Identification

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Name
Brexpiprazole
Accession Number
DB09128
Type
Small Molecule
Groups
Approved, Investigational
Description

Brexpiprazole is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors. Brexpiprazole is approved for the treatment of schizophrenia, and as an adjunctive treatment for major depressive disorder (MDD). Although it failed Phase II clinical trials for ADHD, it has been designed to provide improved efficacy and tolerability (e.g., less akathisia, restlessness and/or insomnia) over established adjunctive treatments for major depressive disorder (MDD).

Structure
Thumb
Synonyms
  • Brexpiprazole
External IDs
OPC-34712
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
RexultiTablet2 mg/1OralOtsuka America Pharmaceutical, Inc.2015-07-10Not applicableUs
RexultiTablet2 mgOralOtsuka Pharmaceutical Co., Ltd.2017-04-19Not applicableCanada
RexultiTablet1 mg/1OralAvera McKennan Hospital2016-06-172018-06-15Us
RexultiTablet1 mgOralOtsuka Pharmaceutical Co., Ltd.2017-04-19Not applicableCanada
RexultiTablet1 mg/1OralOtsuka America Pharmaceutical, Inc.2015-07-10Not applicableUs
RexultiTablet4 mgOralOtsuka Pharmaceutical Co., Ltd.2017-04-19Not applicableCanada
RexultiTablet0.5 mg/1OralOtsuka America Pharmaceutical, Inc.2015-07-10Not applicableUs
RexultiTablet0.5 mgOralOtsuka Pharmaceutical Co., Ltd.2017-04-19Not applicableCanada
RexultiTablet4 mg/1OralOtsuka America Pharmaceutical, Inc.2015-07-10Not applicableUs
RexultiTablet3 mg/1OralOtsuka America Pharmaceutical, Inc.2015-07-10Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
RexultiBrexpiprazole (1 mg) + Brexpiprazole (2 mg)Kit; TabletOralOtsuka Pharmaceutical Co., Ltd.Not applicableNot applicableCanada
RexultiBrexpiprazole (1 mg) + Brexpiprazole (2 mg)Kit; TabletOralOtsuka Pharmaceutical Co., Ltd.Not applicableNot applicableCanada
RexultiBrexpiprazole (0.5 mg) + Brexpiprazole (1 mg)Kit; TabletOralOtsuka Pharmaceutical Co., Ltd.Not applicableNot applicableCanada
RexultiBrexpiprazole (0.5 mg) + Brexpiprazole (1 mg)Kit; TabletOralOtsuka Pharmaceutical Co., Ltd.Not applicableNot applicableCanada
Categories
UNII
2J3YBM1K8C
CAS number
913611-97-9
Weight
Average: 433.57
Monoisotopic: 433.182398295
Chemical Formula
C25H27N3O2S
InChI Key
ZKIAIYBUSXZPLP-UHFFFAOYSA-N
InChI
InChI=1S/C25H27N3O2S/c29-25-9-7-19-6-8-20(18-22(19)26-25)30-16-2-1-11-27-12-14-28(15-13-27)23-4-3-5-24-21(23)10-17-31-24/h3-10,17-18H,1-2,11-16H2,(H,26,29)
IUPAC Name
7-{4-[4-(1-benzothiophen-4-yl)piperazin-1-yl]butoxy}-1,2-dihydroquinolin-2-one
SMILES
O=C1NC2=CC(OCCCCN3CCN(CC3)C3=C4C=CSC4=CC=C3)=CC=C2C=C1

Pharmacology

Indication

As an adjunctive treatment of major depressive disorder (MDD) and for treatment of schizophrenia.

Associated Conditions
Pharmacodynamics
Not Available
Mechanism of action

Although the mechanism of action of brexpiprazole in the treatment of MDD and schizophrenia is unclear, the efficacy of brexpiprazole may be attributed to partial agonist activity at serotonin 1A and dopamine D2 receptors, and antagonist activity at serotonin 2A receptors.

TargetActionsOrganism
A5-hydroxytryptamine receptor 1A
agonist
partial agonist
Humans
AD(2) dopamine receptor
agonist
partial agonist
Humans
A5-hydroxytryptamine receptor 2A
antagonist
Humans
AAlpha-2C adrenergic receptor
antagonist
Humans
AAlpha-1B adrenergic receptor
antagonist
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

Brexpiprazole reaches peak plasma concentration within 4 hours of administration, and steady state occurs within 10-12 days of dosing. Oral bioavailability is 95%, and can be administered with or without food.

Volume of distribution

Intravenous volume of distribution is 1.56L/kg.

Protein binding

>99% protein bound in plasma to serum albumin and α1-acid glycoprotein. Based on in vitro studies, protein binding is not affected by warfarin, diazepam, or digitoxin.

Metabolism

Metabolized mainly by CYP3A4 and CYP2D6 enzymes into its major metabolite, DM-3411. DM-3411 is not considered to contribute any therapeutic effect.

Route of elimination

Approximately 25% urinary and 46% fecal excretion. <1% and ~14% of the unchanged drug was recovered in the urine and feces, respectively.

