Norepinephrine

Identification

Summary

Norepinephrine is a sympathomimetic used in the control of blood pressure during various hypotensive states and as an adjunct treatment during cardiac arrest.

Brand Names
Levophed
Generic Name
Norepinephrine
DrugBank Accession Number
DB00368
Background

Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 169.1778
Monoisotopic: 169.073893223
Chemical Formula
C8H11NO3
Synonyms
  • (−)-arterenol
  • (−)-noradrenaline
  • (−)-norepinephrine
  • (R)-(−)-norepinephrine
  • (R)-4-(2-amino-1-hydroxyethyl)-1,2-benzenediol
  • (R)-noradrenaline
  • (R)-norepinephrine
  • 4-[(1R)-2-Amino-1-hydroxyethyl]-1,2-benzenediol
  • Arterenol
  • L-noradrenaline
  • L-Norepinephrine
  • Nor-adrenaline
  • Noradrenaline
  • Norepinefrina
  • Norepinephrine
  • Norépinéphrine
  • Norepinephrinum

Pharmacology

Indication

Mainly used to treat patients in vasodilatory shock states such as septic shock and neurogenic shock and has shown a survival benefit over dopamine. Also used as a vasopressor medication for patients with critical hypotension.

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Adjunct therapy in management ofCardiac arrest••••••••••••
Adjunct therapy in management ofSevere hypotension••••••••••••
Management ofShock••••••••••••
Management ofAcute, severe hypotension•••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Noradrenaline acts on both alpha-1 and alpha-2 adrenergic receptors to cause vasoconstriction. Its effect in-vitro is often limited to the increasing of blood pressure through antagonising alpha-1 and alpha-2 receptors and causing a resultant increase in systemic vascular resistance.

Mechanism of action

Norepinephrine functions as a peripheral vasoconstrictor by acting on alpha-adrenergic receptors. It is also an inotropic stimulator of the heart and dilator of coronary arteries as a result of it's activity at the beta-adrenergic receptors.

TargetActionsOrganism
AAlpha-1A adrenergic receptor
agonist
Humans
AAlpha-1B adrenergic receptor
agonist
Humans
AAlpha-1D adrenergic receptor
agonist
Humans
AAlpha-2A adrenergic receptor
agonist
Humans
AAlpha-2B adrenergic receptor
agonist
Humans
AAlpha-2C adrenergic receptor
agonist
Humans
ABeta-1 adrenergic receptor
agonist
Humans
ABeta-2 adrenergic receptor
agonist
Humans
ABeta-3 adrenergic receptor
agonist
Humans
NPhenylalanine-4-hydroxylase
inhibitor
Humans
USynaptic vesicular amine transporter
binder
Humans
UChromaffin granule amine transporter
binder
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Hover over products below to view reaction partners

Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

In high dose and especially when it is combined with other vasopressors, it can lead to limb ischemia and limb death.

