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Identification
- Summary
Dopamine is a catecholamine neurotransmitter used to treat hemodynamic imbalances, poor perfusion of vital organs, low cardiac output, and hypotension.
- Generic Name
- Dopamine
- DrugBank Accession Number
- DB00988
- Background
One of the catecholamine neurotransmitters in the brain. It is derived from tyrosine and is the precursor to norepinephrine and epinephrine. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (receptors, dopamine) mediate its action.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Dopamine (DB00988)
- Weight
- Average: 153.1784
Monoisotopic: 153.078978601 - Chemical Formula
- C8H11NO2
- Synonyms
- 2-(3,4-dihydroxyphenyl)ethylamine
- 3-Hydroxytyramine
- 3,4-Dihydroxyphenethylamine
- 4-(2-aminoethyl)-1,2-benzenediol
- 4-(2-Aminoethyl)benzene-1,2-diol
- 4-(2-aminoethyl)catechol
- 4-(2-aminoethyl)pyrocatechol
- Dopamina
- Dopamine
- Dopaminum
- Oxytyramine
- External IDs
- NSC-173182
Pharmacology
- Indication
For the correction of hemodynamic imbalances present in the shock syndrome due to myocardial infarction, trauma, endotoxic septicemia, open-heart surgery, renal failure, and chronic cardiac decompensation as in congestive failure
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
- Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Dopamine is a natural catecholamine formed by the decarboxylation of 3,4-dihydroxyphenylalanine (DOPA). It is a precursor to norepinephrine in noradrenergic nerves and is also a neurotransmitter in certain areas of the central nervous system, especially in the nigrostriatal tract, and in a few peripheral sympathetic nerves. Dopamine produces positive chronotropic and inotropic effects on the myocardium, resulting in increased heart rate and cardiac contractility. This is accomplished directly by exerting an agonist action on beta-adrenoceptors and indirectly by causing release of norepinephrine from storage sites in sympathetic nerve endings.
- Mechanism of action
Dopamine is a precursor to norepinephrine in noradrenergic nerves and is also a neurotransmitter in certain areas of the central nervous system. Dopamine produces positive chronotropic and inotropic effects on the myocardium, resulting in increased heart rate and cardiac contractility. This is accomplished directly by exerting an agonist action on beta-adrenoceptors and indirectly by causing release of norepinephrine from storage sites in sympathetic nerve endings. In the brain, dopamine acts as an agonist to the five dopamine receptor subtypes (D1, D2, D3, D4, D5).
Target Actions Organism AD(2) dopamine receptor agonistHumans AD(1A) dopamine receptor agonistHumans AD(1B) dopamine receptor agonistHumans AD(3) dopamine receptor agonistHumans AD(4) dopamine receptor agonistHumans ASodium-dependent dopamine transporter inducerHumans ADopamine beta-hydroxylase ligandHumans U5-hydroxytryptamine receptor 1A binderHumans U5-hydroxytryptamine receptor 7 binderHumans UD(1) dopamine receptor agonistHumans USodium-dependent noradrenaline transporter inhibitorHumans USodium-dependent serotonin transporter inhibitorHumans U5-hydroxytryptamine receptor 3A Not Available Humans U5-hydroxytryptamine receptor 3B Not Available Humans USuperoxide dismutase [Cu-Zn] Not Available Humans USynaptic vesicular amine transporter Not Available Humans - Absorption
Dopamine is rapidly absorbed from the small intestine.
- Volume of distribution
Not Available
- Protein binding
No information currently available on protein binding.
- Metabolism
Biotransformation of dopamine proceeds rapidly to yield the principal excretion products, 3-4-dihydroxy-phenylacetic acid (DOPAC) and 3-methoxy-4-hydroxy-phenylacetic acid (homovanillic acid, HVA).
Hover over products below to view reaction partners
- Route of elimination
It has been reported that about 80% of the drug is excreted in the urine within 24 hours, primarily as HVA and its sulfate and glucuronide conjugates and as 3,4-dihydroxyphenylacetic acid. A very small portion is excreted unchanged.
- Half-life
2 minutes
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
LD50 oral mice = 1460 mg/kg, LD50 oral rats = 1780 mg/kg. Spasm or closing of eyelids, nausea, vomiting, cardiac arrhythmias, involuntary movements of the body including the face, tongue, arms, hand, head, and upper body; hypotension, haemolytic anaemia, urinary retention, duodenal ulcer, sialorrhea, ataxia, abdominal pain, dry mouth, nightmares, tachypnoea, bruxism, confusion, and insomnia.
