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Identification
NameAripiprazole
Accession NumberDB01238  (APRD00638)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Aripiprazole is an atypical antipsychotic medication used for the treatment of schizophrenia. It has also recently received FDA approval for the treatment of acute manic and mixed episodes associated with bipolar disorder. Aripiprazole appears to mediate its antipsychotic effects primarily by partial agonism at the D2 receptor. In addition to partial agonist activity at the D2 receptor, aripiprazole is also a partial agonist at the 5-HT1A receptor, and like the other atypical antipsychotics, aripiprazole displays an antagonist profile at the 5-HT2A receptor. Aripiprazole has moderate affinity for histamine and alpha adrenergic receptors, and no appreciable affinity for cholinergic muscarinic receptors.

Structure
Thumb
Synonyms
SynonymLanguageCode
AbilifyNot AvailableNot Available
AbilitatNot AvailableNot Available
AripiprazolNot AvailableNot Available
AripiprazoleNot AvailableNot Available
AripiprazolumNot AvailableNot Available
OPC 31Not AvailableNot Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Abilifytablet2 mgoralSTAT Rx USA LLC2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet5 mgoralSTAT Rx USA LLC2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet5 mgoralRebel Distributors Corp.2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet10 mgoralRebel Distributors Corp.2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet15 mgoralRebel Distributors Corp.2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet20 mgoralRebel Distributors Corp.2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet5 mgoralREMEDYREPACK INC.2013-05-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet20 mgoralREMEDYREPACK INC.2013-04-09Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet20 mgoralREMEDYREPACK INC.2013-04-09Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet30 mgoralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-02-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet2 mgoralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-12-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet10 mgoralAphena Pharma Solutions Tennessee, Llc2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet20 mgoralAphena Pharma Solutions Tennessee, Llc2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet30 mgoralAphena Pharma Solutions Tennessee, Llc2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet10 mgoralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-02-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet5 mgoralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-02-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet15 mgoralLake Erie Medical DBA Quality Care Products LLC2010-06-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet20 mgoralLake Erie Medical Surgical & Supply DBA Quality Care Products LLC2011-07-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet5 mgoralH.J. Harkins Company, Inc.2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet10 mgoralPhysicians Total Care, Inc.2006-01-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet2 mgoralPhysicians Total Care, Inc.2011-07-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet10 mgoralCardinal Health2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet2 mgoralCardinal Health2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet5 mgoralCardinal Health2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet20 mgoralCardinal Health2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet15 mgoralCardinal Health2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet30 mgoralCardinal Health2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet10 mgoralPd Rx Pharmaceuticals, Inc.2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet2 mgoralOtsuka America Pharmaceutical, Inc.2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet5 mgoralOtsuka America Pharmaceutical, Inc.2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet10 mgoralOtsuka America Pharmaceutical, Inc.2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet15 mgoralOtsuka America Pharmaceutical, Inc.2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet20 mgoralOtsuka America Pharmaceutical, Inc.2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet30 mgoralOtsuka America Pharmaceutical, Inc.2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifysolution1 mg/mLoralOtsuka America Pharmaceutical, Inc.2004-12-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifyinjection, solution9.75 mg/1.3mLintramuscularOtsuka America Pharmaceutical, Inc.2006-09-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilify MaintenakitOtsuka America Pharmaceutical, Inc.2013-02-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilify MaintenakitOtsuka America Pharmaceutical, Inc.2013-02-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilify MaintenakitOtsuka America Pharmaceutical, Inc.2014-10-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilify MaintenakitOtsuka America Pharmaceutical, Inc.2014-10-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilify DISCMELTtablet, orally disintegrating10 mgoralOtsuka America Pharmaceutical, Inc.2006-06-07Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilify DISCMELTtablet, orally disintegrating15 mgoralOtsuka America Pharmaceutical, Inc.2006-06-07Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet2 mgoralbryant ranch prepack2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet5 mgoralbryant ranch prepack2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet10 mgoralbryant ranch prepack2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet2 mgoralTYA Pharmaceuticals2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet5 mgoralTYA Pharmaceuticals2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet15 mgoralTYA Pharmaceuticals2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet10 mgoralTYA Pharmaceuticals2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet15 mgoralCarilion Materials Management2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet5 mgoralCarilion Materials Management2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet2 mgoralCarilion Materials Management2002-11-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet2.0 mgoralBristol Myers Squibb CanadaNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Abilifytablet5.0 mgoralBristol Myers Squibb CanadaNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Abilifytablet10.0 mgoralBristol Myers Squibb CanadaNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Abilifytablet15.0 mgoralBristol Myers Squibb CanadaNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Abilifytablet20.0 mgoralBristol Myers Squibb CanadaNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Abilifytablet30.0 mgoralBristol Myers Squibb CanadaNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Abilifytablet10 mgoralREMEDYREPACK INC.2010-12-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet30 mgoralREMEDYREPACK INC.2010-12-13Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Abilifytablet15 mgoralREMEDYREPACK INC.2010-12-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Over the Counter ProductsNot Available
International Brands
NameCompany
AbilitatNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
CAS number129722-12-9
WeightAverage: 448.385
Monoisotopic: 447.148032537
Chemical FormulaC23H27Cl2N3O2
InChI KeyCEUORZQYGODEFX-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
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassDiazinanes
Sub ClassPiperazines
Direct ParentPhenylpiperazines
Alternative Parents
Substituents
  • N-arylpiperazine
  • Phenylpiperazine
  • Quinolone
  • Tetrahydroquinolone
  • Tetrahydroquinoline
  • Substituted aniline
  • Dialkylarylamine
  • 1,2-dichlorobenzene
  • N-alkylpiperazine
  • Halobenzene
  • Chlorobenzene
  • Aniline
  • Alkyl aryl ether
  • Benzenoid
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Lactam
  • Carboxamide group
  • Azacycle
  • Ether
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of schizophrenia and related psychotic disorders.
PharmacodynamicsAripiprazole is a psychotropic agent belonging to the chemical class of benzisoxazole derivatives and is indicated for the treatment of schizophrenia. Aripiprazole is a selective monoaminergic antagonist with high affinity for the serotonin Type 2 (5HT2), dopamine Type 2 (D2), 1 and 2 adrenergic, and H1 histaminergic receptors. Aripiprazole acts as an antagonist at other receptors, but with lower potency. Antagonism at receptors other than dopamine and 5HT2 with similar receptor affinities may explain some of the other therapeutic and side effects of Aripiprazole. Aripiprazole's antagonism of histamine H1 receptors may explain the somnolence observed with this drug. Aripiprazole's antagonism of adrenergic a1 receptors may explain the orthostatic hypotension observed with this drug.
Mechanism of actionAripiprazole's antipsychotic activity is likely due to a combination of antagonism at D2 receptors in the mesolimbic pathway and 5HT2A receptors in the frontal cortex. Antagonism at D2 receptors relieves positive symptoms while antagonism at 5HT2A receptors relieves negative symptoms of schizophrenia.
AbsorptionNot Available
Volume of distribution
  • 4.9 L/kg
Protein binding>99%
Metabolism

