Aripiprazole

Identification

Summary

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

Brand Names
Abilify
Generic Name
Aripiprazole
DrugBank Accession Number
DB01238
Background

Aripiprazole is an atypical antipsychotic orally indicated for the treatment of schizophrenia, bipolar I, major depressive disorder, irritability associated with autism, and Tourette's.8 It is also indicated as an injection for agitation associated with schizophrenia or bipolar mania.8 Aripiprazole exerts its effects through agonism of dopaminergic and 5-HT1A receptors and antagonism of alpha-adrenergic and 5-HT2A receptors.8,1 Aripiprazole was given FDA approval on November 15, 2002.6

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

Pharmacology

Indication

Aripiprazole is indicated for the treatment of acute manic and mixed episodes associated with bipolar I disorder, irritability associated with autism spectrum disorder, schizophrenia, and Tourette's disorder.8 It is also used as an adjunctive treatment of major depressive disorder.[L45859 An injectable formulation of aripiprazole is indicated for agitation associated with schizophrenia or bipolar mania.8 Finally, an extended-release, bimonthly injection formulation of aripiprazole is indicated for the treatment of adult schizophrenia and maintenance therapy for adult bipolar I disorder.9

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofAgitation••••••••••••••••••••••••••• ••••••• ••• ••••••••••• •••••••• •••••••• •••••••••• ••••••••• •••••••••• ••••••••••• •••••••• •••••••
Treatment ofAgitation•••••••••••••••••••••• ••••••• ••• ••••••••••• •••••••• •••••••• •••••••••• ••••••••• •••••••••• ••••••••••• •••••••• •••••••
Maintenance ofBipolar 1 disorder••••••••••••••••••••••••••• ••••••••••• •••••••• •••••••
Management ofBipolar 1 disorder•••••••••••••••••
Treatment ofIrritability••••••••••••
Associated Therapies
Contraindications & Blackbox Warnings
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Pharmacodynamics

Aripiprazole exhibits high affinity for dopamine D2 and D3, serotonin 5-HT1a and 5-HT2a receptors (Ki values of 0.34 nM, 0.8 nM, 1.7 nM, and 3.4 nM, respectively), moderate affinity for dopamine D4, serotonin 5-HT2c and 5-HT7, alpha1-adrenergic and histamine H1 receptors (Ki values of 44 nM, 15 nM, 39 nM, 57 nM, and 61 nM, respectively), and moderate affinity for the serotonin reuptake site (Ki=98 nM). Aripiprazole has no appreciable affinity for cholinergic muscarinic receptors (IC50>1000 nM).8

Mechanism of action

The antipsychotic action of aripiprazole is likely due to its partial agonist activity on D2 and 5-HT1A receptors as well as its antagonist activity at 5-HT2A receptors; however, the exact mechanism has not been fully elucidated.1,8 One of the mechanisms that have been proposed is that aripiprazole both stimulates and inhibits dopamine as it engages the D2 receptor. It lowers dopamine neuronal firing at high dopamine concentrations and increases dopamine firing at low concentrations. Its partial agonist activity gives aripiprazole an intermediate level of dopaminergic neuronal tone between full agonist and antagonist of the D2 receptor.5 In addition, some adverse effects may be due to action on other receptors.[L4620] For example, orthostatic hypotension may be explained by antagonism of the adrenergic alpha-1 receptors.1

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

Tablet: Aripiprazole is well absorbed after administration of the tablet, with peak plasma concentrations occurring within 3 hours to 5 hours; the absolute oral bioavailability of the tablet formulation is 87%. ABILIFY can be administered with or without food. Administration of a 15 mg ABILIFY tablet with a standard high-fat meal did not significantly affect the Cmax or AUC of aripiprazole or its active metabolite, dehydro-aripiprazole, but delayed Tmax by 3 hours for aripiprazole and 12 hours for dehydro-aripiprazole.8

Oral Solution: Aripiprazole is well absorbed when administered orally as the solution. At equivalent doses, the plasma concentrations of aripiprazole from the solution were higher than that from the tablet formulation. In a relative bioavailability study comparing the pharmacokinetics of 30 mg aripiprazole as the oral solution to 30 mg aripiprazole tablets in healthy subjects, the solution-to-tablet ratios of geometric mean Cmax and AUC values were 122% and 114%, respectively. The single-dose pharmacokinetics of aripiprazole were linear and dose-proportional between the doses of 5 mg to 30 mg.8

Extended-release injectable suspension, bimonthly injection: Aripiprazole absorption into the systemic circulation is prolonged following gluteal intramuscular injection due to the low solubility of aripiprazole particles. The release profile of aripiprazole from ABILIFY ASIMTUFII results in sustained plasma concentrations over 2 months following gluteal injection(s). Following multiple doses, the median peak:trough ratio for aripiprazole following an ABILIFY ASIMTUFII dose is 1.3, resulting in a flat plasma concentration profile with Tmax ranging between 1 to 49 days following multiple gluteal administrations of 960 mg.9