- Pathways
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Dopamine may decrease the excretion rate of Abacavir which could result in a higher serum level. Acebutolol Dopamine may decrease the antihypertensive activities of Acebutolol. Aceclofenac The risk or severity of hypertension can be increased when Dopamine is combined with Aceclofenac. Acemetacin The risk or severity of hypertension can be increased when Dopamine is combined with Acemetacin. Acetaminophen Acetaminophen may decrease the excretion rate of Dopamine which could result in a higher serum level. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Dopamine hydrochloride 7L3E358N9L 62-31-7 CTENFNNZBMHDDG-UHFFFAOYSA-N - International/Other Brands
- Intropin / Revimine
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Dopamine Hci Injection, solution, concentrate 40 mg/1mL Intravenous HF Acquisition Co LLC, DBA HealthFirst 2018-09-19 Not applicable US 
Dopamine Hci Injection, solution, concentrate 40 mg/1mL Intravenous Hf Acquisition Co. Llc, Dba Health First 2018-08-23 Not applicable US Dopamine Hci In 5% Dextrose Injection, solution 1.6 mg/1mL Intravenous HF Acquisition Co LLC, DBA HealthFirst 2019-12-12 Not applicable US Dopamine HCl Inj 4% Liquid 40 mg / mL Intravenous International Medication Systems, Limited 1980-12-31 1997-08-15 Canada 
DOPamine Hydrochloride Injection, solution, concentrate 40 mg/1mL Intravenous Cardinal Health 1981-05-19 2018-06-30 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Dopamine Injection, solution 80 mg/1mL Intravenous General Injectables & Vaccines 2010-04-01 2014-09-01 US Dopamine HCl Injection, solution 80 mg/1mL Intravenous AMERICAN REGENT, INC. 1990-09-30 2014-03-03 US Dopamine HCl Injection, solution 80 mg/1mL Intravenous Cardinal Health 1990-09-30 2014-09-30 US Dopamine HCl Injection, solution 80 mg/1mL Intravenous Physicians Total Care, Inc. 1990-09-30 2007-06-30 US Dopamine HCl Injection, solution 40 mg/1mL Intravenous AMERICAN REGENT, INC. 1990-09-30 2013-12-19 US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Dopamine HCl 0.8mg/ml Dextrose 5% Inj USP Dopamine hydrochloride (.8 mg / mL) + Dextrose, unspecified form (50 mg / mL) Solution Intravenous Baxter Laboratories 1992-12-31 Not applicable Canada Dopamine HCl 1.6mg/ml Dextrose 5% Inj USP Dopamine hydrochloride (1.6 mg / mL) + Dextrose, unspecified form (50 mg / mL) Solution Intravenous Baxter Laboratories 1990-12-31 Not applicable Canada Dopamine HCl 3.2mg/ml Dextrose 5% Inj USP Dopamine hydrochloride (3.2 mg / mL) + Dextrose, unspecified form (50 mg / mL) Solution Intravenous Baxter Laboratories 1990-12-31 Not applicable Canada Dopamine Hydrochloride and 5% Dextrose Injection USP Dopamine hydrochloride (1.6 mg / mL) + Dextrose, unspecified form (50 mg / mL) Solution Intravenous Hospira Healthcare Ulc 1986-12-31 2018-11-30 Canada Dopamine Hydrochloride and 5% Dextrose Injection USP Dopamine hydrochloride (3.2 mg / mL) + Dextrose, unspecified form (50 mg / mL) Solution Intravenous Hospira Healthcare Ulc 1991-12-31 2018-11-30 Canada - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image DOPAMIN FRESENIUS 10 AMPUL Dopamine hydrochloride (200 mg/5ml) Solution FRESENİUS KABİ İLAÇ SAN. VE TİC. LTD. ŞTİ. 2020-07-21 2022-11-10 Turkey 
DOPAMINE DBL 200 MG/5ML IV INF.ICIN SOL.ICEREN AMPUL Dopamine hydrochloride (200 mg/5ml) Solution Intravenous ORNA İLAÇ TEKSTİL KİMYEVİ MAD. SAN. VE DIŞ TİC. LTD. ŞTİ. 2018-02-20 2021-11-05 Turkey
Categories
- ATC Codes
- C01CA04 — Dopamine
- Drug Categories
- Adrenergic and Dopaminergic Agents
- Agents producing tachycardia
