Identification

Name
Aripiprazole
Accession Number
DB01238  (APRD00638)
Type
Small Molecule
Groups
Approved, 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
  • Aripiprazol
  • Aripiprazole
  • Aripiprazolum
External IDs
OPC 31 / OPC-14597 / OPC-31
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AbilifyTablet5 mg/1OralH.J. Harkins Company2002-11-15Not applicableUs
AbilifyTablet30 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2012-02-172014-12-31Us
AbilifyTablet5 mg/1OralCardinal Health2002-11-152017-09-30Us55154 202920180913 8702 10b5lo1
AbilifyTablet2 mgOralOtsuka Pharmaceutical Co., Ltd.2009-09-30Not applicableCanada
AbilifyTablet, orally disintegrating15 mg/1OralOtsuka Pharmaceutical Co., Ltd.2006-06-07Not applicableUs
AbilifyTablet20 mgOralOtsuka Pharmaceutical Co., Ltd.2009-09-30Not applicableCanada
AbilifyTablet5 mg/1Oralbryant ranch prepack2002-11-15Not applicableUs63629 338720180907 15195 5eot3c
AbilifyTablet15 mg/1OralCarilion Materials Management2002-11-15Not applicableUs68151 446120180907 15195 bygs5j
AbilifyTablet20 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2011-07-28Not applicableUs
AbilifyTablet30 mg/1OralAphena Pharma Solutions Tennessee, Inc.2002-11-15Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-aripiprazoleTablet30 mgOralApotex Corporation2018-04-10Not applicableCanada
Apo-aripiprazoleTablet10 mgOralApotex Corporation2018-04-10Not applicableCanada
Apo-aripiprazoleTablet20 mgOralApotex Corporation2018-04-10Not applicableCanada
Apo-aripiprazoleTablet5 mgOralApotex Corporation2018-04-10Not applicableCanada
Apo-aripiprazoleTablet15 mgOralApotex Corporation2018-04-10Not applicableCanada
Apo-aripiprazoleTablet2 mgOralApotex Corporation2018-04-10Not applicableCanada
AripiprazoleTablet5 mg/1OralRemedy Repack2018-01-22Not applicableUs
AripiprazoleTablet, orally disintegrating10 mg/1OralAlembic Pharmaceuticals Limited2016-07-07Not applicableUs
AripiprazoleTablet15 mg/1OralTorrent Pharmaceuticals Limited2015-04-28Not applicableUs
AripiprazoleTablet30 mg/1OralRemedy Repack2018-07-13Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
AbilifyAripiprazole (10 mg/1)TabletOralRemedy Repack2010-12-142015-05-20Us
AbilifyAripiprazole (30 mg/1)TabletOralRemedy Repack2010-12-132014-06-21Us
AbilifyAripiprazole (15 mg/1)TabletOralRemedy Repack2010-12-142014-08-27Us
AbilifyAripiprazole (20 mg/1)TabletOralRemedy Repack2013-04-092014-08-12Us
International/Other Brands
Abilify / Abilitat
Categories
UNII
82VFR53I78
CAS number
129722-12-9
Weight
Average: 448.385
Monoisotopic: 447.148032537
Chemical Formula
C23H27Cl2N3O2
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

Pharmacology

Indication

For the treatment of schizophrenia and related psychotic disorders.

Associated Conditions
Pharmacodynamics

Aripiprazole 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 action

Aripiprazole'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.

TargetActionsOrganism
A5-hydroxytryptamine receptor 2A
antagonist
Human
AD(2) dopamine receptor
antagonist
partial agonist
Human
U5-hydroxytryptamine receptor 1A
antagonist
partial agonist
Human
U5-hydroxytryptamine receptor 1B
antagonist
Human
U5-hydroxytryptamine receptor 1D
antagonist
Human
U5-hydroxytryptamine receptor 1E
antagonist
Human
U5-hydroxytryptamine receptor 2C
antagonist
Human
U5-hydroxytryptamine receptor 3A
antagonist
Human
U5-hydroxytryptamine receptor 6
antagonist
Human
U5-hydroxytryptamine receptor 7
antagonist
Human
UD(1A) dopamine receptor
antagonist
partial agonist
Human
UD(1B) dopamine receptor
antagonist
partial agonist
Human
UD(3) dopamine receptor
antagonist
partial agonist
Human
UD(4) dopamine receptor
antagonist
partial agonist
Human
NHistamine H1 receptor
antagonist
Human
NAlpha-1A adrenergic receptor
antagonist
Human
NAlpha-1B adrenergic receptor
antagonist
Human
NAlpha-2A adrenergic receptor
antagonist
Human
NAlpha-2B adrenergic receptor
antagonist
Human
NAlpha-2C adrenergic receptor
antagonist
other/unknown
Human
NMuscarinic acetylcholine receptor M1
antagonist
Human
NMuscarinic acetylcholine receptor M2
antagonist
Human
NMuscarinic acetylcholine receptor M3
antagonist
Human
NMuscarinic acetylcholine receptor M4
antagonist
Human
NMuscarinic acetylcholine receptor M5
antagonist
Human
Absorption
Not Available
Volume of distribution
  • 4.9 L/kg
Protein binding

>99%

Metabolism

Hepatic.