Half life

Brexpiprazole and its major metabolite, DM-3411 have half lives of 91 and 96 hours respectively.

Clearance

19.8mL/h/kg

Toxicity

The most commonly observed adverse effects include: weight increase, akathisia, somnolence, tremor and nasopharyngitis. Neonates are at risk for extrapyramidal and/or withdrawal symptoms if exposed to an antipsychotic drug during the third trimester of development.

Affected organisms
Not Available
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
(R)-warfarinThe risk or severity of adverse effects can be increased when Brexpiprazole is combined with (R)-warfarin.
(S)-WarfarinThe risk or severity of adverse effects can be increased when Brexpiprazole is combined with (S)-Warfarin.
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic AcidThe risk or severity of hypertension can be increased when 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid is combined with Brexpiprazole.
1-benzylimidazoleThe risk or severity of hypertension can be increased when 1-benzylimidazole is combined with Brexpiprazole.
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Brexpiprazole.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of serotonin syndrome can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Brexpiprazole.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of adverse effects can be increased when Brexpiprazole is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Brexpiprazole.
3,5-DinitrocatecholThe therapeutic efficacy of 3,5-Dinitrocatechol can be decreased when used in combination with Brexpiprazole.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of adverse effects can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Brexpiprazole.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Evidence Level

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
Not Available

References

General References
  1. Greig SL: Brexpiprazole: First Global Approval. Drugs. 2015 Sep;75(14):1687-97. doi: 10.1007/s40265-015-0462-2. [PubMed:26310190]
  2. Citrome L, Stensbol TB, Maeda K: The preclinical profile of brexpiprazole: what is its clinical relevance for the treatment of psychiatric disorders? Expert Rev Neurother. 2015 Oct;15(10):1219-29. doi: 10.1586/14737175.2015.1086269. Epub 2015 Sep 24. [PubMed:26402059]
  3. Citrome L: Brexpiprazole for schizophrenia and as adjunct for major depressive disorder: a systematic review of the efficacy and safety profile for this newly approved antipsychotic - what is the number needed to treat, number needed to harm and likelihood to be helped or harmed? Int J Clin Pract. 2015 Sep;69(9):978-97. doi: 10.1111/ijcp.12714. Epub 2015 Aug 6. [PubMed:26250067]
External Links
KEGG Drug
D10309
PubChem Compound
11978813
PubChem Substance
310265043
ChemSpider
10152155
BindingDB
194780
ChEBI
134716
ChEMBL
CHEMBL2105760
PharmGKB
PA166160053
Wikipedia
Brexpiprazole
ATC Codes
N05AX16 — Brexpiprazole
AHFS Codes
  • 28:16.08.04 — Atypical Antipsychotics
FDA label
Download (943 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingOtherHealth1
1Active Not RecruitingOtherHealthy Volunteers1
1CompletedBasic ScienceSchizophrenic Disorders1
1CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Autism, Early Infantile / Bipolar I Disorder / Oppositional Defiant Disorder1
1CompletedTreatmentHealthy Adult Males1
1CompletedTreatmentMajor Depressive Disorder (MDD)1
1CompletedTreatmentPsychiatric Disorders / Schizophrenic Disorders1
1CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
1CompletedTreatmentSchizophrenic Disorders3
1TerminatedHealth Services ResearchSchizophrenic Disorders1
2CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)1
2CompletedTreatmentMajor Depressive Disorder (MDD)3
2CompletedTreatmentPost Traumatic Stress Disorder (PTSD)1
2CompletedTreatmentSchizophrenic Disorders2
2RecruitingTreatmentBorderline Personality Disorder (BPD)1
2RecruitingTreatmentSchizophrenic Disorders1
2TerminatedTreatmentPost Traumatic Stress Disorder (PTSD)1
2, 3CompletedTreatmentSchizophrenic Disorders1
2, 3RecruitingTreatmentAgitation Associated With Dementia of the Alzheimer's Type1
2, 3RecruitingTreatmentMajor Depressive Disorder (MDD)1
3Active Not RecruitingTreatmentAcute Mania / Bipolar I Disorder1
3CompletedTreatmentAcute Schizophrenia3
3CompletedTreatmentAgitation Associated With / Alzheimer's Disease (AD) / Alzheimer's Type / Nervous System Diseases / Psychiatric Disorder NOS2
3CompletedTreatmentAcute Manic episode / Bipolar I Disorder2
3CompletedTreatmentDepression / Depressive Disorders / Major Depressive Disorder (MDD) / Moods Disorders / Psychiatric Disorder NOS5
3CompletedTreatmentFeeling Anxious / Major Depressive Disorder (MDD)1
3CompletedTreatmentIrritability / Major Depressive Disorder (MDD)1
3CompletedTreatmentMajor Depressive Disorder (MDD)3
3CompletedTreatmentSchizophrenia With Impulsivity1
3CompletedTreatmentSchizophrenic Disorders6
3CompletedTreatmentSleep Disturbances1
3RecruitingSupportive CareSchizophrenic Disorders1
3RecruitingTreatmentAgitation Associated With Dementia of the Alzheimer's Type1
3RecruitingTreatmentAgitaton Associated With Alzheimer's Dementia / Alzheimer Dementia (AD)1
3RecruitingTreatmentAlzheimer's Disease (AD)1
3RecruitingTreatmentMajor Depressive Disorder (MDD)2
3RecruitingTreatmentSchizophrenic Disorders2
3TerminatedTreatmentMajor Depressive Disorder (MDD)3
3TerminatedTreatmentPost Traumatic Stress Disorder (PTSD)1
3WithdrawnTreatmentMajor Depressive Disorder and Irritability1
3WithdrawnTreatmentSchizophrenic Disorders1
4Active Not RecruitingTreatmentDepression1
4CompletedTreatmentDepression, Bipolar1
4RecruitingTreatmentSchizoaffective Disorders / Schizophrenic Disorders / Substance Use Disorder (SUD)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Kit; tabletOral
TabletOral0.25 mg/1
TabletOral0.25 mg
TabletOral0.5 mg
TabletOral0.5 mg/1
TabletOral1 mg/1
TabletOral1 mg
TabletOral2 mg/1
TabletOral2 mg
TabletOral3 mg/1
TabletOral3 mg
TabletOral4 mg/1
TabletOral4 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8349840No2013-01-082026-04-12Us
US8618109No2013-12-312026-04-12Us
US7888362No2011-02-152027-02-23Us
US9839637No2017-12-122026-04-12Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

