
56835.375 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Details
6. Dopamine D3 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name
DRD3
Uniprot ID
P35462
Uniprot Name
D(3) dopamine receptor
Molecular Weight
44224.335 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Ligand
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1D
Uniprot ID
P28221
Uniprot Name
5-hydroxytryptamine receptor 1D
Molecular Weight
41906.38 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR7
Uniprot ID
P34969
Uniprot Name
5-hydroxytryptamine receptor 7
Molecular Weight
53554.43 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Antagonist
General Function
Thioesterase binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Antagonist
Other/unknown
General Function
Protein homodimerization activity
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name
ADRA2C
Uniprot ID
P18825
Uniprot Name
Alpha-2C adrenergic receptor
Molecular Weight
49521.585 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Details
11. Histamine H1 receptor
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Antagonist
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Ligand
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1B
Uniprot ID
P28222
Uniprot Name
5-hydroxytryptamine receptor 1B
Molecular Weight
43567.535 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
Molecular Weight
51820.705 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Voltage-gated potassium channel activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gate...
Gene Name
HTR3A
Uniprot ID
P46098
Uniprot Name
5-hydroxytryptamine receptor 3A
Molecular Weight
55279.835 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR6
Uniprot ID
P50406
Uniprot Name
5-hydroxytryptamine receptor 6
Molecular Weight
46953.625 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Details
16. Dopamine D1 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
Ligand
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name
DRD1
Uniprot ID
P21728
Uniprot Name
D(1A) dopamine receptor
Molecular Weight
49292.765 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Details
17. Dopamine D4 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
General Function
Sh3 domain binding
Specific Function
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins ...
Gene Name
DRD4
Uniprot ID
P21917
Uniprot Name
D(4) dopamine receptor
Molecular Weight
48359.86 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Antagonist
Ligand
General Function
Epinephrine binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine...
Gene Name
ADRA2B
Uniprot ID
P18089
Uniprot Name
Alpha-2B adrenergic receptor
Molecular Weight
49565.8 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Ligand
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that trig...
Gene Name
HTR1E
Uniprot ID
P28566
Uniprot Name
5-hydroxytryptamine receptor 1E
Molecular Weight
41681.57 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Details
20. Dopamine D5 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
Ligand
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name
DRD5
Uniprot ID
P21918
Uniprot Name
D(1B) dopamine receptor
Molecular Weight
52950.5 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inverse agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation...
Gene Name
HTR2B
Uniprot ID
P41595
Uniprot Name
5-hydroxytryptamine receptor 2B
Molecular Weight
54297.41 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR5A
Uniprot ID
P47898
Uniprot Name
5-hydroxytryptamine receptor 5A
Molecular Weight
40254.69 Da
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Receptor signaling protein activity
Specific Function
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately e...
Gene Name
ADRB1
Uniprot ID
P08588
Uniprot Name
Beta-1 adrenergic receptor
Molecular Weight
51322.1 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Protein homodimerization activity
Specific Function
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately ...
Gene Name
ADRB2
Uniprot ID
P07550
Uniprot Name
Beta-2 adrenergic receptor
Molecular Weight
46458.32 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Histamine receptor activity
Specific Function
The H2 subclass of histamine receptors mediates gastric acid secretion. Also appears to regulate gastrointestinal motility and intestinal secretion. Possible role in regulating cell growth and diff...
Gene Name
HRH2
Uniprot ID
P25021
Uniprot Name
Histamine H2 receptor
Molecular Weight
40097.65 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Histamine receptor activity
Specific Function
The H3 subclass of histamine receptors could mediate the histamine signals in CNS and peripheral nervous system. Signals through the inhibition of adenylate cyclase and displays high constitutive a...
Gene Name
HRH3
Uniprot ID
Q9Y5N1
Uniprot Name
Histamine H3 receptor
Molecular Weight
48670.81 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Histamine receptor activity
Specific Function
The H4 subclass of histamine receptors could mediate the histamine signals in peripheral tissues. Displays a significant level of constitutive activity (spontaneous activity in the absence of agoni...