Route of elimination

Less than 1% of unchanged aripiprazole was excreted in the urine and approximately 18% of the oral dose was recovered unchanged in the feces.

Half life

75-146 hours

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

Interactions

Drug Interactions
DrugInteraction
(1S,6R)-3-{[3-(TRIFLUOROMETHYL)-5,6-DIHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL]CARBONYL}-6-(2,4,5-TRIFLUOROPHENYL)CYCLOHEX-3-EN-1-AMINEThe therapeutic efficacy of (1S,6R)-3-{[3-(TRIFLUOROMETHYL)-5,6-DIHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL]CARBONYL}-6-(2,4,5-TRIFLUOROPHENYL)CYCLOHEX-3-EN-1-AMINE can be decreased when used in combination with Aripiprazole.
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Aripiprazole.
2,5-Dimethoxy-4-ethylamphetamineAripiprazole may decrease the stimulatory activities of 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineAripiprazole may decrease the stimulatory activities of 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-MethylenedioxyamphetamineAripiprazole may decrease the stimulatory activities of 3,4-Methylenedioxyamphetamine.
4-Bromo-2,5-dimethoxyamphetamineAripiprazole may decrease the stimulatory activities of 4-Bromo-2,5-dimethoxyamphetamine.
4-MethoxyamphetamineAripiprazole may decrease the vasoconstricting activities of 4-Methoxyamphetamine.
7-NitroindazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with 7-Nitroindazole.
AbirateroneThe serum concentration of Aripiprazole can be increased when it is combined with Abiraterone.
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Aripiprazole.
Food Interactions
  • Avoid alcohol (possible additive effect to CNS).
  • Food has no significant effect on absorption.
  • Take without regard to meals.

