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
Structure for Aripiprazole (DB01238)
- 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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- Contraindications & Blackbox Warnings
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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.
- 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
- 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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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/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details Cytochrome P450 2D6 CYP2D6*3 Not Available C allele Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*4 Not Available C allele Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*5 Not Available Whole-gene deletion Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*6 Not Available 1707delT Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*7 Not Available 2935A>C Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*8 Not Available 1758G>T Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*11 Not Available 883G>C Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*12 Not Available 124G>A Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*13 Not Available CYP2D7/2D6 hybrid gene structure Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*14A Not Available 1758G>A Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*15 Not Available 137insT, 137_138insT Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*19 Not Available 2539_2542delAACT Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*20 Not Available 1973_1974insG Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*21 Not Available 2573insC Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*31 Not Available -1770G>A / -1584C>G … show all Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*36 Not Available 100C>T / -1426C>T … show all Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*38 Not Available 2587_2590delGACT Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*40 Not Available 1863_1864ins(TTT CGC CCC)2 Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*42 Not Available 3259_3260insGT Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*44 Not Available 2950G>C Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*47 Not Available 100C>T / -1426C>T … show all Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*51 Not Available -1584C>G / -1235A>G … show all Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*56 Not Available 3201C>T Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*57 Not Available 100C>T / 310G>T … show all Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*62 Not Available 4044C>T Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*68A Not Available -1426C>T / -1235A>G … show all Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*68B Not Available Similar but not identical switch region compared to CYP2D6*68A. Found in tandem arrangement with CYP2D6*4. Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*69 Not Available 2988G>A / -1426C>T … show all Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*92 Not Available 1995delC Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*100 Not Available -1426C>T / -1235A>G … show all Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*101 Not Available -1426C>T / -1235A>G … show all Effect Inferred Poor 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.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of adverse effects can be increased when Aripiprazole is combined with 1,2-Benzodiazepine. Abaloparatide Aripiprazole may increase the hypotensive activities of Abaloparatide. Abametapir The serum concentration of Aripiprazole can be increased when it is combined with Abametapir. Abatacept The metabolism of Aripiprazole can be increased when combined with Abatacept. Abiraterone The metabolism of Aripiprazole can be decreased when combined with Abiraterone. Acalabrutinib The metabolism of Aripiprazole can be decreased when combined with Acalabrutinib. Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Aripiprazole. Acebutolol The risk or severity of hypotension can be increased when Aripiprazole is combined with Acebutolol. Aceclofenac The risk or severity of hypertension can be increased when Aripiprazole is combined with Aceclofenac. Acemetacin The risk or severity of hypertension can be increased when Aripiprazole is combined with Acemetacin. 