Volume of distribution

The steady-state volume of distribution of aripiprazole following intravenous administration is high (404 L or 4.9 L/kg), indicating extensive extravascular distribution.8,2

Protein binding

At therapeutic concentrations, aripiprazole and its major metabolite are greater than 99% bound to serum proteins, primarily to albumin.8

Metabolism

Aripiprazole is metabolized primarily by three biotransformation pathways: dehydrogenation, hydroxylation, and N-dealkylation. Based on in vitro studies, CYP3A4 and CYP2D6 enzymes are responsible for the dehydrogenation and hydroxylation of aripiprazole, and N-dealkylation is catalyzed by CYP3A4. Aripiprazole is the predominant drug moiety in systemic circulation. At steady-state, dehydro-aripiprazole, the active metabolite, represents about 40% of aripiprazole AUC in plasma.8

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Route of elimination

Following a single oral dose of [14C]-labeled aripiprazole, approximately 25% and 55% of the administered radioactivity was recovered in the urine and feces, respectively. Less than 1% of unchanged aripiprazole was excreted in the urine and approximately 18% of the oral dose was recovered unchanged in the feces.8,4

Half-life

The mean elimination half-lives are about 75 hours and 94 hours for aripiprazole and dehydro-aripiprazole, respectively.8 For populations that are poor CYP2D6 metabolizers, the half-life of aripiprazole is 146 hours and these patients should be treated with half the normal dose.8 Other studies have reported a half-life of 61.03±19.59 hours for aripiprazole and 279±299 hours for the active metabolite.3

Clearance

The clearance of aripiprazole was estimated to be 0.8mL/min/kg.2 Other studies have also reported a clearance rate of 3297±1042mL/hr.3

Adverse Effects
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Toxicity

Neonates exposed to antipsychotic drugs, including ABILIFY, during the third trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symptoms following delivery. Overall available data from published epidemiologic studies of pregnant women exposed to aripiprazole have not established a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. There are risks to the mother associated with untreated schizophrenia, bipolar I disorder, or major depressive disorder, and with exposure to antipsychotics, including ABILIFY, during pregnancy.8

In animal reproduction studies, oral and intravenous aripiprazole administration during organogenesis in rats and/or rabbits at doses 10 and 19 times, respectively, the maximum recommended human dose (MRHD) of 30 mg/day based on mg/m2 body surface area, produced fetal death, decreased fetal weight, undescended testicles, delayed skeletal ossification, skeletal abnormalities, and diaphragmatic hernia. Oral and intravenous aripiprazole administration during the pre- and post-natal period in rats at doses 10 times the MRHD based on mg/m2 body surface area, produced prolonged gestation, stillbirths, decreased pup weight, and decreased pup survival.8

ABILIFY has not been systematically studied in humans for its potential for abuse, tolerance, or physical dependence. Consequently, patients should be evaluated carefully for a history of drug abuse, and such patients should be observed closely for signs of ABILIFY misuse or abuse (e.g., development of tolerance, increases in dose, drug-seeking behavior).8

In physical dependence studies in monkeys, withdrawal symptoms were observed upon abrupt cessation of dosing. While the clinical trials did not reveal any tendency for any drug-seeking behavior, these observations were not systematic and it is not possible to predict on the basis of this limited experience the extent to which a CNS-active drug will be misused, diverted, and/or abused once marketed.8

In clinical trials and in postmarketing experience, adverse reactions of deliberate or accidental overdosage with oral ABILIFY have been reported worldwide. These include overdoses with oral ABILIFY alone and in combination with other substances. No fatality was reported with ABILIFY alone. The largest known dose with a known outcome involved acute ingestion of 1,260 mg of oral ABILIFY (42 times the maximum recommended daily dose) by a patient who fully recovered. Deliberate or accidental overdosage was also reported in children (age 12 years and younger) involving oral ABILIFY ingestions up to 195 mg with no fatalities.8

Common adverse reactions (reported in at least 5% of all overdose cases) reported with oral ABILIFY overdosage (alone or in combination with other substances) include vomiting, somnolence, and tremor. Other clinically important signs and symptoms observed in one or more patients with ABILIFY overdoses (alone or with other substances) include acidosis, aggression, aspartate aminotransferase increased, atrial fibrillation, bradycardia, coma, confusional state, convulsion, blood creatine phosphokinase increased, depressed level of consciousness, hypertension, hypokalemia, hypotension, lethargy, loss of consciousness, QRS complex prolonged, QT prolonged, pneumonia aspiration, respiratory arrest, status epilepticus, and tachycardia.8

No specific information is available on the treatment of overdose with ABILIFY. An electrocardiogram should be obtained in case of overdosage and if QT interval prolongation is present, cardiac monitoring should be instituted. Otherwise, management of overdose should concentrate on supportive therapy, maintaining an adequate airway, oxygenation and ventilation, and management of symptoms. Close medical supervision and monitoring should continue until the patient recovers.8
Charcoal: In the event of an overdose of ABILIFY, an early charcoal administration may be useful in partially preventing the absorption of aripiprazole. Administration of 50 g of activated charcoal, one hour after a single 15 mg oral dose of ABILIFY, decreased the mean AUC and Cmax of aripiprazole by 50%.8 Hemodialysis: Although there is no information on the effect of hemodialysis in treating an overdose with ABILIFY, hemodialysis is unlikely to be useful in overdose management since aripiprazole is highly bound to plasma proteins.8