References

Synthesis Reference
US5006528
General References
Not Available
External Links
Human Metabolome Database
HMDB0005042
KEGG Drug
D01164
KEGG Compound
C12564
PubChem Compound
60795
PubChem Substance
46505745
ChemSpider
54790
BindingDB
50130293
ChEBI
31236
ChEMBL
CHEMBL1112
Therapeutic Targets Database
DAP000076
PharmGKB
PA10026
IUPHAR
34
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Aripiprazole
ATC Codes
N05AX12 — Aripiprazole
AHFS Codes
  • 28:16.08.04 — Atypical Antipsychotics
FDA label
Download (262 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableBipolar Disorder (BD)1
1CompletedNot AvailableDepressive Disorders1
1CompletedNot AvailableHealthy Volunteers2
1CompletedNot AvailableHuman Immunodeficiency Virus (HIV) Infections2
1CompletedNot AvailableSchizophrenic Disorders1
1CompletedBasic ScienceAlzheimer's Disease (AD)1
1CompletedBasic ScienceBipolar Disorder (BD) / Depressive Disorders / Psychotic Disorder NOS / Schizophrenic Disorders1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedBasic ScienceSchizophrenic Disorders1
1CompletedOtherAntipsychotics / Immunoassay1
1CompletedSupportive CareSchizophrenic Disorders1
1CompletedTreatmentCocaine-Related Disorders1
1CompletedTreatmentHealthy Male Adults1
1CompletedTreatmentNervous System Diseases / Psychiatric Disorder NOS / Schizophrenic Disorders1
1CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
1CompletedTreatmentSchizophrenic Disorders5
1Not Yet RecruitingOtherSchizophrenic Disorders1
1RecruitingOtherSchizophrenic Disorders1
1Unknown StatusTreatmentAmphetamine-Related Disorders1
1, 2RecruitingBasic ScienceSchizophrenic Disorders1
2CompletedTreatmentAcute Schizophrenia / Schizoaffective Disorders1
2CompletedTreatmentAlcohol Dependence1
2CompletedTreatmentAsperger's Disorder / Autism, Early Infantile / Pervasive Developmental Disorder NOS1
2CompletedTreatmentAsperger's Disorder / Pervasive Developmental Disorder NOS1
2CompletedTreatmentAsperger's Syndrome / Autism Spectrum Conditions/Disorders / Autistic Disorder1
2CompletedTreatmentAutism, Early Infantile1
2CompletedTreatmentBehavioral Problems Associated With Fragile X Syndrome / Fragile X Syndrome (FXS)1
2CompletedTreatmentBipolar I Disorder / Major Depressive Disorder (MDD) / Schizophrenic Disorders1
2CompletedTreatmentCocaine Abuse1
2CompletedTreatmentDepression1
2CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Substance Abuse1
2CompletedTreatmentMania / Schizophrenic Disorders1
2CompletedTreatmentPTSD1
2CompletedTreatmentSchizophrenic Disorders3
2RecruitingTreatmentAutism Spectrum Conditions/Disorders1
2RecruitingTreatmentSchizophrenic Disorders1
2TerminatedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)1
2TerminatedTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
2Unknown StatusTreatmentDependence, Cocaine / Schizophrenic Disorders1
2WithdrawnTreatmentBipolar 1 Disorder / Nervous System Diseases / Psychiatric Disorder NOS / Schizophrenic Disorders1
2, 3CompletedTreatmentAlcohol Dependence1
2, 3CompletedTreatmentPsychosis / Schizophrenic Disorders1
2, 3CompletedTreatmentSchizophrenic Disorders2
2, 3Not Yet RecruitingTreatmentPharmacotherapy / Schizophrenia and Related Disorders / Stimulant Abuse / Stimulant Dependence / Stimulant Use With Stimulant-Induced Psychotic Disorder (Diagnosis)1
2, 3TerminatedTreatmentSchizophrenic Disorders1
2, 3WithdrawnTreatmentDiabetes Mellitus (DM)1
3Active Not RecruitingTreatmentPsychotic Disorder NOS / Schizophrenic Disorders1
3Active Not RecruitingTreatmentSchizophrenic Disorders1
3CompletedNot AvailableSchizophrenia and Schizoaffective Disorder1
3CompletedDiagnosticMajor Depressive Disorder (MDD)2
3CompletedPreventionBipolar Disorder (BD)1
3CompletedTreatmentAlcohol Dependence1
3CompletedTreatmentAlzheimer's Disease (AD)2
3CompletedTreatmentAlzheimer's Disease (AD) / Dementias1
3CompletedTreatmentAutistic Disorder4
3CompletedTreatmentAutistic Disorder / Behavioral Symptoms2
3CompletedTreatmentBipolar Disorder (BD)9
3CompletedTreatmentBipolar Disorder (BD) / Schizophrenic Disorders1