Pathways
PathwayCategory
Aromatic L-Aminoacid Decarboxylase DeficiencyDisease
Benzocaine Action PathwayDrug action
Bupivacaine Action PathwayDrug action
Lidocaine (Local Anaesthetic) Action PathwayDrug action
Proparacaine Action PathwayDrug action
Codeine Action PathwayDrug action
Hydromorphone Action PathwayDrug action
Fentanyl Action PathwayDrug action
Sufentanil Action PathwayDrug action
Methadyl Acetate Action PathwayDrug action
Dimethylthiambutene Action PathwayDrug action
Dihydromorphine Action PathwayDrug action
Ketobemidone Action PathwayDrug action
AlkaptonuriaDisease
HawkinsinuriaDisease
Oxybuprocaine Action PathwayDrug action
Morphine Action PathwayDrug action
Hydrocodone Action PathwayDrug action
Oxymorphone Action PathwayDrug action
Remifentanil Action PathwayDrug action
Fluoxetine Action PathwayDrug action
Nicotine Action PathwayDrug action
Tyrosinemia, Transient, of the NewbornDisease
Tyrosine Hydroxylase DeficiencyDisease
Dopamine beta-Hydroxylase DeficiencyDisease
Monoamine Oxidase-A Deficiency (MAO-A)Disease
Propoxyphene Action PathwayDrug action
Anileridine Action PathwayDrug action
3-Methylthiofentanyl Action PathwayDrug action
Levallorphan Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AcebutololThe therapeutic efficacy of Acebutolol can be increased when used in combination with Norepinephrine.
AceclofenacThe risk or severity of hypertension can be increased when Norepinephrine is combined with Aceclofenac.
AcemetacinThe risk or severity of hypertension can be increased when Norepinephrine is combined with Acemetacin.
AcetazolamideThe risk or severity of Cardiac Arrhythmia can be increased when Norepinephrine is combined with Acetazolamide.
AcetyldigitoxinThe risk or severity of Cardiac Arrhythmia can be increased when Norepinephrine is combined with Acetyldigitoxin.
Food Interactions
No interactions found.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Norepinephrine bitartrateIFY5PE3ZRW108341-18-0LNBCGLZYLJMGKP-LUDZCAPTSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
LevophedSolution1 mg / mLIntravenousPfizer Canada Ulc2001-10-01Not applicableCanada flag
LevophedInjection, solution, concentrate1 mg/1mLIntravenousHospira, Inc.2024-03-11Not applicableUS flag
LevophedInjection, solution, concentrate1 mg/1mLIntravenousHospira, Inc.2005-04-302019-05-01US flag
LevophedInjection, solution, concentrate1 mg/1mLIntravenousHospira, Inc.2009-04-27Not applicableUS flag
LevophedInjection, solution, concentrate1 mg/1mLIntravenousGeneral Injectables & Vaccines, Inc2010-03-012019-05-01US flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Norepinephr BitartInjection, solution, concentrate1 mg/1mLIntravenousDelpharm Boucherville Canada Inc.2019-04-23Not applicableUS flag
NorepinephrineInjection1 mg/1mLIntravenousBedford Pharmaceuticals2003-11-172012-02-29US flag
Norepinephrine BitartrateInjection1 mg/1mLIntravenousHF Acquisition Co LLC, DBA HealthFirst2021-08-08Not applicableUS flag
Norepinephrine BitartrateInjection, solution, concentrate1 mg/1mLIntravenousBreckenridge Pharmaceutical, Inc.2021-07-01Not applicableUS flag
Norepinephrine BitartrateSolution1 mg/1mLIntravenousFresenius Kabi USA, LLC2021-03-01Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
XYLONOR %3 NORADRENALINE ENJEKSIYONLUK SOLUSYON ICEREN KULLANIMA HAZIR 50 KARTUSNorepinephrine bitartrate (0.08 mg/mL) + Lidocaine (30 mg/mL)Injection, solutionFARMALİNK SAĞLIK ÜRÜNLERİ SAN. VE TİC.LTD.2010-12-31Not applicableTurkey flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Norepinephrine BitartrateNorepinephrine bitartrate (16 ug/1mL)Injection, solutionIntravenousCantrell Drug Company2015-02-202017-12-06US flag
Norepinephrine BitartrateNorepinephrine bitartrate (32 ug/1mL)Injection, solutionIntravenousCantrell Drug Company2012-04-122015-03-06US flag
Norepinephrine BitartrateNorepinephrine bitartrate (32 ug/1mL)Injection, solutionIntravenousCantrell Drug Company2015-02-182017-12-06US flag
Norepinephrine BitartrateNorepinephrine bitartrate (16 ug/1mL)Injection, solutionIntravenousCantrell Drug Company2015-03-06Not applicableUS flag
Norepinephrine BitartrateNorepinephrine bitartrate (64 ug/1mL)Injection, solutionIntravenousCantrell Drug Company2012-06-222015-03-12US flag

Categories

ATC Codes
C01CA03 — Norepinephrine
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as catechols. These are compounds containing a 1,2-benzenediol moiety.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Phenols
Sub Class
Benzenediols
Direct Parent
Catechols
Alternative Parents
Aralkylamines / 1-hydroxy-4-unsubstituted benzenoids / 1-hydroxy-2-unsubstituted benzenoids / Benzene and substituted derivatives / Secondary alcohols / 1,2-aminoalcohols / Organopnictogen compounds / Monoalkylamines / Hydrocarbon derivatives / Aromatic alcohols
Substituents
1,2-aminoalcohol / 1-hydroxy-2-unsubstituted benzenoid / 1-hydroxy-4-unsubstituted benzenoid / Alcohol / Amine / Aralkylamine / Aromatic alcohol / Aromatic homomonocyclic compound / Catechol / Hydrocarbon derivative
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
noradrenaline (CHEBI:18357) / Biogenic amines, Adrenalines (C00547)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
X4W3ENH1CV
CAS number
51-41-2
InChI Key
SFLSHLFXELFNJZ-QMMMGPOBSA-N
InChI
InChI=1S/C8H11NO3/c9-4-8(12)5-1-2-6(10)7(11)3-5/h1-3,8,10-12H,4,9H2/t8-/m0/s1
IUPAC Name
4-[(1R)-2-amino-1-hydroxyethyl]benzene-1,2-diol
SMILES
NC[C@H](O)C1=CC(O)=C(O)C=C1

References

General References
Not Available
Human Metabolome Database
HMDB0000216
KEGG Drug
D00076
KEGG Compound
C00547
PubChem Compound
439260
PubChem Substance
46506201
ChemSpider
388394
BindingDB
50029051
RxNav
7512
ChEBI
18357
ChEMBL
CHEMBL1437
ZINC
ZINC000000057624
Therapeutic Targets Database
DNC001034
PharmGKB
PA450649
PDBe Ligand
LNR
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Norepinephrine
PDB Entries
2qeo / 3dye / 3hcd / 4pah / 4y4j / 6m0z / 6m2r