Lifetime carcinogenicity studies were conducted in ICR mice, F344 rats, and Sprague-Dawley (SD) rats. Aripiprazole was administered for 2 years in the diet at doses of 1, 3, 10, and 30 mg/kg/day to ICR mice and 1, 3, and 10 mg/kg/day to F344 rats (0.2, 0.5, 2 and 5 times and 0.3, 1 and 3 times the MRHD of 30 mg/day based on mg/m2 body surface area, respectively). In addition, SD rats were dosed orally for 2 years at 10, 20, 40, and 60 mg/kg/day, which are 3, 6, 13 and 19 times the MRHD based on mg/m2 body surface area. Aripiprazole did not induce tumors in male mice or male rats. In female mice, the incidences of pituitary gland adenomas and mammary gland adenocarcinomas and adenoacanthomas were increased at dietary doses of 3 to 30 mg/kg/day (0.5 to 5 times the MRHD). In female rats, the incidence of mammary gland fibroadenomas was increased at a dietary dose of 10 mg/kg/day (3 times the MRHD); and the incidences of adrenocortical carcinomas and combined adrenocortical adenomas/carcinomas were increased at an oral dose of 60 mg/kg/day (19 times the MRHD).8

An increase in mammary, pituitary, and endocrine pancreas neoplasms has been found in rodents after chronic administration of other antipsychotic drugs and is considered to be mediated by prolonged dopamine D2-receptor antagonism and hyperprolactinemia. Serum prolactin was not measured in the aripiprazole carcinogenicity studies. However, increases in serum prolactin levels were observed in female mice in a 13 week dietary study at the doses associated with mammary gland and pituitary tumors. Serum prolactin was not increased in female rats in 4 week and 13 week dietary studies at the dose associated with mammary gland tumors. The relevance for human risk of the findings of prolactin-mediated endocrine tumors in rodents is unclear.8

The mutagenic potential of aripiprazole was tested in the in vitro bacterial reverse-mutation assay, the in vitro bacterial DNA repair assay, the in vitro forward gene mutation assay in mouse lymphoma cells, the in vitro chromosomal aberration assay in Chinese hamster lung (CHL) cells, the in vivo micronucleus assay in mice, and the unscheduled DNA synthesis assay in rats. Aripiprazole and a metabolite (2,3-DCPP) were clastogenic in the in vitro chromosomal aberration assay in CHL cells with and without metabolic activation. The metabolite, 2,3-DCPP, increased numerical aberrations in the in vitro assay in CHL cells in the absence of metabolic activation. A positive response was obtained in the in vivo micronucleus assay in mice; however, the response was due to a mechanism not considered relevant to humans.8

Female rats were treated orally with aripiprazole from 2 weeks prior to mating through gestation Day 7 at doses of 2, 6, and 20 mg/kg/day, which are 0.6, 2, and 6 times the MRHD of 30 mg/day based on mg/m2 body surface area. Estrus cycle irregularities and increased corpora lutea were seen at all doses, but no impairment of fertility was seen. Increased pre-implantation loss was seen at 2 and 6 times the MRHD, and decreased fetal weight was seen at 6 times the MRHD.8

Male rats were treated orally with aripiprazole from 9 weeks prior to mating through mating at doses of 20, 40, and 60 mg/kg/day, which are 6, 13, and 19 times the MRHD of 30 mg/day based on mg/m2 body surface area. Disturbances in spermatogenesis were seen at 19 times the MRHD and prostate atrophy was seen at 13 and 19 times the MRHD without impairment of fertility.8

Pharmacokinetic properties in patients 10-17 years of age are similar to that of adults once body weight has been corrected for. No dosage adjustment is necessary in elderly patients however aripiprazole is not approved for Alzheimer's associated psychosis. Patients classified as CYP2D6 poor metabolizers should be prescribed half the regular dose of aripiprazole. Hepatic and renal function as well as sex, race, and smoking status do not affect dosage requirements for aripiprazole 8,3

Pathways
Not Available
Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
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 Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
1,2-BenzodiazepineThe risk or severity of CNS depression can be increased when Aripiprazole is combined with 1,2-Benzodiazepine.
AbaloparatideAripiprazole may increase the hypotensive activities of Abaloparatide.
AbametapirThe serum concentration of Aripiprazole can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Aripiprazole can be increased when combined with Abatacept.
AbirateroneThe metabolism of Aripiprazole can be decreased when combined with Abiraterone.
Food Interactions
  • Avoid alcohol. Alcohol may increase CNS effects.
  • Drink plenty of fluids. Drink water to avoid dehydration while taking aripiprazole.
  • Take with or without food. Food does not affect absorption.