3CompletedTreatmentBipolar Disorder Mania1
3CompletedTreatmentBipolar I1
3CompletedTreatmentBipolar I Disorder6
3CompletedTreatmentBody Weight Changes / Psychotic Disorder NOS / Schizoaffective Disorders / Schizophrenic Disorders1
3CompletedTreatmentChronic Motor or Vocal Tic Disorder / Tourette's Disorder1
3CompletedTreatmentDementia, Alzheimer Type1
3CompletedTreatmentMajor Depressive Disorder (MDD)6
3CompletedTreatmentPervasive Developmental Disorder NOS1
3CompletedTreatmentPostpartum Depression1
3CompletedTreatmentPosttraumatic Stress Disorders1
3CompletedTreatmentPsychotic Depression1
3CompletedTreatmentPsychotic Disorder NOS / Schizophrenic Disorders1
3CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders2
3CompletedTreatmentSchizophrenia and Schizoaffective Disorder1
3CompletedTreatmentSchizophrenic Disorders20
3CompletedTreatmentTic Disorders / Tourette's Disorder2
3CompletedTreatmentTourette's Disorder3
3RecruitingTreatmentAlcohol Abuse / Alcoholism / Bipolar Disorder (BD)1
3RecruitingTreatmentAutistic Disorder1
3RecruitingTreatmentDepression, Bipolar1
3RecruitingTreatmentGilles de la Tourette's Syndrome1
3RecruitingTreatmentSchizophrenic Disorders3
3TerminatedTreatmentAcute Depressive Episode / Bipolar Disorder (BD)1
3TerminatedTreatmentAdolescent Schizophrenia / Child or Adolescent Bipolar I Disorder, Manic or Mixed Episode With or Without Psychotic Features1
3TerminatedTreatmentAgitation Associated With Dementia of the Alzheimer's Type1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
3TerminatedTreatmentBipolar Disorder (BD) / Schizoaffective Disorders / Schizophrenic Disorders1
3TerminatedTreatmentBipolar I Disorder / Metabolic Syndromes / Schizoaffective Disorders / Schizophrenic Disorders1
3TerminatedTreatmentMajor Depressive Disorder (MDD)3
3TerminatedTreatmentSchizophrenic Disorders3
3TerminatedTreatmentTherapy-Resistant Depression1
3Unknown StatusTreatmentAnorexia Nervosa (AN)1
3Unknown StatusTreatmentPsychosis Nos/Other1
3WithdrawnTreatmentBipolar Disorder (BD)1
4CompletedNot AvailableBipolar Disorder (BD) / Schizophrenic Disorders1
4CompletedNot AvailableMoods Disorders / Schizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorder1
4CompletedBasic ScienceCYP3A4 Protein, Human / Cytochrome P-450 CYP2D6 / Pharmacokinetics1
4CompletedBasic ScienceDiabetes Mellitus (DM)2
4CompletedBasic SciencePsychosis / Schizophrenic Disorders1
4CompletedPreventionSchizophrenic Disorders1
4CompletedSupportive CareAutistic Disorder1
4CompletedTreatmentAggressive Behavior / Attention Deficit Disorder With Hyperactivity (ADHD) / Attention Deficit-Hyperactivity / Bipolar Disorder (BD) / Oppositional Defiant Disorder / PDD / Pervasive Development Disorders1
4CompletedTreatmentAlcoholism1
4CompletedTreatmentAlzheimer's Disease (AD) / Dementias / Schizophrenic Disorders1
4CompletedTreatmentAnxiety Disorders / Bipolar Disorder (BD) / Major Depressive Disorder (MDD) / Schizoaffective Disorders / Schizophrenic Disorders / Substance Abuse1
4CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)1
4CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Bipolar Disorder (BD)1
4CompletedTreatmentAutism Spectrum Conditions/Disorders1
4CompletedTreatmentBMI >27 kg/m2 / Cardiovascular Disease (CVD) / Hyperlipidemias1
4CompletedTreatmentBipolar Disorder (BD)7
4CompletedTreatmentBipolar Disorder (BD) / Mania1
4CompletedTreatmentBipolar Disorder (BD) / Metabolic Complications1
4CompletedTreatmentBipolar Disorder (BD) / Metabolic Syndromes / Schizoaffective Disorders / Schizophrenic Disorders1
4CompletedTreatmentDSM-IV Schizophrenia / Schizoaffective Disorders1
4CompletedTreatmentDepression, Bipolar2
4CompletedTreatmentEating Disorders1
4CompletedTreatmentFirst Episode Psychosis1
4CompletedTreatmentGeneralized Anxiety Disorder (GAD) / Panic Disorders1
4CompletedTreatmentGilles de la Tourette's Syndrome / Tic Disorders1
4CompletedTreatmentInsulin Resistance / Schizophrenic Disorders1
4CompletedTreatmentIrritability Associated With Autistic Disorder1