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentPost Traumatic Stress Disorder (PTSD)1
4CompletedBasic ScienceEndotoxaemia1
4CompletedDiagnosticBipolar Disorder (BD) / Major Depressive Disorder (MDD)1
4CompletedDiagnosticBlood Pressures / Ventricular Dysfunction, Right1
4CompletedDiagnosticFree Flaps / Head And Neck Cancer / Hypotension / Oral Cancer1

Pharmacoeconomics

Manufacturers
  • Hospira inc
Packagers
  • Bedford Labs
  • Cardinal Health
  • Draxis Specialty Pharmaceuticals Inc.
  • Hospira Inc.
  • Paddock Labs
  • Pharmedium
  • Sicor Pharmaceuticals
  • Teva Pharmaceutical Industries Ltd.
Dosage Forms
FormRouteStrength
SolutionIntravenous7.548 mg
Injection, solution, concentrateIntravenous25 mg/25ml
Injection, solution, concentrateIntravenous4 mg/4ml
SolutionIntravenous7.7976 mg
InjectionIntravenous1 mg/ml
InjectionIntravenous4 mg/4ml
LiquidIntravenous1 mg / mL
SolutionIntravenous1 mg/ml
SolutionIntravenous7.974 mg
Injection, solutionParenteral5 Mikrogramm/ml
Injection, solutionIntravenous
SolutionIntravenous4.000 mg
SolutionParenteral4.000 mg
SolutionParenteral0.08 mg/ml
SolutionParenteral0.25 mg/ml
Injection, solution, concentrateIntravenous1 MG/ML
Injection, solutionParenteral0.16 MG/ML
Injection, solutionParenteral0.5 MG/ML
Injection, solution, concentrateIntravenous; Parenteral2 MG/ML
Injection, solution0.4 mg/ml
Injection, solution
Injection, solution, concentrateIntravenous
Injection, solution1 MG/ML
Injection, solution1 mg/1ml
Injection, solutionIntravenous1 mg/ml
SolutionIntravenous7.55 mg
SolutionIntravenous4 mg
InjectionIntravenous1 mg/1mL
SolutionIntravenous16 ug/1mL
SolutionIntravenous32 ug/1mL
SolutionIntravenous64 ug/1mL
InjectionIntravenous
Injection, solutionIntravenous16 ug/1mL
Injection, solutionIntravenous16 mg/250mL
Injection, solutionIntravenous32 ug/1mL
Injection, solutionIntravenous4 mg/250mL
Injection, solutionIntravenous64 ug/1mL
Injection, solutionIntravenous8 mg/250mL
Injection, solution, concentrateIntravenous1 mg/1mL
SolutionIntravenous1 mg/1mL
SolutionIntravenous0.016 mg / mL
SolutionIntravenous0.032 mg / mL
Injection, solutionIntravenous0.016 mg/1mL
Injection, solutionIntravenous0.032 mg/1mL
Injection, solutionIntravenous0.064 mg/1mL
SolutionIntravenous1 mg / mL
SolutionIntravenous4.00 mg
SolutionParenteral0.06 mg/ml
SolutionParenteral0.1 mg/ml
SolutionParenteral0.12 mg/ml
SolutionParenteral0.2 mg/ml
SolutionIntravenous7.97 mg
Injection, solution10 MICROGRAMMI/ML
Injection, solution
Solution1 mg/1ml
Injection, solutionIntravenous1 mg/1ml
Prices
Unit descriptionCostUnit
Norepinephrine 4 mg/4 ml amp2.68USD ml
Levophed 1 mg/ml ampul1.49USD ml
Norepinephrine 1 mg/ml vial0.96USD ml
Levophed 1 mg/ml vial0.48USD ml
Norepinephrine-d5w 4 mg/250 ml0.16USD ml
Norepinephrine-ns 4 mg/250 ml0.16USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US10888534No2021-01-122039-04-26US flag
US11413259No2018-01-302038-01-30US flag
US10420735No2019-09-242038-01-30US flag
US10226436No2019-03-122038-01-30US flag
US10159657No2018-12-252038-01-30US flag
US10568850No2020-02-252038-01-30US flag
US11602508No2018-01-302038-01-30US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)217 dec °CPhysProp
logP-1.24HANSCH,C ET AL. (1995)
pKa8.58PERRIN,DD (1965)
Predicted Properties
PropertyValueSource
Water Solubility12.5 mg/mLALOGPS
logP-1.4ALOGPS
logP-0.68Chemaxon
logS-1.1ALOGPS
pKa (Strongest Acidic)9.5Chemaxon
pKa (Strongest Basic)8.85Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count4Chemaxon
Hydrogen Donor Count4Chemaxon
Polar Surface Area86.71 Å2Chemaxon
Rotatable Bond Count2Chemaxon
Refractivity44.46 m3·mol-1Chemaxon
Polarizability16.96 Å3Chemaxon
Number of Rings1Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9837
Blood Brain Barrier-0.9762
Caco-2 permeable-0.7985
P-glycoprotein substrateNon-substrate0.6046
P-glycoprotein inhibitor INon-inhibitor0.9441
P-glycoprotein inhibitor IINon-inhibitor0.9285