Hepatic.

Route of eliminationLess than 1% of unchanged aripiprazole was excreted in the urine and approximately 18% of the oral dose was recovered unchanged in the feces.
Half life75-146 hours
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 substrateInhibitor0.6682
CYP450 2D6 substrateInhibitor0.6633
CYP450 2C19 substrateInhibitor0.8934
CYP450 3A4 substrateInhibitor0.5256
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
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, solutionintramuscular9.75 mg/1.3mL
Kit
Solutionoral1 mg/mL
Tabletoral10 mg
Tabletoral10.0 mg
Tabletoral15 mg
Tabletoral15.0 mg
Tabletoral2 mg
Tabletoral2.0 mg
Tabletoral20 mg
Tabletoral20.0 mg
Tabletoral30 mg
Tabletoral30.0 mg
Tabletoral5 mg
Tabletoral5.0 mg
Tablet, orally disintegratingoral10 mg
Tablet, orally disintegratingoral15 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
CountryPatent NumberApprovedExpires (estimated)
United States50065281994-10-202014-10-20
United States71155872005-01-212025-01-21
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP4.5Not Available
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 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity124.34 m3·mol-1ChemAxon
Polarizability49.23 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceUS5006528
General ReferenceNot Available
External Links
ATC CodesN05AX12
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (262 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
CarbamazepineCarbamazepine, a strong CYP3A4 inducer, may decrease the serum concentration of aripiprazole by increasing its metabolism.
Dihydroquinidine barbiturateQuinidine increases the effect and toxicity of aripiprazole
EtravirineAriprazole, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to increase the dose of oral aripiprazole to maintain therapeutic efficacy, and to adjust the dose of aripiprazole appropriately when the dose of etravirine is altered.
ItraconazoleItraconazole may increase the effect of aripiprazole.
KetoconazoleKetoconazole may increase the effect of aripiprazole.
QuinidineQuinidine increases the effect and toxicity of aripiprazole
Quinidine barbiturateQuinidine increases the effect and toxicity of aripiprazole
TacrineTacrine, a central acetylcholinesterase inhibitor, may augment the central neurotoxic effect of antipsychotics such as Aripiprazole. Monitor for extrapyramidal symptoms.
TelithromycinTelithromycin may reduce clearance of Aripiprazole. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Aripiprazole if Telithromycin is initiated, discontinued or dose changed.
TerbinafineTerbinafine may reduce the metabolism and clearance of Aripiprazole. Consider alternate therapy or monitor for therapeutic/adverse effects of Aripiprazole if Terbinafine is initiated, discontinued or dose changed.
TetrabenazineMay cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
TriprolidineThe CNS depressants, Triprolidine and Aripiprazole, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
VoriconazoleVoriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of aripiprazole by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of aripiprazole if voriconazole is initiated, discontinued or dose changed.
Food Interactions
  • Avoid alcohol (possible additive effect to CNS).
  • Food has no significant effect on absorption.
  • Take without regard to meals.