4CompletedTreatmentMajor Depressive Disorder (MDD)3
4CompletedTreatmentOppositional Defiant Disorder1
4CompletedTreatmentParkinson's Disease (PD) / Psychosis1
4CompletedTreatmentPsychotic Disorder NOS1
4CompletedTreatmentPsychotic Disorder NOS / Schizophrenic Disorders5
4CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders5
4CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders / Social Anxiety Disorder (SAD)1
4CompletedTreatmentSchizophrenic Disorders19
4CompletedTreatmentSchizophrenic Disorders / Type 2 Diabetes Mellitus1
4CompletedTreatmentIdiopathic hyperprolactinemic disorder1
4Enrolling by InvitationTreatmentPsychosis / Psychotic Disorder NOS / Schizophrenic Disorders1
4Enrolling by InvitationTreatmentPsychotic Disorder NOS / Schizophrenic Disorders1
4Not Yet RecruitingTreatmentAcute Schizophrenia Episode1
4Not Yet RecruitingTreatmentDiagnosis and Treatment of Depression1
4Not Yet RecruitingTreatmentSchizophrenic Disorders2
4Not Yet RecruitingTreatmentTourette's Disorder (TD)1
4RecruitingDiagnosticAsthma Bronchial / Asthma: [Nos] or [Attack] / Major Depressive Disorder (MDD)1
4RecruitingDiagnosticFirst Episode Psychosis / Schizoaffective Disorders / Schizophrenic Disorders1
4RecruitingOtherAttenuated Psychosis Syndrome1
4RecruitingTreatmentAntipsychotics Weight Gain1
4RecruitingTreatmentAntipsychotics / Aripiprazole / LAI / Long-Acting Injection / Schizophrenic Disorders1
4RecruitingTreatmentBipolar Disorder (BD) / Medication Adherence / Medication Non Adherence1
4RecruitingTreatmentGeriatric Depression / Late Life Depression (LLD) / Major Depressive Disorder (MDD) / Treatment Resistant Depression (TRD) / Treatment-Refractory Depression1
4RecruitingTreatmentMajor Depressive Disorder (MDD)1
4RecruitingTreatmentSchizophrenic Disorders2
4RecruitingTreatmentTreatment Resistant Major Depressive Disorder / Treatment Resistant Major Depressive Disorder Depression1
4TerminatedNot AvailableHigh Risk MC4R Genotype / Low Risk MC4R Genotype / One Week or Less Antipsychotic Lifetime Exposure1
4TerminatedTreatmentMajor Depressive Disorder (MDD)1
4TerminatedTreatmentMetabolic Syndromes / Schizophrenic Disorders1
4TerminatedTreatmentMethamphetamine Dependence2
4TerminatedTreatmentPediatric Bipolar Disorder1
4TerminatedTreatmentSchizophrenic Disorders2
4TerminatedTreatmentSexual Dysfunctions1
4Unknown StatusTreatmentAutism, Early Infantile1
4Unknown StatusTreatmentBipolar I Disorder1
4Unknown StatusTreatmentBipolar / Schizophrenic Disorders1
4Unknown StatusTreatmentDyskinesia, Drug-Induced1
4Unknown StatusTreatmentDyslipidemias / Idiopathic hyperprolactinemic disorder / Weight gain therapy1
4Unknown StatusTreatmentPsychosis1
4Unknown StatusTreatmentSchizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorder1
4Unknown StatusTreatmentSchizophrenia or Schizoaffective Disorder1
4Unknown StatusTreatmentSchizophrenia, Tardive Dyskinesia, Metabolic Syndrome1
4Unknown StatusTreatmentSchizophrenic Disorders3
4Unknown StatusTreatmentIdiopathic hyperprolactinemic disorder / Sexual Dysfunctions1
4WithdrawnPreventionSchizophrenic Disorders1
4WithdrawnTreatmentDepressive Disorder Not Otherwise Specified (NOS) / Dysthymic Disorder / Major Depressive Disorder (MDD)1
4WithdrawnTreatmentMethamphetamine Dependence1
Not AvailableActive Not RecruitingTreatmentSchizophrenia Relapse1
Not AvailableCompletedNot AvailableBipolar Disorder (BD)1
Not AvailableCompletedNot AvailableBipolar Disorder (BD) / Metabolic Syndromes / Psychotic Disorder NOS1
Not AvailableCompletedNot AvailableBipolar Disorder (BD) / Psychotic Disorder NOS / Schizoaffective Disorders / Schizophrenic Disorders / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableNormal Volunteers1
Not AvailableCompletedNot AvailableSchizoaffective Disorders / Schizophenia Disorder1
Not AvailableCompletedNot AvailableSchizophrenic Disorders1
Not AvailableCompletedBasic ScienceAntipsychotics / Brain Metabolism / Cognition / Dopamine Receptor Occupancy1
Not AvailableCompletedDiagnosticSchizophrenic Disorders1