Renal organic cation transporterNon-inhibitor0.9004
CYP450 2C9 substrateNon-substrate0.8702
CYP450 2D6 substrateNon-substrate0.8667
CYP450 3A4 substrateNon-substrate0.7986
CYP450 1A2 substrateNon-inhibitor0.9135
CYP450 2C9 inhibitorNon-inhibitor0.9675
CYP450 2D6 inhibitorNon-inhibitor0.9798
CYP450 2C19 inhibitorNon-inhibitor0.9446
CYP450 3A4 inhibitorNon-inhibitor0.9209
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8839
Ames testNon AMES toxic0.5053
CarcinogenicityNon-carcinogens0.8942
BiodegradationReady biodegradable0.5401
Rat acute toxicity2.2298 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9028
hERG inhibition (predictor II)Non-inhibitor0.7864
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
GC-MS Spectrum - GC-MS (5 TMS)GC-MSsplash10-00di-1900000000-c9b4a0a230d610dd0e61
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-001i-7900000000-ce77a851a3951304f4d0
GC-MS Spectrum - EI-BGC-MSsplash10-000l-4900000000-b0893c23c186c5f8a344
GC-MS Spectrum - GC-MSGC-MSsplash10-00di-1900000000-c9b4a0a230d610dd0e61
MS/MS Spectrum - Quattro_QQQ 10V, N/A (Annotated)LC-MS/MSsplash10-0udi-0900000000-5610e21bd478a4ca7bde
MS/MS Spectrum - Quattro_QQQ 25V, N/A (Annotated)LC-MS/MSsplash10-0a6r-5900000000-5d7cd24a6af23a36af3a
MS/MS Spectrum - Quattro_QQQ 40V, N/A (Annotated)LC-MS/MSsplash10-004i-9000000000-3c8de1511861fa1d028c
MS/MS Spectrum - EI-B (HITACHI M-80) , PositiveLC-MS/MSsplash10-000l-4900000000-b0893c23c186c5f8a344
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 10V, PositiveLC-MS/MSsplash10-0udi-0900000000-11725b1d61843966aa7c
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 20V, PositiveLC-MS/MSsplash10-0udi-1900000000-6931e73a397f3917ad96
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 30V, PositiveLC-MS/MSsplash10-0a4i-3900000000-bddd6ee748aa9ebecb15
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 40V, PositiveLC-MS/MSsplash10-056r-9500000000-6abd3337785c1b580668
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 50V, PositiveLC-MS/MSsplash10-004i-9100000000-ede02e0e3e74bdddc9f4
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0udi-0900000000-11725b1d61843966aa7c
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0udi-1900000000-6931e73a397f3917ad96
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0a4i-3900000000-918c4cbdffc5e02eafd5
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-056r-9500000000-6abd3337785c1b580668
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-004i-9100000000-ede02e0e3e74bdddc9f4
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0f79-0900000000-896484e430e3087072a9
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-014i-0900000000-49133b6a8427bb3f1ca7
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-000i-0900000000-0627daf392c4b672c266
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-00dr-0900000000-545365e11d4807acbd03
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0ff0-7900000000-270051fc2fc1371045c1
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0a59-7900000000-f0efc4da363b1812a0d9
13C NMR Spectrum1D NMRNot Applicable
1H NMR Spectrum1D NMRNot Applicable
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-141.0314961
predicted
DarkChem Lite v0.1.0
[M-H]-133.6656269
predicted
DarkChem Standard v0.1.0
[M-H]-140.8243961
predicted
DarkChem Lite v0.1.0
[M-H]-140.6239961
predicted
DarkChem Lite v0.1.0
[M-H]-137.99013
predicted
DeepCCS 1.0 (2019)
[M+H]+141.7213961
predicted
DarkChem Lite v0.1.0
[M+H]+141.8932961
predicted
DarkChem Lite v0.1.0
[M+H]+141.7634961
predicted
DarkChem Lite v0.1.0
[M+H]+141.6445961
predicted
DarkChem Lite v0.1.0
[M+H]+140.38571
predicted
DeepCCS 1.0 (2019)
[M+Na]+141.2930961
predicted
DarkChem Lite v0.1.0
[M+Na]+141.0862961
predicted
DarkChem Lite v0.1.0
[M+Na]+140.9580961
predicted
DarkChem Lite v0.1.0
[M+Na]+140.8363961
predicted
DarkChem Lite v0.1.0
[M+Na]+147.78914
predicted
DeepCCS 1.0 (2019)