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- 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
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Images
- International/Other Brands
- Abilitat
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Abilify Tablet 30 mg Oral Otsuka Pharmaceutical Netherlands B.V. 2021-01-12 Not applicable EU 
Abilify Tablet 15 mg/1 Oral Rebel Distributors 2002-11-15 Not applicable US 
Abilify Tablet 30 mg/1 Oral Remedy Repack 2010-12-13 2014-06-21 US Abilify Tablet 5 mg/1 Oral Cardinal Health 2002-11-15 2017-09-30 US 
Abilify Tablet 15 mg/1 Oral Otsuka America Pharmaceutical, Inc. 2002-11-15 Not applicable US Abilify Tablet 5 mg Oral Otsuka Pharmaceutical Netherlands B.V. 2021-01-12 Not applicable EU Abilify Tablet, orally disintegrating 30 mg Oral Otsuka Pharmaceutical Netherlands B.V. 2021-01-12 Not applicable EU Abilify Tablet 10 mg/1 Oral Aphena Pharma Solutions Tennessee, Inc. 2002-11-15 Not applicable US Abilify Tablet 2 mg/1 Oral Otsuka America Pharmaceutical, Inc. 2002-11-15 Not applicable US Abilify Tablet 15 mg Oral Otsuka Pharmaceutical Co., Ltd. 2009-09-30 Not applicable Canada 
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-aripiprazole Tablet 15 mg Oral Apotex Corporation 2018-04-10 Not applicable Canada Apo-aripiprazole Tablet 2 mg Oral Apotex Corporation 2018-04-10 Not applicable Canada Apo-aripiprazole Tablet 30 mg Oral Apotex Corporation 2018-04-10 Not applicable Canada Apo-aripiprazole Tablet 10 mg Oral Apotex Corporation 2018-04-10 Not applicable Canada Apo-aripiprazole Tablet 20 mg Oral Apotex Corporation 2018-04-10 Not applicable Canada Apo-aripiprazole Tablet 5 mg Oral Apotex Corporation 2018-04-10 Not applicable Canada Aripiprazole Tablet 30 mg/1 Oral Major Pharmaceuticals 2015-08-25 Not applicable US Aripiprazole Tablet 2 mg/1 Oral Major Pharmaceuticals 2015-04-28 2015-04-28 US Aripiprazole Tablet 20 mg/1 Oral Camber Pharmaceuticals, Inc. 2015-04-28 Not applicable US Aripiprazole Solution 1 mg/1mL Oral Aurobindo Pharma Limited 2019-01-29 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Abilify Aripiprazole (15 mg/1) Tablet Oral Remedy Repack 2010-12-14 2014-08-27 US Abilify Aripiprazole (20 mg/1) Tablet Oral Remedy Repack 2013-04-09 2014-08-12 US Abilify Aripiprazole (10 mg/1) Tablet Oral Remedy Repack 2010-12-14 2015-05-20 US Abilify Aripiprazole (30 mg/1) Tablet Oral Remedy Repack 2010-12-13 2014-06-21 US CUREXOL 5 MG TABLET, 28 ADET Aripiprazole (5 mg) Tablet Oral ACTAVİS İLAÇLARI A.Ş. 2020-08-14 Not applicable Turkey 
Categories
- ATC Codes
- N05AX12 — Aripiprazole
- Drug Categories
- Adrenergic alpha-1 Receptor Antagonists
- Adrenergic alpha-Antagonists
- Adrenergic Antagonists
- Agents producing tachycardia
- Agents that produce hypertension
- Anticholinergic Agents
- Antidepressive Agents
- Antidepressive Agents Indicated for Depression
- Antipsychotic Agents
- Antipsychotic Agents (Second Generation [Atypical])
- Aripiprazole and prodrugs
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A7 Substrates
- Cytochrome P-450 Substrates
- Dopamine Agents
- Dopamine Agonists
- Dopamine Antagonists
- Dopamine D2 Receptor Antagonists
- Heterocyclic Compounds, Fused-Ring
- Histamine Antagonists
- Histamine H1 Antagonists
- Hyperglycemia-Associated Agents
- Muscarinic Antagonists
- Nervous System
- Neurotoxic agents
- Neurotransmitter Agents
- Piperazines
- Potential QTc-Prolonging Agents
- Psycholeptics
- Psychotropic Drugs
- QTc Prolonging Agents
- QTc shortening agents
- Quinolines
- Quinolones
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin 5-HT1 Receptor Agonists
- Serotonin 5-HT1 Receptor Antagonists
- Serotonin 5-HT1D Receptor Antagonists
- Serotonin 5-HT2 Receptor Antagonists
- Serotonin 5-HT2A Receptor Antagonists
- Serotonin 5-HT2C Receptor Antagonists
- Serotonin Agents
- Serotonin Receptor Agonists
- Serotonin Receptor Antagonists
- Tranquilizing Agents
- 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
- 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]
- 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]
- 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]
- Prommer E: Aripiprazole. Am J Hosp Palliat Care. 2017 Mar;34(2):180-185. doi: 10.1177/1049909115612800. Epub 2016 Jul 10. [Article]
- FDA Drug Approval Package: Aripiprazole [Link]