Not AvailableCompletedOtherMajor Depressive Disorder (MDD)1
Not AvailableCompletedPreventionBipolar Disorder (BD) / Depression / Psychotic Disorder NOS / Schizophrenic Disorders1
Not AvailableCompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Bipolar Disorder (BD)1
Not AvailableCompletedTreatmentAutism, Early Infantile1
Not AvailableCompletedTreatmentBipolar Disorder (BD)1
Not AvailableCompletedTreatmentMajor Depressive Disorder (MDD)1
Not AvailableCompletedTreatmentMetabolic Syndromes1
Not AvailableCompletedTreatmentObsessive Compulsive Disorder (OCD) / Schizophrenia OCD1
Not AvailableCompletedTreatmentTrichotillomania1
Not AvailableCompletedTreatmentIdiopathic hyperprolactinemic disorder1
Not AvailableEnrolling by InvitationNot AvailableBipolar Disorder (BD)1
Not AvailableNot Yet RecruitingNot AvailableWeight, Body1
Not AvailableNot Yet RecruitingTreatmentObsessive-Compulsive Disorder (OCD)1
Not AvailableRecruitingNot AvailableAcute Bacterial Exacerbation of Chronic Bronchitis (ABECB) / Acute Bacterial Sinusitis (ABS) / Acute Decompensated Heart Failure (ADHF) / Acute Pyelonephritis / Adenovirus / Adjunct to general anesthesia therapy / Adrenal Insufficiency / Airway Swelling / Anaesthesia therapy / Anxiolysis / Arterial Hypotension / Autism, Early Infantile / Autistic Disorder / Bartonellosis / Benzodiazepine Withdrawal / Benzodiazepines / Bipolar Disorder (BD) / Bloodstream Infections / Bone and Joint Infections / Brain Swelling / Bronchospasm / Brucellosis / Cardiac Arrest / Central Nervous System Infections / Cholera / Chronic Bacterial Prostatitis / Community Acquired Pneumonia (CAP) / Complicated Urinary Tract Infections / Convulsions / Cyanide Poisoning / Cytomegalovirus Retinitis / Drug hypersensitivity reaction / Early-onset Schizophrenia Spectrum Disorders / Edema / Epilepsies / Feeling Anxious / Flu caused by Influenza / Gastroparesis / Gynaecological infection / Headaches / Herpes Simplex Virus / High Blood Pressure (Hypertension) / High Cholesterol / Hospital-acquired bacterial pneumonia / Hyperlipidemias / Infantile Hemangiomas / Infection NOS / Inflammatory Conditions / Inflammatory Reaction / Influenza Treatment or Prophylaxis / Inhalational Anthrax (Post-Exposure) / Intra-Abdominal Infections / Life-threatening Fungal Infections / Lower Respiratory Tract Infection (LRTI) / Meningitis, Bacterial / Migraines / Muscle Spasms / Nausea / Opioid Addiction / Pain / Plague / Pneumonia / Prophylaxis / Psittacosis / Q Fever / Reflux / Relapsing Fever / Rocky Mountain Spotted Fever / Schizophrenic Disorders / Sedation therapy / Seizures / Sepsis / Skeletal Muscle Spasms / Skin and Subcutaneous Tissue Bacterial Infections / Skin Structures and Soft Tissue Infections / Stable Angina (SA) / Thromboprophylaxis / Thrombosis / Trachoma / Treatment-resistant Schizophrenia / Tularemia / Typhus Fever / Uncomplicated Skin and Skin Structure Infections / Uncomplicated Urinary Tract Infections / Urinary Tract Infections (UTIs) / Vomiting / Withdrawal1
Not AvailableRecruitingNot AvailableAdverse Drug Effect of Antipsychotics and Neuroleptics / Efficacy / Individualed Opitmal Therapy / Schizophrenic Disorders1
Not AvailableRecruitingNot AvailableAnorexia Nervosa (AN) / Attention Deficit Disorder With Hyperactivity (ADHD) / Depression1
Not AvailableRecruitingNot AvailableBipolar Disorder (BD) / First-Episode Psychosis1
Not AvailableRecruitingOtherBioequivalence1
Not AvailableRecruitingTreatmentSchizophrenic Disorders2
Not AvailableTerminatedNot AvailableSchizophrenic Disorders1
Not AvailableTerminatedOtherBipolar Disorder (BD)1
Not AvailableTerminatedTreatmentBipolar Disorder (BD) / Metabolic Syndromes1
Not AvailableTerminatedTreatmentGilles de la Tourette's Syndrome1
Not AvailableTerminatedTreatmentProdromal Psychosis / Prodromal Schizophrenia1
Not AvailableTerminatedTreatmentSchizoaffective Disorders / Schizophrenic Disorders2
Not AvailableUnknown StatusPreventionPsychotic Disorder NOS1
Not AvailableUnknown StatusTreatmentMajor Depressive Disorder (MDD)1