- Agents that produce hypertension
- Amines
- Autonomic Agents
- Benzene Derivatives
- Biogenic Amines
- Biogenic Monoamines
- Cardiac Stimulants Excl. Cardiac Glycosides
- Cardiac Therapy
- Cardiotonic Agents
- Cardiovascular Agents
- Catecholamines
- Catechols
- Compounds used in a research, industrial, or household setting
- COMT Substrates
- Dopamine Agents
- Dopamine, metabolism
- Drugs that are Mainly Renally Excreted
- Monoamine Oxidase A Substrates
- Neurotransmitter Agents
- OCT1 substrates
- OCT2 Inhibitors
- OCT2 Substrates
- Peripheral Nervous System Agents
- Phenols
- Protective Agents
- Selective Beta 1-adrenergic Agonists
- Sympathomimetics
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as catecholamines and derivatives. These are compounds containing 4-(2-Aminoethyl)pyrocatechol [4-(2-aminoethyl)benzene-1,2-diol] or a derivative thereof formed by substitution.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Phenols
- Sub Class
- Benzenediols
- Direct Parent
- Catecholamines and derivatives
- Alternative Parents
- Phenethylamines / 2-arylethylamines / Aralkylamines / 1-hydroxy-4-unsubstituted benzenoids / 1-hydroxy-2-unsubstituted benzenoids / Organopnictogen compounds / Organooxygen compounds / Monoalkylamines / Hydrocarbon derivatives
- Substituents
- 1-hydroxy-2-unsubstituted benzenoid / 1-hydroxy-4-unsubstituted benzenoid / 2-arylethylamine / Amine / Aralkylamine / Aromatic homomonocyclic compound / Catecholamine / Hydrocarbon derivative / Monocyclic benzene moiety / Organic nitrogen compound
- Molecular Framework
- Aromatic homomonocyclic compounds
- External Descriptors
- catecholamine (CHEBI:18243) / Biogenic amines, Tyramine derivatives, Dopamine (C03758)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- VTD58H1Z2X
- CAS number
- 51-61-6
- InChI Key
- VYFYYTLLBUKUHU-UHFFFAOYSA-N
- InChI
- InChI=1S/C8H11NO2/c9-4-3-6-1-2-7(10)8(11)5-6/h1-2,5,10-11H,3-4,9H2
- IUPAC Name
- 4-(2-aminoethyl)benzene-1,2-diol
- SMILES
- NCCC1=CC(O)=C(O)C=C1
References
- Synthesis Reference
Klaus Schoellkopf, Rudolf Albrecht, Manfred Lehmann, Gertrud Schroeder, "Novel dopamine derivatives, processes for their preparation, and their use as medicinal agents." U.S. Patent US4958026, issued February, 1972.
US4958026- General References
- Barron AB, Maleszka R, Vander Meer RK, Robinson GE: Octopamine modulates honey bee dance behavior. Proc Natl Acad Sci U S A. 2007 Jan 30;104(5):1703-7. Epub 2007 Jan 19. [Article]
- Giuliano F, Allard J: Dopamine and male sexual function. Eur Urol. 2001 Dec;40(6):601-8. [Article]
- Giuliano F, Allard J: Dopamine and sexual function. Int J Impot Res. 2001 Aug;13 Suppl 3:S18-28. [Article]
- Berridge KC, Robinson TE: What is the role of dopamine in reward: hedonic impact, reward learning, or incentive salience? Brain Res Brain Res Rev. 1998 Dec;28(3):309-69. [Article]
- Pecina S, Cagniard B, Berridge KC, Aldridge JW, Zhuang X: Hyperdopaminergic mutant mice have higher "wanting" but not "liking" for sweet rewards. J Neurosci. 2003 Oct 15;23(28):9395-402. [Article]
- External Links
- Human Metabolome Database
- HMDB0000073
- KEGG Drug
- D07870
- KEGG Compound
- C03758
- PubChem Compound
- 681
- PubChem Substance
- 46506043
- ChemSpider
- 661
- BindingDB
- 55121
- 3628
- ChEBI
- 18243
- ChEMBL
- CHEMBL59
- ZINC
- ZINC000000033882
- Therapeutic Targets Database
- DAP000212
- PharmGKB
- PA449396
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- LDP
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Dopamine
- PDB Entries
- 2a3r / 2qmz / 2vq5 / 4a7v / 4dtz / 4du2 / 4dub / 4xp1 / 5log / 5pah … show 20 more