Targets

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Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
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Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Lachnit WG, Tran AM, Clarke DE, Ford AP: Pharmacological characterization of an alpha 1A-adrenoceptor mediating contractile responses to noradrenaline in isolated caudal artery of rat. Br J Pharmacol. 1997 Mar;120(5):819-26. [Article]
  4. Burt RP, Chapple CR, Marshall I: The role of diacylglycerol and activation of protein kinase C in alpha 1A-adrenoceptor-mediated contraction to noradrenaline of rat isolated epididymal vas deferens. Br J Pharmacol. 1996 Jan;117(1):224-30. [Article]
  5. Bishop MJ: Recent advances in the discovery of alpha1-adrenoceptor agonists. Curr Top Med Chem. 2007;7(2):135-45. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Izzo NJ Jr, Tulenko TN, Colucci WS: Phorbol esters and norepinephrine destabilize alpha 1B-adrenergic receptor mRNA in vascular smooth muscle cells. J Biol Chem. 1994 Jan 21;269(3):1705-10. [Article]
  4. Testa R, Guarneri L, Poggesi E, Simonazzi I, Taddei C, Leonardi A: Mediation of noradrenaline-induced contractions of rat aorta by the alpha 1B-adrenoceptor subtype. Br J Pharmacol. 1995 Feb;114(4):745-50. [Article]
  5. Izzo NJ Jr, Colucci WS: Regulation of alpha 1B-adrenergic receptor half-life: protein synthesis dependence and effect of norepinephrine. Am J Physiol. 1994 Mar;266(3 Pt 1):C771-5. [Article]
  6. Bishop MJ: Recent advances in the discovery of alpha1-adrenoceptor agonists. Curr Top Med Chem. 2007;7(2):135-45. [Article]
  7. Gilsbach R, Hein L: Presynaptic metabotropic receptors for acetylcholine and adrenaline/noradrenaline. Handb Exp Pharmacol. 2008;(184):261-88. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Alpha1-adrenergic receptor activity
Specific Function
This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
Gene Name
ADRA1D
Uniprot ID
P25100
Uniprot Name
Alpha-1D adrenergic receptor
Molecular Weight
60462.205 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Cleary L, Slattery J, Bexis S, Docherty JR: Sympathectomy reveals alpha 1A- and alpha 1D-adrenoceptor components to contractions to noradrenaline in rat vas deferens. Br J Pharmacol. 2004 Nov;143(6):745-52. Epub 2004 Sep 27. [Article]
  4. Kenny BA, Chalmers DH, Philpott PC, Naylor AM: Characterization of an alpha 1D-adrenoceptor mediating the contractile response of rat aorta to noradrenaline. Br J Pharmacol. 1995 Jul;115(6):981-6. [Article]
  5. Testa R, Destefani C, Guarneri L, Poggesi E, Simonazzi I, Taddei C, Leonardi A: The alpha 1d-adrenoceptor subtype is involved in the noradrenaline-induced contractions of rat aorta. Life Sci. 1995;57(13):PL159-63. [Article]
  6. Bishop MJ: Recent advances in the discovery of alpha1-adrenoceptor agonists. Curr Top Med Chem. 2007;7(2):135-45. [Article]
  7. Gilsbach R, Hein L: Presynaptic metabotropic receptors for acetylcholine and adrenaline/noradrenaline. Handb Exp Pharmacol. 2008;(184):261-88. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Nyronen T, Pihlavisto M, Peltonen JM, Hoffren AM, Varis M, Salminen T, Wurster S, Marjamaki A, Kanerva L, Katainen E, Laaksonen L, Savola JM, Scheinin M, Johnson MS: Molecular mechanism for agonist-promoted alpha(2A)-adrenoceptor activation by norepinephrine and epinephrine. Mol Pharmacol. 2001 May;59(5):1343-54. [Article]
  4. MacLennan SJ, Reynen PH, Martin RS, Eglen RM, Martin GR: Characterization of human recombinant alpha(2A)-adrenoceptors expressed in Chinese hamster lung cells using extracellular acidification rate changes. Br J Pharmacol. 2000 Apr;129(7):1333-8. [Article]
  5. Hieble JP, Hehr A, Li YO, Ruffolo RR Jr: Molecular basis for the stereoselective interactions of catecholamines with alpha-adrenoceptors. Proc West Pharmacol Soc. 1998;41:225-8. [Article]
  6. Nash DT: Alpha-adrenergic blockers: mechanism of action, blood pressure control, and effects of lipoprotein metabolism. Clin Cardiol. 1990 Nov;13(11):764-72. [Article]
  7. Giovannoni MP, Ghelardini C, Vergelli C, Dal Piaz V: Alpha2-agonists as analgesic agents. Med Res Rev. 2009 Mar;29(2):339-68. doi: 10.1002/med.20134. [Article]