- Clinicaltrails.gov: National Pregnancy Registry for Atypical Antipsychotics [Link]
- External Links
- Human Metabolome Database
- HMDB0005042
- KEGG Drug
- D01164
- KEGG Compound
- C12564
- PubChem Compound
- 60795
- PubChem Substance
- 46505745
- ChemSpider
- 54790
- BindingDB
- 50130293
- 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
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Dementia / Depression / Geriatric Depression / Late Life Depression (LLD) / Major Depressive Disorder (MDD) / Major depressive disorder, recurrent episode / Mild Cognitive Impairment (MCI) / Treatment-Refractory Depression 1 4 Completed Basic Science CYP3A4 Protein, Human / Cytochrome P-450 CYP2D6 / Pharmacokinetics 1 4 Completed Basic Science Diabetes 2 4 Completed Basic Science Psychosis / Schizophrenia 1 4 Completed Health Services Research First Episode Psychosis (FEP) / Schizoaffective Disorders / Schizophrenia 1 4 Completed Health Services Research Schizophrenia 1 4 Completed Prevention Schizophrenia 1 4 Completed Supportive Care Autism Disorder 1 4 Completed Treatment Adherence, Medication / Bipolar Disorder (BD) / Nonadherence, Medication 1 4 Completed Treatment Aggression / Attention Deficit Hyperactivity Disorder (ADHD) / Bipolar Disorder (BD) / Defiant Disorder, Oppositional / Pervasive Development Disorder 1
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
Form Route Strength Injection Injection, solution Intramuscular 7.5 MG/ML Injection, solution Intramuscular 9.75 mg/1.3mL Solution Oral Tablet Oral 10 mg/1 Tablet Oral 15 mg/1 Tablet Oral 2 mg/1 Tablet Oral 20 mg/1 Tablet Oral 30 mg/1 Tablet Oral 5 mg/1 Tablet, orally disintegrating Oral 5 MG Injection, solution Intramuscular Injection, powder, for suspension, extended release Intramuscular 300 mg / syr Injection, powder, for suspension, extended release Intramuscular 300 mg Injection, powder, for suspension, extended release Intramuscular 400 mg / syr Injection, powder, for suspension, extended release Intramuscular 400 mg Injection, powder, for suspension, extended release Intramuscular; Parenteral 300 MG Injection, powder, for suspension, extended release Intramuscular; Parenteral 400 MG Injection, powder, for suspension, extended release; kit Intramuscular 300 mg / vial Injection, powder, for suspension, extended release; kit Intramuscular 400 mg / vial Injection, powder, lyophilized, for suspension, extended release Intramuscular 300 mg/1.5mL Injection, powder, lyophilized, for suspension, extended release Intramuscular 400 mg/2.0mL Injection, suspension, extended release; kit Intramuscular 300 mg/1.5mL Injection, suspension, extended release; kit Intramuscular 400 mg/1.9mL Injection, powder, for suspension Intramuscular 300 mg/1vial Injection, powder, for suspension Intramuscular 400 mg/1vial Injection, suspension, extended release Intramuscular Injection, powder, for suspension Intramuscular Injection, suspension, extended release Intramuscular 400 mg Injection, powder, for suspension, extended release Intramuscular 400 mg/vial Solution Oral 1.0 mg/ml Tablet Oral 10.0 mg Tablet Oral 2 mg Tablet Oral 5.0 mg Tablet Oral 20 mg Tablet Oral 10 mg Tablet Oral 15 mg Tablet, orally disintegrating Oral 10 mg Tablet, orally disintegrating Oral 15 mg Tablet Oral Tablet Oral 5 mg Tablet, soluble Buccal Tablet, orally disintegrating Oral Solution Oral 1 mg/1mL Tablet, orally disintegrating Oral 10 mg/1 Tablet, orally disintegrating Oral 15 mg/1 Tablet, orally disintegrating Oral 20 mg/1 Tablet, orally disintegrating Oral 30 mg/1 Tablet, soluble Oral Solution Oral 1 MG/ML Tablet, orally disintegrating Oral 30 MG Tablet Oral 30 mg Solution Oral 100 mg Solution Oral 1 mg Tablet, soluble Buccal 15 mg Tablet, coated Oral 10 mg Tablet, coated Oral 15 mg Tablet, coated Oral 5 mg - Prices