Targets

1. 5-hydroxytryptamine receptor 2A

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 2A P28223 Details

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. Pubmed
  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. Pubmed
  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. Pubmed

2. D(2) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist partial agonist

Components

Name UniProt ID Details
D(2) dopamine receptor P14416 Details

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. Pubmed
  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. Pubmed
  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. Pubmed
  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. Pubmed
  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. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

3. 5-hydroxytryptamine receptor 1A

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist partial agonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1A P08908 Details

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. Pubmed
  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. Pubmed
  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. Pubmed
  4. Swainston Harrison T, Perry CM: Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder. Drugs. 2004;64(15):1715-36. Pubmed
  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. Pubmed

4. 5-hydroxytryptamine receptor 1B

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1B P28222 Details

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. Pubmed

5. 5-hydroxytryptamine receptor 1D

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1D P28221 Details

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. Pubmed

6. 5-hydroxytryptamine receptor 1E

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1E P28566 Details

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. Pubmed

7. 5-hydroxytryptamine receptor 2C

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 2C P28335 Details

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. Pubmed

8. 5-hydroxytryptamine receptor 3A

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 3A P46098 Details

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. Pubmed

9. 5-hydroxytryptamine receptor 6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 6 P50406 Details

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. Pubmed

10. 5-hydroxytryptamine receptor 7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 7 P34969 Details

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. Pubmed

11. D(1A) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist partial agonist

Components

Name UniProt ID Details
D(1A) dopamine receptor P21728 Details

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. Pubmed

12. D(1B) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist partial agonist

Components

Name UniProt ID Details
D(1B) dopamine receptor P21918 Details

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. Pubmed

13. D(3) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist partial agonist

Components

Name UniProt ID Details
D(3) dopamine receptor P35462 Details

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. Pubmed

14. D(4) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist partial agonist

Components

Name UniProt ID Details
D(4) dopamine receptor P21917 Details

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. Pubmed

15. Histamine H1 receptor

Kind: protein

Organism: Human

Pharmacological action: no

Actions: antagonist

Components

Name UniProt ID Details
Histamine H1 receptor P35367 Details

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. Pubmed

16. Alpha-1A adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: no

Actions: antagonist

Components

Name UniProt ID Details
Alpha-1A adrenergic receptor P35348 Details

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. Pubmed

17. Alpha-1B adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: no

Actions: antagonist

Components

Name UniProt ID Details
Alpha-1B adrenergic receptor P35368 Details

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. Pubmed

18. Alpha-2A adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: no

Actions: antagonist

Components

Name UniProt ID Details
Alpha-2A adrenergic receptor P08913 Details

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. Pubmed

19. Alpha-2B adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: no

Actions: antagonist

Components

Name UniProt ID Details
Alpha-2B adrenergic receptor P18089 Details

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. Pubmed

20. Alpha-2C adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: no

Actions: antagonist other/unknown

Components

Name UniProt ID Details
Alpha-2C adrenergic receptor P18825 Details

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. Pubmed

21. Muscarinic acetylcholine receptor M1

Kind: protein

Organism: Human

Pharmacological action: no

Actions: antagonist

Components

Name UniProt ID Details
Muscarinic acetylcholine receptor M1 P11229 Details

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. Pubmed

22. Muscarinic acetylcholine receptor M2

Kind: protein

Organism: Human

Pharmacological action: no

Actions: antagonist

Components

Name UniProt ID Details
Muscarinic acetylcholine receptor M2 P08172 Details

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. Pubmed

23. Muscarinic acetylcholine receptor M3

Kind: protein

Organism: Human

Pharmacological action: no

Actions: antagonist

Components

Name UniProt ID Details
Muscarinic acetylcholine receptor M3 P20309 Details

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. Pubmed

24. Muscarinic acetylcholine receptor M4

Kind: protein

Organism: Human

Pharmacological action: no

Actions: antagonist

Components

Name UniProt ID Details
Muscarinic acetylcholine receptor M4 P08173 Details

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. Pubmed

25. Muscarinic acetylcholine receptor M5

Kind: protein

Organism: Human

Pharmacological action: no

Actions: antagonist

Components

Name UniProt ID Details
Muscarinic acetylcholine receptor M5 P08912 Details

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. Pubmed

Enzymes

1. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

2. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor inducer

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

3. Cytochrome P450 3A5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A5 P20815 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.

4. Cytochrome P450 3A7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A7 P24462 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.

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Drug created on June 13, 2005 07:24 / Updated on April 10, 2014 12:38