Products

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Product Images
International/Other Brands
Abilitat
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AbilifyTablet30 mg/1OralCardinal Health2002-11-152013-12-31US flag
AbilifyTablet15 mg/1OralOtsuka America Pharmaceutical, Inc.2002-11-15Not applicableUS flag
AbilifyTablet, orally disintegrating15 mgOralOtsuka Pharmaceutical Netherlands B.V.2021-01-12Not applicableEU flag
AbilifyTablet15 mgOralOtsuka Pharmaceutical Netherlands B.V.2021-01-12Not applicableEU flag
AbilifyTablet10 mg/1OralCardinal Health2002-11-152017-08-31US flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-aripiprazoleTablet15 mgOralApotex Corporation2018-04-10Not applicableCanada flag
Apo-aripiprazoleTablet2 mgOralApotex Corporation2018-04-10Not applicableCanada flag
Apo-aripiprazoleTablet30 mgOralApotex Corporation2018-04-10Not applicableCanada flag
Apo-aripiprazoleTablet10 mgOralApotex Corporation2018-04-10Not applicableCanada flag
Apo-aripiprazoleTablet20 mgOralApotex Corporation2018-04-10Not applicableCanada flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
AbilifyAripiprazole (15 mg/1)TabletOralRemedy Repack2010-12-142014-08-27US flag
AbilifyAripiprazole (20 mg/1)TabletOralRemedy Repack2013-04-092014-08-12US flag
AbilifyAripiprazole (10 mg/1)TabletOralRemedy Repack2010-12-142015-05-20US flag
AbilifyAripiprazole (30 mg/1)TabletOralRemedy Repack2010-12-132014-06-21US flag
CUREXOL 5 MG TABLET, 28 ADETAripiprazole (5 mg)TabletOralACTAVİS İLAÇLARI A.Ş.2019-08-06Not applicableTurkey flag

Categories

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

Chemical Identifiers

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

References

Synthesis Reference
US5006528
General References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. Bauman JN, Frederick KS, Sawant A, Walsky RL, Cox LM, Obach RS, Kalgutkar AS: Comparison of the bioactivation potential of the antidepressant and hepatotoxin nefazodone with aripiprazole, a structural analog and marketed drug. Drug Metab Dispos. 2008 Jun;36(6):1016-29. doi: 10.1124/dmd.108.020545. Epub 2008 Mar 10. [Article]
  3. Kubo M, Koue T, Maune H, Fukuda T, Azuma J: Pharmacokinetics of aripiprazole, a new antipsychotic, following oral dosing in healthy adult Japanese volunteers: influence of CYP2D6 polymorphism. Drug Metab Pharmacokinet. 2007 Oct;22(5):358-66. [Article]
  4. Prommer E: Aripiprazole. Am J Hosp Palliat Care. 2017 Mar;34(2):180-185. doi: 10.1177/1049909115612800. Epub 2016 Jul 10. [Article]
  5. Frankel JS, Schwartz TL: Brexpiprazole and cariprazine: distinguishing two new atypical antipsychotics from the original dopamine stabilizer aripiprazole. Ther Adv Psychopharmacol. 2017 Jan;7(1):29-41. doi: 10.1177/2045125316672136. Epub 2016 Oct 17. [Article]
  6. FDA Drug Approval Package: Aripiprazole [Link]
  7. Clinicaltrails.gov: National Pregnancy Registry for Atypical Antipsychotics [Link]
  8. FDA Approved Drug Products: ABILIFY (aripiprazole) tablets for oral use, orally disintegrating tablets, oral solution, injection for intramuscular use only (November 2022) [Link]
  9. FDA Approved Drug Products: ABILIFY ASIMTUFII® (aripiprazole) extended-release injectable suspension, for intramuscular use [Link]
Human Metabolome Database
HMDB0005042
KEGG Drug
D01164
KEGG Compound
C12564
PubChem Compound
60795
PubChem Substance
46505745
ChemSpider
54790
BindingDB
50130293
RxNav
89013
ChEBI
31236
ChEMBL
CHEMBL1112
ZINC
ZINC000001851149
Therapeutic Targets Database
DAP000076
PharmGKB
PA10026
Guide to Pharmacology
GtP Drug Page
PDBe Ligand
9SC
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Aripiprazole
PDB Entries
6a7p / 7e2z / 7voe / 7vr9 / 7wkz
FDA label
Download (1.35 MB)
MSDS
Download (24.6 KB)