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Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00227 mg/mLALOGPS
logP5.38ALOGPS
logP4.65ChemAxon
logS-5.3ALOGPS
pKa (Strongest Acidic)13.56ChemAxon
pKa (Strongest Basic)8.4ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area44.81 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity129.16 m3·mol-1ChemAxon
Polarizability49.48 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
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

Taxonomy

Description
This compound belongs to the class of organic compounds known as n-arylpiperazines. These are organic compounds containing a piperazine ring where the nitrogen ring atom carries an aryl group.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazinanes
Sub Class
Piperazines
Direct Parent
N-arylpiperazines
Alternative Parents
Hydroquinolones / Hydroquinolines / 1-benzothiophenes / Dialkylarylamines / N-alkylpiperazines / Pyridinones / Alkyl aryl ethers / Benzenoids / Thiophenes / Heteroaromatic compounds
show 6 more
Substituents
N-arylpiperazine / Dihydroquinolone / Dihydroquinoline / Quinoline / Benzothiophene / 1-benzothiophene / Dialkylarylamine / Tertiary aliphatic/aromatic amine / Alkyl aryl ether / Pyridinone
show 19 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
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. Maeda K, Sugino H, Akazawa H, Amada N, Shimada J, Futamura T, Yamashita H, Ito N, McQuade RD, Mork A, Pehrson AL, Hentzer M, Nielsen V, Bundgaard C, Arnt J, Stensbol TB, Kikuchi T: Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator. J Pharmacol Exp Ther. 2014 Sep;350(3):589-604. doi: 10.1124/jpet.114.213793. Epub 2014 Jun 19. [PubMed:24947465]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
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. Maeda K, Sugino H, Akazawa H, Amada N, Shimada J, Futamura T, Yamashita H, Ito N, McQuade RD, Mork A, Pehrson AL, Hentzer M, Nielsen V, Bundgaard C, Arnt J, Stensbol TB, Kikuchi T: Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator. J Pharmacol Exp Ther. 2014 Sep;350(3):589-604. doi: 10.1124/jpet.114.213793. Epub 2014 Jun 19. [PubMed:24947465]
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. Maeda K, Sugino H, Akazawa H, Amada N, Shimada J, Futamura T, Yamashita H, Ito N, McQuade RD, Mork A, Pehrson AL, Hentzer M, Nielsen V, Bundgaard C, Arnt J, Stensbol TB, Kikuchi T: Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator. J Pharmacol Exp Ther. 2014 Sep;350(3):589-604. doi: 10.1124/jpet.114.213793. Epub 2014 Jun 19. [PubMed:24947465]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
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. Oosterhof CA, El Mansari M, Blier P: Acute effects of brexpiprazole on serotonin, dopamine, and norepinephrine systems: an in vivo electrophysiologic characterization. J Pharmacol Exp Ther. 2014 Dec;351(3):585-95. doi: 10.1124/jpet.114.218578. Epub 2014 Sep 15. [PubMed:25225185]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
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. Oosterhof CA, El Mansari M, Blier P: Acute effects of brexpiprazole on serotonin, dopamine, and norepinephrine systems: an in vivo electrophysiologic characterization. J Pharmacol Exp Ther. 2014 Dec;351(3):585-95. doi: 10.1124/jpet.114.218578. Epub 2014 Sep 15. [PubMed:25225185]

Enzymes

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. Greig SL: Brexpiprazole: First Global Approval. Drugs. 2015 Sep;75(14):1687-97. doi: 10.1007/s40265-015-0462-2. [PubMed:26310190]
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. Greig SL: Brexpiprazole: First Global Approval. Drugs. 2015 Sep;75(14):1687-97. doi: 10.1007/s40265-015-0462-2. [PubMed:26310190]

Drug created on September 28, 2015 17:01 / Updated on May 24, 2019 23:09