Not AvailableUnknown StatusTreatmentSchizophrenic Disorders2
Not AvailableUnknown StatusTreatmentSchizophrenic Disorders / Sensory Gating1
Not AvailableWithdrawnTreatmentPsychotic Disorder NOS1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Bristol-Myers Squibb Co.
  • Bryant Ranch Prepack
  • Cardinal Health
  • Comprehensive Consultant Services Inc.
  • DispenseXpress Inc.
  • E.R. Squibb and Sons LLC
  • Murfreesboro Pharmaceutical Nursing Supply
  • Otsuka America
  • PD-Rx Pharmaceuticals Inc.
  • Physician Partners Ltd.
  • Physicians Total Care Inc.
  • Quality Care
  • Rebel Distributors Corp.
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Southwood Pharmaceuticals
  • Stat Rx Usa
Dosage forms
FormRouteStrength
Injection, solutionIntramuscular9.75 mg/1.3mL
TabletOral10 mg/1
TabletOral15 mg/1
TabletOral2 mg/1
TabletOral2 mg
TabletOral20 mg/1
TabletOral30 mg/1
TabletOral5 mg/1
Injection, powder, for suspension, extended releaseIntramuscular300 mg
Injection, powder, for suspension, extended releaseIntramuscular400 mg
Injection, powder, for suspension, extended release; kitIntramuscular300 mg
Injection, powder, for suspension, extended release; kitIntramuscular400 mg
Injection, powder, lyophilized, for suspension, extended releaseIntramuscular300 mg/1.5mL
Injection, powder, lyophilized, for suspension, extended releaseIntramuscular400 mg/2.0mL
Kit300 mg/1.5mL
Kit400 mg/1.9mL
SolutionOral1 mg/1mL
Tablet, orally disintegratingOral10 mg/1
Tablet, orally disintegratingOral15 mg/1
TabletOral10 mg
TabletOral15 mg
TabletOral30 mg
TabletOral5 mg
TabletOral20 mg
Tablet, orally disintegratingOral10 mg
Tablet, orally disintegratingOral15 mg
Tablet, orally disintegratingOral30 mg
Prices
Unit descriptionCostUnit
Abilify Discmelt 30 10 mg Dispersible Tablet Box636.3USD box
Abilify 30 mg tablet32.12USD tablet
Abilify 15 mg tablet26.07USD tablet
Abilify 10 mg tablet23.53USD tablet
Abilify 5 mg tablet23.53USD tablet
Abilify 2 mg tablet22.25USD tablet
Abilify 20 mg tablet21.99USD tablet
Abilify discmelt 10 mg tablet20.39USD tablet
Abilify discmelt 15 mg tablet20.39USD tablet
Abilify 9.7 mg/1.3 ml vial16.04USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5006528No1994-10-202014-10-20Us
US7053092No2002-01-282022-01-28Us
US8642600Yes2002-07-282022-07-28Us
US8759350No2007-03-022027-03-02Us
US9125939No2006-07-282026-07-28Us
US9089567No2002-01-282022-01-28Us
US8017615Yes2004-12-162024-12-16Us
US8580796Yes2003-03-252023-03-25Us
US8642760Yes2003-03-252023-03-25Us
US6977257Yes2002-10-242022-10-24Us
US8518421Yes2001-07-242021-07-24Us
US7115587Yes2005-01-212025-01-21Us
US7550445Yes2005-01-212025-01-21Us
US8030313No2004-10-192024-10-19Us
US8338427No2005-03-152025-03-15Us
US8338428No2003-08-062023-08-06Us
US8759351No2003-08-062023-08-06Us
US7807680No2004-10-192024-10-19Us
US8993761No2002-09-252022-09-25Us
US8722679No2004-10-192024-10-19Us
US8399469No2005-06-292025-06-29Us
US9193685No2013-10-242033-10-24Us
US8796276No2010-06-242030-06-24Us
US9034867No2012-11-072032-11-07Us
US8431576No2010-10-262030-10-26Us
US9387182No2003-12-252023-12-25Us
US9359302No2002-09-252022-09-25Us
US9358207No2000-04-122020-04-12Us
US9526726No2015-03-192035-03-19Us
US9452131No2015-03-192035-03-19Us
US8945005No2009-08-192029-08-19Us
US8847766No2010-03-292030-03-29Us
US9787511No2014-09-192034-09-19Us
US8674825No2009-04-092029-04-09Us
US9270503No2014-09-192034-09-19Us
US9268909No2013-10-152033-10-15Us
US8956288No2009-07-062029-07-06Us
US9444503No2007-11-192027-11-19Us
US8547248No2010-12-182030-12-18Us
US9577864No2013-10-032033-10-03Us
US8545402No2010-04-272030-04-27Us
US9433371No2009-09-152029-09-15Us
US8114021No2006-11-022026-11-02Us
US9320455No2011-12-152031-12-15Us
US9119554No2008-12-162028-12-16Us
US9258035No2009-03-052029-03-05Us
US8258962No2010-11-252030-11-25Us
US7978064No2006-09-142026-09-14Us
US8718193No2009-12-052029-12-05Us
US8961412No2010-11-172030-11-17Us
US9060708No2009-03-052029-03-05Us
US9149577No2009-12-152029-12-15Us
US9941931No2010-11-042030-11-04Us