- MSDS
- Download (72.1 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Active Not Recruiting Not Available Autonomic Failure / Multiple System Atrophy (MSA) / Parkinson's Disease (PD) 1 somestatus stop reason just information to hide Not Available Active Not Recruiting Not Available Myocardial Dysfunction / Newborn Morbidity / Obesity, Maternal 1 somestatus stop reason just information to hide Not Available Active Not Recruiting Treatment Parkinson's Disease (PD) 1 somestatus stop reason just information to hide Not Available Completed Not Available Lung Transplant; Complications 1 somestatus stop reason just information to hide Not Available Completed Not Available Neurodegenerative Disorders 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Abbott laboratories hosp products div
- Abraxis pharmaceutical products
- Astrazeneca lp
- Baxter healthcare corp anesthesia and critical care
- Hospira inc
- International medication system
- Luitpold pharmaceuticals inc
- Smith and nephew solopak div smith and nephew
- Teva parenteral medicines inc
- Warner chilcott div warner lambert co
- B braun medical inc
- Baxter healthcare corp
- Packagers
- American Regent
- B. Braun Melsungen AG
- Baxter International Inc.
- Bristol-Myers Squibb Co.
- Cardinal Health
- General Injectables and Vaccines Inc.
- Hospira Inc.
- Luitpold Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Dosage Forms
Form Route Strength Injection, solution Intravenous 200 mg/5ml Injection Intravenous Injection, solution, concentrate Intravenous 200 mg/5ml Solution Solution 200 mg/5ml Injection, solution, concentrate Intravenous 40 mg/ml Solution Intravenous 200 mg Solution Intravenous 40 mg Injection, solution Intravenous Injection, solution, concentrate Intravenous; Parenteral 40 MG/ML Injection, solution, concentrate Intravenous; Parenteral 200 MG/5ML Solution Intravenous 200 mg/5ml Injection, solution Intravenous 160 mg/1mL Injection, solution Intravenous 80 mg/1mL Solution Intravenous Liquid Intravenous 40 mg / mL Injection Intravenous 40 mg/1mL Injection Intravenous 40 mg/5ml Injection Intravenous 80 mg/1mL Injection, solution Intravenous 40 mg/1mL Injection, solution Intravenous 40 mg Injection, solution, concentrate Intravenous 40 mg/1mL Injection, solution, concentrate Intravenous 80 mg/1mL Injection, solution Intravenous 160 mg/100mL Injection, solution Intravenous 320 mg/100mL Injection, solution Intravenous 80 mg/100mL Injection, solution Intravenous Injection, solution Intravenous 0.8 mg/1mL Injection, solution Intravenous 1.6 mg/1mL Injection, solution Intravenous 3.2 mg/1mL Solution 40 MG/ML Solution Parenteral 200 mg Solution Parenteral 10 mg/ml Solution Parenteral 250 mg Injection Intravenous 40 mg Solution Intravenous 200.000 mg Solution Intravenous 40 mg / mL Injection Parenteral Injection Intravenous 40 mg/ml Solution Parenteral 200.000 MG Injection, solution Intravenous 800 mcg/ml Injection Intravenous Injection, solution Intravenous 1.5 mg/ml Injection, solution Intravenous 4.5 mg/ml Injection, solution, concentrate 10 mg/mL Solution Intravenous 50 mg/5ml Injection Intravenous 20 MG/ML Injection, solution, concentrate Intravenous Injection Intravenous 200 mg/5ml Solution 10 mg/1ml Solution 20 mg/1ml Solution 25 mg/1ml Solution 50 mg/1ml - Prices
Unit description Cost Unit Dopamine 40 mg/ml vial 0.15USD ml Dopamine 800 mg-d5w 500 ml 0.05USD ml Dopamine 400 mg-d5w 250 ml 0.04USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 128 °C PhysProp boiling point (°C) 227 °C at 2.30E+01 mm Hg PhysProp water solubility 600 g/L Not Available logP -0.98 HANSCH,C ET AL. (1995) Caco2 permeability -5.03 ADME Research, USCD pKa 8.93 PERRIN,DD (1965) - Predicted Properties