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Bristol-Myers Squibb Co.
  • Bryant Ranch Prepack
  • Cardinal Health
  • Comprehensive Consultant Services Inc.
  • DispenseXpress Inc.
  • E.R. Squibb and Sons LLC
  • Murfreesboro Pharmaceutical Nursing Supply
  • Otsuka America
  • PD-Rx Pharmaceuticals Inc.
  • Physician Partners Ltd.
  • Physicians Total Care Inc.
  • Quality Care
  • Rebel Distributors Corp.
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Southwood Pharmaceuticals
  • Stat Rx Usa
Dosage Forms
FormRouteStrength
Injection
Injection, solutionIntramuscular7.5 MG/ML
Injection, solutionIntramuscular9.75 mg/1.3mL
SolutionOral
TabletOral10 mg/1
TabletOral15 mg/1
TabletOral15.000 mg
TabletOral2 mg/1
TabletOral20 mg
TabletOral20 mg/1
TabletOral30 mg/1
TabletOral5 mg/1
Tablet, orally disintegratingOral5 MG
SolutionOral1 MG/ML
Injection, suspension, extended releaseIntramuscular720 mg/2.4mL
Injection, suspension, extended releaseIntramuscular960 mg/3.2mL
Injection, powder, for suspension, extended releaseIntramuscular300 mg / syr
Injection, powder, for suspension, extended releaseIntramuscular300 mg
Injection, powder, for suspension, extended releaseIntramuscular400 mg
Injection, powder, for suspension, extended releaseIntramuscular400 mg / syr
Injection, powder, for suspension, extended releaseIntramuscular; Parenteral300 MG
Injection, powder, for suspension, extended releaseIntramuscular; Parenteral400 MG
Injection, powder, for suspension, extended release; kitIntramuscular300 mg / vial
Injection, powder, for suspension, extended release; kitIntramuscular400 mg / vial
Injection, powder, lyophilized, for suspension, extended releaseIntramuscular300 mg/1.5mL
Injection, powder, lyophilized, for suspension, extended releaseIntramuscular400 mg/2.0mL
Injection, suspension, extended release; kitIntramuscular300 mg/1.5mL
Injection, suspension, extended release; kitIntramuscular400 mg/1.9mL
Injection, powder, for suspensionIntramuscular300 mg/1vial
Injection, powder, for suspensionIntramuscular400 mg/1vial
Injection, suspension, extended releaseIntramuscular300 mg
Injection, powder, for suspensionIntramuscular
Injection, suspension, extended releaseIntramuscular400 mg
Injection, powder, for suspension, extended releaseIntramuscular400 mg/vial
SolutionOral1.0 mg/ml
TabletOral10.0 mg
TabletOral2 mg
TabletOral5.0 mg
TabletOral10 mg
TabletOral15 mg
Tablet, orally disintegratingOral10 mg
Tablet, orally disintegratingOral15 mg
TabletOral20.00 mg
TabletOral
TabletOral5 mg
Tablet, solubleBuccal
Tablet, orally disintegratingOral30 MG
Tablet, orally disintegratingOral
SolutionOral1 mg/1mL
Tablet, orally disintegratingOral10 mg/1
Tablet, orally disintegratingOral15 mg/1
Tablet, orally disintegratingOral20 mg/1
Tablet, orally disintegratingOral30 mg/1
Tablet, solubleOral
TabletOral30 MG
TabletOral30.000 mg
SolutionOral100 mg
SolutionOral10000000 mg
TabletOral10.000 mg
SolutionOral1 mg
SolutionOral100000 mg
Tablet, solubleBuccal15 mg
Tablet, coatedOral10 mg
Tablet, coatedOral15 mg
Tablet, coatedOral5 mg
Prices
Unit descriptionCostUnit
Abilify Discmelt 30 10 mg Dispersible Tablet Box636.3USD box
Abilify 30 mg tablet32.12USD tablet
Abilify 15 mg tablet26.07USD tablet
Abilify 10 mg tablet23.53USD tablet
Abilify 5 mg tablet23.53USD tablet
Abilify 2 mg tablet22.25USD tablet
Abilify 20 mg tablet21.99USD tablet
Abilify discmelt 10 mg tablet20.39USD tablet
Abilify discmelt 15 mg tablet20.39USD tablet
Abilify 9.7 mg/1.3 ml vial16.04USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5006528No1991-04-092014-10-20US flag
US7053092No2006-05-302022-01-28US flag
US8642600Yes2014-02-042022-07-28US flag
US8759350No2014-06-242027-03-02US flag
US9125939No2015-09-082026-07-28US flag
US9089567No2015-07-282022-01-28US flag
US8017615Yes2011-09-132024-12-16US flag
US8580796Yes2013-11-122023-03-25US flag
US8642760Yes2014-02-042023-03-25US flag
US6977257Yes2005-12-202022-10-24US flag
US8518421Yes2013-08-272021-07-24US flag
US7115587Yes2006-10-032025-01-21US flag