Properties

State
Solid
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 RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9934
Blood Brain Barrier+0.992
Caco-2 permeable+0.5
P-glycoprotein substrateSubstrate0.7431
P-glycoprotein inhibitor IInhibitor0.9585
P-glycoprotein inhibitor IIInhibitor0.9321
Renal organic cation transporterInhibitor0.5175
CYP450 2C9 substrateNon-substrate0.8663
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.7408
CYP450 1A2 substrateInhibitor0.6581
CYP450 2C9 inhibitorInhibitor0.6682
CYP450 2D6 inhibitorInhibitor0.6633
CYP450 2C19 inhibitorInhibitor0.8934
CYP450 3A4 inhibitorInhibitor0.5256
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9104
Ames testNon AMES toxic0.6124
CarcinogenicityNon-carcinogens0.8765
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.8894 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.62
hERG inhibition (predictor II)Inhibitor0.8814
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

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

Taxonomy

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
Phenylpiperazine / N-arylpiperazine / Tetrahydroquinolone / Quinolone / Tetrahydroquinoline / 1,2-dichlorobenzene / Tertiary aliphatic/aromatic amine / Aniline or substituted anilines / Dialkylarylamine / Alkyl aryl ether
show 28 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
N-arylpiperazine, dichlorobenzene, N-alkylpiperazine, quinolone (CHEBI:31236)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Virus receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 Da
References
  1. Meltzer HY, Li Z, Kaneda Y, Ichikawa J: Serotonin receptors: their key role in drugs to treat schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry. 2003 Oct;27(7):1159-72. [PubMed:14642974]
  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:17242925]
  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:17265076]
Details
2. D(2) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
Partial agonist
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Hirose T, Kikuchi T: Aripiprazole, a novel antipsychotic agent: dopamine D2 receptor partial agonist. J Med Invest. 2005 Nov;52 Suppl:284-90. [PubMed:16366516]
  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:9083792]
  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:16925992]
  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:16981227]
  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:17501690]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da
References
  1. Jordan S, Koprivica V, Chen R, Tottori K, Kikuchi T, Altar CA: The antipsychotic aripiprazole is a potent, partial agonist at the human 5-HT1A receptor. Eur J Pharmacol. 2002 Apr 26;441(3):137-40. [PubMed:12063084]
  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:14647959]
  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:14709325]
  4. Swainston Harrison T, Perry CM: Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder. Drugs. 2004;64(15):1715-36. [PubMed:15257633]
  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:15862515]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1B
Uniprot ID
P28222
Uniprot Name
5-hydroxytryptamine receptor 1B
Molecular Weight
43567.535 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1D
Uniprot ID
P28221
Uniprot Name
5-hydroxytryptamine receptor 1D
Molecular Weight
41906.38 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that trig...
Gene Name
HTR1E
Uniprot ID
P28566
Uniprot Name
5-hydroxytryptamine receptor 1E
Molecular Weight
41681.57 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
Molecular Weight
51820.705 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Voltage-gated potassium channel activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gate...
Gene Name
HTR3A
Uniprot ID
P46098
Uniprot Name
5-hydroxytryptamine receptor 3A
Molecular Weight
55279.835 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR6
Uniprot ID
P50406
Uniprot Name
5-hydroxytryptamine receptor 6
Molecular Weight
46953.625 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
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
HTR7
Uniprot ID
P34969
Uniprot Name
5-hydroxytryptamine receptor 7
Molecular Weight
53554.43 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Details
11. D(1A) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name
DRD1
Uniprot ID
P21728
Uniprot Name
D(1A) dopamine receptor
Molecular Weight
49292.765 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Details
12. D(1B) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name
DRD5
Uniprot ID
P21918
Uniprot Name
D(1B) dopamine receptor
Molecular Weight
52950.5 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Details
13. D(3) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name
DRD3
Uniprot ID
P35462
Uniprot Name
D(3) dopamine receptor
Molecular Weight
44224.335 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Details
14. D(4) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
General Function
Sh3 domain binding
Specific Function
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins ...
Gene Name
DRD4
Uniprot ID
P21917
Uniprot Name
D(4) dopamine receptor
Molecular Weight
48359.86 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Details
15. Histamine H1 receptor
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
Molecular Weight
51486.005 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1B
Uniprot ID
P35368
Uniprot Name
Alpha-1B adrenergic receptor
Molecular Weight
56835.375 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Thioesterase binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Epinephrine binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine...
Gene Name
ADRA2B
Uniprot ID
P18089
Uniprot Name
Alpha-2B adrenergic receptor
Molecular Weight
49565.8 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
Other/unknown
General Function
Protein homodimerization activity
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name
ADRA2C
Uniprot ID
P18825
Uniprot Name
Alpha-2C adrenergic receptor
Molecular Weight
49521.585 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [PubMed:17848919]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
Molecular Weight
51420.375 Da
References
  1. 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:17848919]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
G-protein coupled acetylcholine receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM2
Uniprot ID
P08172
Uniprot Name
Muscarinic acetylcholine receptor M2
Molecular Weight
51714.605 Da
References
  1. 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:17848919]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM3
Uniprot ID
P20309
Uniprot Name
Muscarinic acetylcholine receptor M3
Molecular Weight
66127.445 Da
References
  1. 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:17848919]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Guanyl-nucleotide exchange factor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM4
Uniprot ID
P08173
Uniprot Name
Muscarinic acetylcholine receptor M4
Molecular Weight
53048.65 Da
References
  1. 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:17848919]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM5
Uniprot ID
P08912
Uniprot Name
Muscarinic acetylcholine receptor M5
Molecular Weight
60073.205 Da
References
  1. 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:17848919]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. 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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. 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. [PubMed:17214606]
  3. Swainston Harrison T, Perry CM: Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder. Drugs. 2004;64(15):1715-36. [PubMed:15257633]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. 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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]

Drug created on June 13, 2005 07:24 / Updated on October 16, 2018 08:35