  8. Gilsbach R, Hein L: Presynaptic metabotropic receptors for acetylcholine and adrenaline/noradrenaline. Handb Exp Pharmacol. 2008;(184):261-88. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Gobbi M, Frittoli E, Mennini T: The modulation of [3H]noradrenaline and [3H]serotonin release from rat brain synaptosomes is not mediated by the alpha 2B-adrenoceptor subtype. Naunyn Schmiedebergs Arch Pharmacol. 1990 Oct;342(4):382-6. [Article]
  4. Vizi ES, Katona I, Freund TF: Evidence for presynaptic cannabinoid CB(1) receptor-mediated inhibition of noradrenaline release in the guinea pig lung. Eur J Pharmacol. 2001 Nov 16;431(2):237-44. [Article]
  5. Rudling JE, Richardson J, Evans PD: A comparison of agonist-specific coupling of cloned human alpha(2)-adrenoceptor subtypes. Br J Pharmacol. 2000 Nov;131(5):933-41. [Article]
  6. Nash DT: Alpha-adrenergic blockers: mechanism of action, blood pressure control, and effects of lipoprotein metabolism. Clin Cardiol. 1990 Nov;13(11):764-72. [Article]
  7. Gilsbach R, Hein L: Presynaptic metabotropic receptors for acetylcholine and adrenaline/noradrenaline. Handb Exp Pharmacol. 2008;(184):261-88. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Shreve PE, Toews ML, Bylund DB: Alpha 2A- and alpha 2C-adrenoceptor subtypes are differentially down-regulated by norepinephrine. Eur J Pharmacol. 1991 Jul 12;207(3):275-6. [Article]
  4. Rump LC, Bohmann C, Schaible U, Schollhorn J, Limberger N: Alpha 2C-adrenoceptor-modulated release of noradrenaline in human right atrium. Br J Pharmacol. 1995 Nov;116(6):2617-24. [Article]
  5. Bruck H, Schwerdtfeger T, Toliat M, Leineweber K, Heusch G, Philipp T, Nurnberg P, Brodde OE: Presynaptic alpha-2C adrenoceptor-mediated control of noradrenaline release in humans: genotype- or age-dependent? Clin Pharmacol Ther. 2007 Nov;82(5):525-30. Epub 2007 Apr 4. [Article]
  6. Nash DT: Alpha-adrenergic blockers: mechanism of action, blood pressure control, and effects of lipoprotein metabolism. Clin Cardiol. 1990 Nov;13(11):764-72. [Article]
  7. Gilsbach R, Hein L: Presynaptic metabotropic receptors for acetylcholine and adrenaline/noradrenaline. Handb Exp Pharmacol. 2008;(184):261-88. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  2. Mersmann HJ: Overview of the effects of beta-adrenergic receptor agonists on animal growth including mechanisms of action. J Anim Sci. 1998 Jan;76(1):160-72. [Article]
  3. El-Armouche A, Eschenhagen T: Beta-adrenergic stimulation and myocardial function in the failing heart. Heart Fail Rev. 2009 Dec;14(4):225-41. doi: 10.1007/s10741-008-9132-8. [Article]
  4. Gilsbach R, Hein L: Presynaptic metabotropic receptors for acetylcholine and adrenaline/noradrenaline. Handb Exp Pharmacol. 2008;(184):261-88. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Sanders VM: The role of norepinephrine and beta-2-adrenergic receptor stimulation in the modulation of Th1, Th2, and B lymphocyte function. Adv Exp Med Biol. 1998;437:269-78. [Article]
  4. Tarizzo VI, Coppes RP, Dahlof C, Zaagsma J: Pre- and postganglionic stimulation-induced noradrenaline overflow is markedly facilitated by a prejunctional beta 2-adrenoceptor-mediated control mechanism in the pithed rat. Naunyn Schmiedebergs Arch Pharmacol. 1994 Jun;349(6):570-7. [Article]
  5. Weinshenker D, Szot P, Miller NS, Palmiter RD: Alpha(1) and beta(2) adrenoreceptor agonists inhibit pentylenetetrazole-induced seizures in mice lacking norepinephrine. J Pharmacol Exp Ther. 2001 Sep;298(3):1042-8. [Article]
  6. Mersmann HJ: Overview of the effects of beta-adrenergic receptor agonists on animal growth including mechanisms of action. J Anim Sci. 1998 Jan;76(1):160-72. [Article]
  7. El-Armouche A, Eschenhagen T: Beta-adrenergic stimulation and myocardial function in the failing heart. Heart Fail Rev. 2009 Dec;14(4):225-41. doi: 10.1007/s10741-008-9132-8. [Article]
  8. Gilsbach R, Hein L: Presynaptic metabotropic receptors for acetylcholine and adrenaline/noradrenaline. Handb Exp Pharmacol. 2008;(184):261-88. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Protein homodimerization activity
Specific Function
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. Beta-3 is involved in the regulation of lipolysis and thermogenesis.
Gene Name
ADRB3
Uniprot ID
P13945
Uniprot Name
Beta-3 adrenergic receptor
Molecular Weight