Gene Name
HRH4
Uniprot ID
Q9H3N8
Uniprot Name
Histamine H4 receptor
Molecular Weight
44495.375 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
Molecular Weight
51420.375 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
G-protein coupled acetylcholine receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM2
Uniprot ID
P08172
Uniprot Name
Muscarinic acetylcholine receptor M2
Molecular Weight
51714.605 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM3
Uniprot ID
P20309
Uniprot Name
Muscarinic acetylcholine receptor M3
Molecular Weight
66127.445 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Guanyl-nucleotide exchange factor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM4
Uniprot ID
P08173
Uniprot Name
Muscarinic acetylcholine receptor M4
Molecular Weight
53048.65 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM5
Uniprot ID
P08912
Uniprot Name
Muscarinic acetylcholine receptor M5
Molecular Weight
60073.205 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Opioid receptor activity
Specific Function
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synt...
Gene Name
OPRK1
Uniprot ID
P41145
Uniprot Name
Kappa-type opioid receptor
Molecular Weight
42644.665 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Voltage-gated calcium channel activity
Specific Function
Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone...
Gene Name
OPRM1
Uniprot ID
P35372
Uniprot Name
Mu-type opioid receptor
Molecular Weight
44778.855 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Opioid receptor activity
Specific Function
G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine n...
Gene Name
OPRD1
Uniprot ID
P41143
Uniprot Name
Delta-type opioid receptor
Molecular Weight
40368.235 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Voltage-gated cation channel activity
Specific Function
NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. This protein plays a key role in synaptic p...

Components:
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Modulator
General Function
Monoamine transmembrane transporter activity
Specific Function
Amine transporter. Terminates the action of dopamine by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name
SLC6A3
Uniprot ID
Q01959
Uniprot Name
Sodium-dependent dopamine transporter
Molecular Weight
68494.255 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Modulator
General Function
Serotonin:sodium symporter activity
Specific Function
Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into t...
Gene Name
SLC6A4
Uniprot ID
P31645
Uniprot Name
Sodium-dependent serotonin transporter
Molecular Weight
70324.165 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Molden E, Lunde H, Lunder N, Refsum H: Pharmacokinetic variability of aripiprazole and the active metabolite dehydroaripiprazole in psychiatric patients. Ther Drug Monit. 2006 Dec;28(6):744-9. doi: 10.1097/01.ftd.0000249944.42859.bf. [Article]
  2. Azuma J, Hasunuma T, Kubo M, Miyatake M, Koue T, Higashi K, Fujiwara T, Kitahara S, Katano T, Hara S: The relationship between clinical pharmacokinetics of aripiprazole and CYP2D6 genetic polymorphism: effects of CYP enzyme inhibition by coadministration of paroxetine or fluvoxamine. Eur J Clin Pharmacol. 2012 Jan;68(1):29-37. doi: 10.1007/s00228-011-1094-4. Epub 2011 Jul 8. [Article]
  3. Flockhart Table of Drug Interactions [Link]
  4. Aripiprazole Therapy and CYP2D6 Genotype [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Spina E, de Leon J: Metabolic drug interactions with newer antipsychotics: a comparative review. Basic Clin Pharmacol Toxicol. 2007 Jan;100(1):4-22. doi: 10.1111/j.1742-7843.2007.00017.x. [Article]
  2. Swainston Harrison T, Perry CM: Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder. Drugs. 2004;64(15):1715-36. [Article]
  3. Kubo M, Koue T, Inaba A, Takeda H, Maune H, Fukuda T, Azuma J: Influence of itraconazole co-administration and CYP2D6 genotype on the pharmacokinetics of the new antipsychotic ARIPIPRAZOLE. Drug Metab Pharmacokinet. 2005 Feb;20(1):55-64. [Article]
  4. Flockhart Table of Drug Interactions [Link]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da

Drug created at June 13, 2005 13:24 / Updated at March 24, 2023 20:20