US7550445Yes2009-06-232025-01-21US flag
US8030313No2011-10-042024-10-19US flag
US8338427No2012-12-252025-03-15US flag
US8338428No2012-12-252023-08-06US flag
US8759351No2014-06-242023-08-06US flag
US7807680No2010-10-052024-10-19US flag
US8993761No2015-03-312022-09-25US flag
US8722679No2014-05-132024-10-19US flag
US8399469No2013-03-192025-06-29US flag
US9193685No2015-11-242033-10-24US flag
US8796276No2014-08-052030-06-24US flag
US9034867No2015-05-192032-11-07US flag
US8431576No2013-04-302030-10-26US flag
US9387182No2016-07-122023-12-25US flag
US9359302No2016-06-072022-09-25US flag
US9358207No2016-06-072020-04-12US flag
US9526726No2016-12-272035-03-19US flag
US9452131No2016-09-272035-03-19US flag
US8945005No2015-02-032029-08-19US flag
US8847766No2014-09-302030-03-29US flag
US9787511No2017-10-102034-09-19US flag
US8674825No2014-03-182029-04-09US flag
US9270503No2016-02-232034-09-19US flag
US9268909No2016-02-232033-10-15US flag
US8956288No2015-02-172029-07-06US flag
US9444503No2016-09-132027-11-19US flag
US8547248No2013-10-012030-12-18US flag
US9577864No2017-02-212033-10-03US flag
US8545402No2013-10-012030-04-27US flag
US9433371No2016-09-062029-09-15US flag
US8114021No2012-02-142026-11-02US flag
US9320455No2016-04-262031-12-15US flag
US9119554No2015-09-012028-12-16US flag
US9258035No2016-02-092029-03-05US flag
US8258962No2012-09-042030-11-25US flag
US7978064No2011-07-122026-09-14US flag
US8718193No2014-05-062029-12-05US flag
US8961412No2015-02-242030-11-17US flag
US9060708No2015-06-232029-03-05US flag
US9149577No2015-10-062029-12-15US flag
US9941931No2018-04-102030-11-04US flag
US10097388No2018-10-092034-09-19US flag
US10441194No2019-10-152029-05-12US flag
US10525057No2020-01-072034-03-08US flag
US10517507No2019-12-312032-06-13US flag
US10980803No2021-04-202033-09-24US flag
US11154553No2021-10-262033-09-24US flag
US11229378No2011-07-112031-07-11US flag
US11344547No2013-09-242033-09-24US flag
US11400087No2013-09-242033-09-24US flag
US11476952No2006-04-282026-04-28US flag
US11464423No2010-09-152030-09-15US flag
US11638757No2013-04-232033-04-23US flag
US11097007No2021-08-242033-04-23US flag
US10517951No2019-12-312033-04-23US flag
US11648347No2014-04-062034-04-06US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)137-140http://www.chemspider.com/Chemical-Structure.54790.html
water solubility0.00001%https://medsafe.govt.nz/profs/Datasheet/a/Abilifytab.pdf
pKa7.6https://medsafe.govt.nz/profs/Datasheet/a/Abilifytab.pdf
Predicted Properties
PropertyValueSource
Water Solubility0.00777 mg/mLALOGPS
logP5.21ALOGPS
logP4.9Chemaxon
logS-4.8ALOGPS
pKa (Strongest Acidic)13.51Chemaxon
pKa (Strongest Basic)7.46Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count4Chemaxon
Hydrogen Donor Count1Chemaxon
Polar Surface Area44.81 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-MSsplash10-0w4i-1490100000-261de3e19904b78dcdc2
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSsplash10-000i-3970100000-6b98b53e8175df39986e
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0f72-0340900000-34d93478ad0d9f5cf2b0
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000i-3970100000-6b98b53e8175df39986e
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0002-0110900000-0a383252828a2840589e
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0002-0010900000-aea972cdfc8df21c61e4
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0002-0000900000-f042b48ddd254d9eb879
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0002-2154900000-fbe546c50dba06e2bc47
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-002r-0690000000-8b01525bb049b9e68d2e
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0007-2933600000-0da39b22d3c29458077f
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-208.6003939
predicted
DarkChem Lite v0.1.0
[M-H]-200.73216
predicted
DeepCCS 1.0 (2019)
[M+H]+209.4845939
predicted
DarkChem Lite v0.1.0
[M+H]+203.18477
predicted
DeepCCS 1.0 (2019)
[M+Na]+208.7707939
predicted
DarkChem Lite v0.1.0
[M+Na]+210.92848
predicted
DeepCCS 1.0 (2019)