43518.615 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Carpene C, Galitzky J, Collon P, Esclapez F, Dauzats M, Lafontan M: Desensitization of beta-1 and beta-2, but not beta-3, adrenoceptor-mediated lipolytic responses of adipocytes after long-term norepinephrine infusion. J Pharmacol Exp Ther. 1993 Apr;265(1):237-47. [Article]
  4. Galitzky J, Carpene C, Lafontan M, Berlan M: [Specific stimulation of adipose tissue adrenergic beta 3 receptors by octopamine]. C R Acad Sci III. 1993;316(5):519-23. [Article]
  5. Tamaoki J, Chiyotani A, Sakai N, Konno K: Stimulation of ciliary motility mediated by atypical beta-adrenoceptor in canine bronchial epithelium. Life Sci. 1993;53(20):1509-15. [Article]
  6. Mersmann HJ: Overview of the effects of beta-adrenergic receptor agonists on animal growth including mechanisms of action. J Anim Sci. 1998 Jan;76(1):160-72. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
General Function
Phenylalanine 4-monooxygenase activity
Specific Function
Not Available
Gene Name
PAH
Uniprot ID
P00439
Uniprot Name
Phenylalanine-4-hydroxylase
Molecular Weight
51861.565 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Martinez A, Andersson KK, Haavik J, Flatmark T: EPR and 1H-NMR spectroscopic studies on the paramagnetic iron at the active site of phenylalanine hydroxylase and its interaction with substrates and inhibitors. Eur J Biochem. 1991 Jun 15;198(3):675-82. [Article]
  4. Martinez A, Haavik J, Flatmark T: Cooperative homotropic interaction of L-noradrenaline with the catalytic site of phenylalanine 4-monooxygenase. Eur J Biochem. 1990 Oct 5;193(1):211-9. [Article]
  5. Molinoff PB: The regulation of the noradrenergic neuron. J Psychiatr Res. 1974;11:339-45. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Monoamine transmembrane transporter activity
Specific Function
Involved in the ATP-dependent vesicular transport of biogenic amine neurotransmitters. Pumps cytosolic monoamines including dopamine, norepinephrine, serotonin, and histamine into synaptic vesicles...
Gene Name
SLC18A2
Uniprot ID
Q05940
Uniprot Name
Synaptic vesicular amine transporter
Molecular Weight
55712.075 Da
References
  1. Erickson JD, Schafer MK, Bonner TI, Eiden LE, Weihe E: Distinct pharmacological properties and distribution in neurons and endocrine cells of two isoforms of the human vesicular monoamine transporter. Proc Natl Acad Sci U S A. 1996 May 14;93(10):5166-71. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Serotonin transmembrane transporter activity
Specific Function
Involved in the transport of biogenic monoamines, such as serotonin, from the cytoplasm into the secretory vesicles of neuroendocrine and endocrine cells.
Gene Name
SLC18A1
Uniprot ID
P54219
Uniprot Name
Chromaffin granule amine transporter
Molecular Weight
56256.71 Da
References
  1. Erickson JD, Schafer MK, Bonner TI, Eiden LE, Weihe E: Distinct pharmacological properties and distribution in neurons and endocrine cells of two isoforms of the human vesicular monoamine transporter. Proc Natl Acad Sci U S A. 1996 May 14;93(10):5166-71. [Article]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Norepinephrine:sodium symporter activity
Specific Function
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name
SLC6A2
Uniprot ID
P23975
Uniprot Name
Sodium-dependent noradrenaline transporter
Molecular Weight
69331.42 Da
References
  1. Habecker BA, Willison BD, Shi X, Woodward WR: Chronic depolarization stimulates norepinephrine transporter expression via catecholamines. J Neurochem. 2006 May;97(4):1044-51. Epub 2006 Mar 29. [Article]
  2. Bonisch H, Bruss M: The norepinephrine transporter in physiology and disease. Handb Exp Pharmacol. 2006;(175):485-524. [Article]
  3. Mandela P, Ordway GA: KCl stimulation increases norepinephrine transporter function in PC12 cells. J Neurochem. 2006 Sep;98(5):1521-30. Epub 2006 Jul 31. [Article]
  4. Gutman DA, Owens MJ: Serotonin and norepinephrine transporter binding profile of SSRIs. Essent Psychopharmacol. 2006;7(1):35-41. [Article]
  5. Ksiazek P, Buraczynska K, Buraczynska M: Norepinephrine transporter gene (NET) polymorphism in patients with type 2 diabetes. Kidney Blood Press Res. 2006;29(6):338-43. Epub 2006 Nov 23. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Quaternary ammonium group transmembrane transporter activity