Unit description Cost Unit Abilify Discmelt 30 10 mg Dispersible Tablet Box 636.3USD box Abilify 30 mg tablet 32.12USD tablet Abilify 15 mg tablet 26.07USD tablet Abilify 10 mg tablet 23.53USD tablet Abilify 5 mg tablet 23.53USD tablet Abilify 2 mg tablet 22.25USD tablet Abilify 20 mg tablet 21.99USD tablet Abilify discmelt 10 mg tablet 20.39USD tablet Abilify discmelt 15 mg tablet 20.39USD tablet Abilify 9.7 mg/1.3 ml vial 16.04USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5006528 No 1991-04-09 2014-10-20 US US7053092 No 2006-05-30 2022-01-28 US US8642600 Yes 2014-02-04 2022-07-28 US US8759350 No 2014-06-24 2027-03-02 US US9125939 No 2015-09-08 2026-07-28 US US9089567 No 2015-07-28 2022-01-28 US US8017615 Yes 2011-09-13 2024-12-16 US US8580796 Yes 2013-11-12 2023-03-25 US US8642760 Yes 2014-02-04 2023-03-25 US US6977257 Yes 2005-12-20 2022-10-24 US US8518421 Yes 2013-08-27 2021-07-24 US US7115587 Yes 2006-10-03 2025-01-21 US US7550445 Yes 2009-06-23 2025-01-21 US US8030313 No 2011-10-04 2024-10-19 US US8338427 No 2012-12-25 2025-03-15 US US8338428 No 2012-12-25 2023-08-06 US US8759351 No 2014-06-24 2023-08-06 US US7807680 No 2010-10-05 2024-10-19 US US8993761 No 2015-03-31 2022-09-25 US US8722679 No 2014-05-13 2024-10-19 US US8399469 No 2013-03-19 2025-06-29 US US9193685 No 2015-11-24 2033-10-24 US US8796276 No 2014-08-05 2030-06-24 US US9034867 No 2015-05-19 2032-11-07 US US8431576 No 2013-04-30 2030-10-26 US US9387182 No 2016-07-12 2023-12-25 US US9359302 No 2016-06-07 2022-09-25 US US9358207 No 2016-06-07 2020-04-12 US US9526726 No 2016-12-27 2035-03-19 US US9452131 No 2016-09-27 2035-03-19 US US8945005 No 2015-02-03 2029-08-19 US US8847766 No 2014-09-30 2030-03-29 US US9787511 No 2017-10-10 2034-09-19 US US8674825 No 2014-03-18 2029-04-09 US US9270503 No 2016-02-23 2034-09-19 US US9268909 No 2016-02-23 2033-10-15 US US8956288 No 2015-02-17 2029-07-06 US US9444503 No 2016-09-13 2027-11-19 US US8547248 No 2013-10-01 2030-12-18 US US9577864 No 2017-02-21 2033-10-03 US US8545402 No 2013-10-01 2030-04-27 US US9433371 No 2016-09-06 2029-09-15 US US8114021 No 2012-02-14 2026-11-02 US US9320455 No 2016-04-26 2031-12-15 US US9119554 No 2015-09-01 2028-12-16 US US9258035 No 2016-02-09 2029-03-05 US US8258962 No 2012-09-04 2030-11-25 US US7978064 No 2011-07-12 2026-09-14 US US8718193 No 2014-05-06 2029-12-05 US US8961412 No 2015-02-24 2030-11-17 US US9060708 No 2015-06-23 2029-03-05 US US9149577 No 2015-10-06 2029-12-15 US US9941931 No 2018-04-10 2030-11-04 US US10097388 No 2018-10-09 2034-09-19 US US10441194 No 2019-10-15 2029-05-12 US US10525057 No 2020-01-07 2034-03-08 US US10517507 No 2019-12-31 2032-06-13 US US10980803 No 2021-04-20 2033-09-24 US US11154553 No 2021-10-26 2033-09-24 US US11229378 No 2011-07-11 2031-07-11 US US11344547 No 2013-09-24 2033-09-24 US US11400087 No 2013-09-24 2033-09-24 US US11476952 No 2006-04-28 2026-04-28 US US11464423 No 2010-09-15 2030-09-15 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 137-140 http://www.chemspider.com/Chemical-Structure.54790.html water solubility 0.00001% https://medsafe.govt.nz/profs/Datasheet/a/Abilifytab.pdf pKa 7.6 https://medsafe.govt.nz/profs/Datasheet/a/Abilifytab.pdf - Predicted Properties
Property Value Source Water Solubility 0.00777 mg/mL ALOGPS logP 5.21 ALOGPS logP 4.9 Chemaxon logS -4.8 ALOGPS pKa (Strongest Acidic) 13.51 Chemaxon pKa (Strongest Basic) 7.46 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 44.81 Å2 Chemaxon Rotatable Bond Count 7 Chemaxon Refractivity 124.34 m3·mol-1 Chemaxon Polarizability 49.23 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9934 Blood Brain Barrier + 0.992 Caco-2 permeable + 0.5 P-glycoprotein substrate Substrate 0.7431 P-glycoprotein inhibitor I Inhibitor 0.9585 P-glycoprotein inhibitor II Inhibitor 0.9321 Renal organic cation transporter Inhibitor 0.5175 CYP450 2C9 substrate Non-substrate 0.8663 CYP450 2D6 substrate Substrate 0.8918 CYP450 3A4 substrate Substrate 0.7408 CYP450 1A2 substrate Inhibitor 0.6581 CYP450 2C9 inhibitor Inhibitor 0.6682 CYP450 2D6 inhibitor Inhibitor 0.6633 CYP450 2C19 inhibitor Inhibitor 0.8934 CYP450 3A4 inhibitor Inhibitor 0.5256 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.9104 Ames test Non AMES toxic 0.6124 Carcinogenicity Non-carcinogens 0.8765 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.8894 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.62 hERG inhibition (predictor II) Inhibitor 0.8814
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available LC-MS/MS Spectrum - LC-ESI-qTof , Positive LC-MS/MS Not Available MS/MS Spectrum - , positive LC-MS/MS splash10-0f72-0340900000-34d93478ad0d9f5cf2b0 MS/MS Spectrum - , positive LC-MS/MS splash10-000i-3970100000-6b98b53e8175df39986e
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- AntagonistPartial 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
- Hirose T, Kikuchi T: Aripiprazole, a novel antipsychotic agent: dopamine D2 receptor partial agonist. J Med Invest. 2005 Nov;52 Suppl:284-90. [Article]