Targets

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Details
1. Dopamine D2 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
Partial agonist
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Hirose T, Kikuchi T: Aripiprazole, a novel antipsychotic agent: dopamine D2 receptor partial agonist. J Med Invest. 2005 Nov;52 Suppl:284-90. [Article]
  2. Inoue A, Miki S, Seto M, Kikuchi T, Morita S, Ueda H, Misu Y, Nakata Y: Aripiprazole, a novel antipsychotic drug, inhibits quinpirole-evoked GTPase activity but does not up-regulate dopamine D2 receptor following repeated treatment in the rat striatum. Eur J Pharmacol. 1997 Feb 19;321(1):105-11. [Article]
  3. Wood MD, Scott C, Clarke K, Westaway J, Davies CH, Reavill C, Hill M, Rourke C, Newson M, Jones DN, Forbes IT, Gribble A: Aripiprazole and its human metabolite are partial agonists at the human dopamine D2 receptor, but the rodent metabolite displays antagonist properties. Eur J Pharmacol. 2006 Sep 28;546(1-3):88-94. Epub 2006 Jul 21. [Article]
  4. Kim E, Yu KS, Cho JY, Shin YW, Yoo SY, Kim YY, Jang IJ, Shin SG, Kwon JS: Effects of DRD2 and CYP2D6 genotypes on delta EEG power response to aripiprazole in healthy male volunteers: a preliminary study. Hum Psychopharmacol. 2006 Dec;21(8):519-28. [Article]
  5. Wood M, Reavill C: Aripiprazole acts as a selective dopamine D2 receptor partial agonist. Expert Opin Investig Drugs. 2007 Jun;16(6):771-5. [Article]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  7. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
  8. Cosi C, Carilla-Durand E, Assie MB, Ormiere AM, Maraval M, Leduc N, Newman-Tancredi A: Partial agonist properties of the antipsychotics SSR181507, aripiprazole and bifeprunox at dopamine D2 receptors: G protein activation and prolactin release. Eur J Pharmacol. 2006 Mar 27;535(1-3):135-44. doi: 10.1016/j.ejphar.2006.01.051. Epub 2006 Mar 22. [Article]
  9. FDA Approved Drug Products: ABILIFY (aripiprazole) tablets for oral use, orally disintegrating tablets, oral solution, injection for intramuscular use only (November 2022) [Link]
Kind
Protein
Organism
Humans
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. [Article]
  2. Stark AD, Jordan S, Allers KA, Bertekap RL, Chen R, Mistry Kannan T, Molski TF, Yocca FD, Sharp T, Kikuchi T, Burris KD: Interaction of the novel antipsychotic aripiprazole with 5-HT1A and 5-HT 2A receptors: functional receptor-binding and in vivo electrophysiological studies. Psychopharmacology (Berl). 2007 Feb;190(3):373-82. Epub 2006 Nov 25. [Article]
  3. Bortolozzi A, Diaz-Mataix L, Toth M, Celada P, Artigas F: In vivo actions of aripiprazole on serotonergic and dopaminergic systems in rodent brain. Psychopharmacology (Berl). 2007 Apr;191(3):745-58. Epub 2007 Jan 30. [Article]
  4. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
  5. FDA Approved Drug Products: ABILIFY (aripiprazole) tablets for oral use, orally disintegrating tablets, oral solution, injection for intramuscular use only (November 2022) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Partial agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da
References
  1. Jordan S, Koprivica V, Chen R, Tottori K, Kikuchi T, Altar CA: The antipsychotic aripiprazole is a potent, partial agonist at the human 5-HT1A receptor. Eur J Pharmacol. 2002 Apr 26;441(3):137-40. [Article]
  2. Marona-Lewicka D, Nichols DE: Aripiprazole (OPC-14597) fully substitutes for the 5-HT1A receptor agonist LY293284 in the drug discrimination assay in rats. Psychopharmacology (Berl). 2004 Apr;172(4):415-21. Epub 2003 Nov 28. [Article]
  3. Jordan S, Koprivica V, Dunn R, Tottori K, Kikuchi T, Altar CA: In vivo effects of aripiprazole on cortical and striatal dopaminergic and serotonergic function. Eur J Pharmacol. 2004 Jan 1;483(1):45-53. [Article]
  4. Swainston Harrison T, Perry CM: Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder. Drugs. 2004;64(15):1715-36. [Article]
  5. Cosi C, Waget A, Rollet K, Tesori V, Newman-Tancredi A: Clozapine, ziprasidone and aripiprazole but not haloperidol protect against kainic acid-induced lesion of the striatum in mice, in vivo: role of 5-HT1A receptor activation. Brain Res. 2005 May 10;1043(1-2):32-41. [Article]
  6. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
  7. FDA Approved Drug Products: ABILIFY (aripiprazole) tablets for oral use, orally disintegrating tablets, oral solution, injection for intramuscular use only (November 2022) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
Molecular Weight
51486.005 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1B
Uniprot ID
P35368
Uniprot Name
Alpha-1B adrenergic receptor
Molecular Weight
56835.375 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Details
6. Dopamine D3 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name
DRD3
Uniprot ID
P35462
Uniprot Name
D(3) dopamine receptor
Molecular Weight
44224.335 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Ligand
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1D
Uniprot ID
P28221
Uniprot Name
5-hydroxytryptamine receptor 1D
Molecular Weight
41906.38 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR7
Uniprot ID
P34969
Uniprot Name
5-hydroxytryptamine receptor 7
Molecular Weight
53554.43 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Antagonist
General Function
Thioesterase binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Antagonist
Other/unknown
General Function
Protein homodimerization activity
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name
ADRA2C
Uniprot ID
P18825
Uniprot Name
Alpha-2C adrenergic receptor
Molecular Weight
49521.585 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Details
11. Histamine H1 receptor
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Antagonist
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Ligand
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1B
Uniprot ID
P28222
Uniprot Name
5-hydroxytryptamine receptor 1B
Molecular Weight
43567.535 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
Molecular Weight
51820.705 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Voltage-gated potassium channel activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gate...
Gene Name
HTR3A
Uniprot ID
P46098
Uniprot Name
5-hydroxytryptamine receptor 3A
Molecular Weight
55279.835 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR6
Uniprot ID
P50406
Uniprot Name
5-hydroxytryptamine receptor 6
Molecular Weight