Specific Function
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
Gene Name
SLC22A2
Uniprot ID
O15244
Uniprot Name
Solute carrier family 22 member 2
Molecular Weight
62579.99 Da
References
  1. Urakami Y, Akazawa M, Saito H, Okuda M, Inui K: cDNA cloning, functional characterization, and tissue distribution of an alternatively spliced variant of organic cation transporter hOCT2 predominantly expressed in the human kidney. J Am Soc Nephrol. 2002 Jul;13(7):1703-10. [Article]
  2. Wu X, Kekuda R, Huang W, Fei YJ, Leibach FH, Chen J, Conway SJ, Ganapathy V: Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain. J Biol Chem. 1998 Dec 4;273(49):32776-86. [Article]
  3. Busch AE, Karbach U, Miska D, Gorboulev V, Akhoundova A, Volk C, Arndt P, Ulzheimer JC, Sonders MS, Baumann C, Waldegger S, Lang F, Koepsell H: Human neurons express the polyspecific cation transporter hOCT2, which translocates monoamine neurotransmitters, amantadine, and memantine. Mol Pharmacol. 1998 Aug;54(2):342-52. [Article]
  4. Grundemann D, Koster S, Kiefer N, Breidert T, Engelhardt M, Spitzenberger F, Obermuller N, Schomig E: Transport of monoamine transmitters by the organic cation transporter type 2, OCT2. J Biol Chem. 1998 Nov 20;273(47):30915-20. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Toxin transporter activity
Specific Function
Mediates potential-dependent transport of a variety of organic cations. May play a significant role in the disposition of cationic neurotoxins and neurotransmitters in the brain.
Gene Name
SLC22A3
Uniprot ID
O75751
Uniprot Name
Solute carrier family 22 member 3
Molecular Weight
61279.485 Da
References
  1. Wu X, Kekuda R, Huang W, Fei YJ, Leibach FH, Chen J, Conway SJ, Ganapathy V: Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain. J Biol Chem. 1998 Dec 4;273(49):32776-86. [Article]
  2. Grundemann D, Schechinger B, Rappold GA, Schomig E: Molecular identification of the corticosterone-sensitive extraneuronal catecholamine transporter. Nat Neurosci. 1998 Sep;1(5):349-51. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Symporter activity
Specific Function
Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine. Also transports organic cat...
Gene Name
SLC22A5
Uniprot ID
O76082
Uniprot Name
Solute carrier family 22 member 5
Molecular Weight
62751.08 Da
References
  1. Ohashi R, Tamai I, Nezu Ji J, Nikaido H, Hashimoto N, Oku A, Sai Y, Shimane M, Tsuji A: Molecular and physiological evidence for multifunctionality of carnitine/organic cation transporter OCTN2. Mol Pharmacol. 2001 Feb;59(2):358-66. [Article]
  2. Wu X, Huang W, Prasad PD, Seth P, Rajan DP, Leibach FH, Chen J, Conway SJ, Ganapathy V: Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine transporter. J Pharmacol Exp Ther. 1999 Sep;290(3):1482-92. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Secondary active organic cation transmembrane transporter activity
Specific Function
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
Gene Name
SLC22A1
Uniprot ID
O15245
Uniprot Name
Solute carrier family 22 member 1
Molecular Weight
61153.345 Da
References
  1. Busch AE, Quester S, Ulzheimer JC, Gorboulev V, Akhoundova A, Waldegger S, Lang F, Koepsell H: Monoamine neurotransmitter transport mediated by the polyspecific cation transporter rOCT1. FEBS Lett. 1996 Oct 21;395(2-3):153-6. [Article]
  2. Breidert T, Spitzenberger F, Grundemann D, Schomig E: Catecholamine transport by the organic cation transporter type 1 (OCT1). Br J Pharmacol. 1998 Sep;125(1):218-24. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Ubiquitin protein ligase binding
Specific Function
Transcription factor that binds to the octamer motif (5'-ATTTGCAT-3'). Forms a trimeric complex with SOX2 on DNA and controls the expression of a number of genes involved in embryonic development s...
Gene Name
POU5F1
Uniprot ID
Q01860
Uniprot Name
POU domain, class 5, transcription factor 1
Molecular Weight
38570.415 Da
References
  1. Zhu HJ, Appel DI, Grundemann D, Markowitz JS: Interaction of organic cation transporter 3 (SLC22A3) and amphetamine. J Neurochem. 2010 Jul;114(1):142-9. doi: 10.1111/j.1471-4159.2010.06738.x. Epub 2010 Apr 6. [Article]

Drug created at June 13, 2005 13:24 / Updated at March 18, 2024 16:48