- 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]
- 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]
- 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]
- 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]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- 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
- AntagonistPartial 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
- 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]
- 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]
- 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]
- 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
- 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]
- 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]
- 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]
- Swainston Harrison T, Perry CM: Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder. Drugs. 2004;64(15):1715-36. [Article]
- 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]
- 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
- 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]
- 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
- 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]
- 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
- AntagonistPartial 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
- 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]
- 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
- AntagonistLigand
- 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
- 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]
- 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
- AntagonistPartial 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
- 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]
- 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
- 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]
- 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
- AntagonistOther/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
- 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]
- 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
- 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
- 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]
- 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
- AntagonistLigand
- 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
- 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]
- 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
- AntagonistPartial 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
- 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]
- 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
- 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
- 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]
- 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
- AntagonistPartial agonistLigand
- 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
- 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]
- 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
- AntagonistPartial 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
- 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]
- 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
- AntagonistLigand
- 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
- 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]
- 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
- AntagonistLigand
- 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
- 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]
- 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
- AntagonistPartial agonistLigand
- 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
- 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]
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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]
- 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]
- Flockhart Table of Drug Interactions [Link]
- 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
- 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
- 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
- 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]
- Swainston Harrison T, Perry CM: Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder. Drugs. 2004;64(15):1715-36. [Article]
- 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]
- 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