46953.625 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Details
16. Dopamine D1 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
Ligand
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name
DRD1
Uniprot ID
P21728
Uniprot Name
D(1A) dopamine receptor
Molecular Weight
49292.765 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Details
17. Dopamine D4 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
General Function
Sh3 domain binding
Specific Function
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins ...
Gene Name
DRD4
Uniprot ID
P21917
Uniprot Name
D(4) dopamine receptor
Molecular Weight
48359.86 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Antagonist
Ligand
General Function
Epinephrine binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine...
Gene Name
ADRA2B
Uniprot ID
P18089
Uniprot Name
Alpha-2B adrenergic receptor
Molecular Weight
49565.8 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Ligand
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that trig...
Gene Name
HTR1E
Uniprot ID
P28566
Uniprot Name
5-hydroxytryptamine receptor 1E
Molecular Weight
41681.57 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Details
20. Dopamine D5 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Partial agonist
Ligand
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name
DRD5
Uniprot ID
P21918
Uniprot Name
D(1B) dopamine receptor
Molecular Weight
52950.5 Da
References
  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
  2. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inverse agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation...
Gene Name
HTR2B
Uniprot ID
P41595
Uniprot Name
5-hydroxytryptamine receptor 2B
Molecular Weight
54297.41 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR5A
Uniprot ID
P47898
Uniprot Name
5-hydroxytryptamine receptor 5A
Molecular Weight
40254.69 Da
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Receptor signaling protein activity
Specific Function
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately e...
Gene Name
ADRB1
Uniprot ID
P08588
Uniprot Name
Beta-1 adrenergic receptor
Molecular Weight
51322.1 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Protein homodimerization activity
Specific Function
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately ...
Gene Name
ADRB2
Uniprot ID
P07550
Uniprot Name
Beta-2 adrenergic receptor
Molecular Weight
46458.32 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Histamine receptor activity
Specific Function
The H2 subclass of histamine receptors mediates gastric acid secretion. Also appears to regulate gastrointestinal motility and intestinal secretion. Possible role in regulating cell growth and diff...
Gene Name
HRH2
Uniprot ID
P25021
Uniprot Name
Histamine H2 receptor
Molecular Weight
40097.65 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Histamine receptor activity
Specific Function
The H3 subclass of histamine receptors could mediate the histamine signals in CNS and peripheral nervous system. Signals through the inhibition of adenylate cyclase and displays high constitutive a...
Gene Name
HRH3
Uniprot ID
Q9Y5N1
Uniprot Name
Histamine H3 receptor
Molecular Weight
48670.81 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Histamine receptor activity
Specific Function
The H4 subclass of histamine receptors could mediate the histamine signals in peripheral tissues. Displays a significant level of constitutive activity (spontaneous activity in the absence of agoni...
Gene Name
HRH4
Uniprot ID
Q9H3N8
Uniprot Name
Histamine H4 receptor
Molecular Weight
44495.375 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
Molecular Weight
51420.375 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
G-protein coupled acetylcholine receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM2
Uniprot ID
P08172
Uniprot Name
Muscarinic acetylcholine receptor M2
Molecular Weight
51714.605 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM3
Uniprot ID
P20309
Uniprot Name
Muscarinic acetylcholine receptor M3
Molecular Weight
66127.445 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Guanyl-nucleotide exchange factor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM4
Uniprot ID
P08173
Uniprot Name
Muscarinic acetylcholine receptor M4
Molecular Weight
53048.65 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM5
Uniprot ID
P08912
Uniprot Name
Muscarinic acetylcholine receptor M5
Molecular Weight
60073.205 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Opioid receptor activity
Specific Function
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synt...
Gene Name
OPRK1
Uniprot ID
P41145
Uniprot Name
Kappa-type opioid receptor
Molecular Weight
42644.665 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Voltage-gated calcium channel activity
Specific Function
Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone...
Gene Name
OPRM1
Uniprot ID
P35372
Uniprot Name
Mu-type opioid receptor
Molecular Weight
44778.855 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Opioid receptor activity
Specific Function
G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine n...
Gene Name
OPRD1
Uniprot ID
P41143
Uniprot Name
Delta-type opioid receptor
Molecular Weight
40368.235 Da
References
  1. de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3. [Article]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Voltage-gated cation channel activity
Specific Function
NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. This protein plays a key role in synaptic p...

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

Enzymes

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

Carriers

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

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Nagasaka Y, Oda K, Iwatsubo T, Kawamura A, Usui T: Effects of aripiprazole and its active metabolite dehydroaripiprazole on the activities of drug efflux transporters expressed both in the intestine and at the blood-brain barrier. Biopharm Drug Dispos. 2012 Sep;33(6):304-15. doi: 10.1002/bdd.1801. Epub 2012 Aug 18. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. Nagasaka Y, Oda K, Iwatsubo T, Kawamura A, Usui T: Effects of aripiprazole and its active metabolite dehydroaripiprazole on the activities of drug efflux transporters expressed both in the intestine and at the blood-brain barrier. Biopharm Drug Dispos. 2012 Sep;33(6):304-15. doi: 10.1002/bdd.1801. Epub 2012 Aug 18. [Article]

Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55