Property Value Source Water Solubility 7.43 mg/mL ALOGPS logP -0.4 ALOGPS logP 0.03 Chemaxon logS -1.3 ALOGPS pKa (Strongest Acidic) 10.01 Chemaxon pKa (Strongest Basic) 9.27 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 66.48 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 43.25 m3·mol-1 Chemaxon Polarizability 16.21 Å3 Chemaxon Number of Rings 1 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9547 Blood Brain Barrier - 0.8414 Caco-2 permeable - 0.5479 P-glycoprotein substrate Non-substrate 0.5431 P-glycoprotein inhibitor I Non-inhibitor 0.9739 P-glycoprotein inhibitor II Non-inhibitor 0.9357 Renal organic cation transporter Non-inhibitor 0.7115 CYP450 2C9 substrate Non-substrate 0.8462 CYP450 2D6 substrate Non-substrate 0.6383 CYP450 3A4 substrate Non-substrate 0.6905 CYP450 1A2 substrate Non-inhibitor 0.9046 CYP450 2C9 inhibitor Non-inhibitor 0.9459 CYP450 2D6 inhibitor Non-inhibitor 0.9422 CYP450 2C19 inhibitor Non-inhibitor 0.9477 CYP450 3A4 inhibitor Non-inhibitor 0.9001 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8648 Ames test AMES toxic 0.9107 Carcinogenicity Non-carcinogens 0.8642 Biodegradation Ready biodegradable 0.7449 Rat acute toxicity 2.1415 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.7712 hERG inhibition (predictor II) Non-inhibitor 0.5715
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 135.8965042 predictedDarkChem Lite v0.1.0 [M-H]- 134.6696571 predictedDarkChem Standard v0.1.0 [M-H]- 135.7188042 predictedDarkChem Lite v0.1.0 [M-H]- 135.6712042 predictedDarkChem Lite v0.1.0 [M-H]- 130.9612 predictedDeepCCS 1.0 (2019) [M+H]+ 136.2634042 predictedDarkChem Lite v0.1.0 [M+H]+ 136.4476042 predictedDarkChem Lite v0.1.0 [M+H]+ 136.0352042 predictedDarkChem Lite v0.1.0 [M+H]+ 136.5997042 predictedDarkChem Lite v0.1.0 [M+H]+ 134.75922 predictedDeepCCS 1.0 (2019) [M+Na]+ 135.8105042 predictedDarkChem Lite v0.1.0 [M+Na]+ 135.8023042 predictedDarkChem Lite v0.1.0 [M+Na]+ 135.9300042 predictedDarkChem Lite v0.1.0 [M+Na]+ 135.7405042 predictedDarkChem Lite v0.1.0 [M+Na]+ 144.22823 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase (PubMed:21645528). Positively regulates postnatal regression of retinal hyaloid vessels via suppression of VEGFR2/KDR activity, downstream of OPN5 (By similarity)
- Specific Function
- Dopamine binding
- Gene Name
- DRD2
- Uniprot ID
- P14416
- Uniprot Name
- D(2) dopamine receptor
- Molecular Weight
- 50618.91 Da
References
- Ostadali MR, Ahangari G, Eslami MB, Razavi A, Zarrindast MR, Ahmadkhaniha HR, Boulhari J: The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase
- Specific Function
- Arrestin family protein binding
- Gene Name
- DRD1
- Uniprot ID
- P21728
- Uniprot Name
- D(1A) dopamine receptor
- Molecular Weight
- 49292.765 Da
References
- Ostadali MR, Ahangari G, Eslami MB, Razavi A, Zarrindast MR, Ahmadkhaniha HR, Boulhari J: The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74. [Article]
- Dolzan V, Plesnicar BK, Serretti A, Mandelli L, Zalar B, Koprivsek J, Breskvar K: Polymorphisms in dopamine receptor DRD1 and DRD2 genes and psychopathological and extrapyramidal symptoms in patients on long-term antipsychotic treatment. Am J Med Genet B Neuropsychiatr Genet. 2007 Sep 5;144B(6):809-15. [Article]
- Hoenicka J, Aragues M, Ponce G, Rodriguez-Jimenez R, Jimenez-Arriero MA, Palomo T: From dopaminergic genes to psychiatric disorders. Neurotox Res. 2007 Jan;11(1):61-72. [Article]
- da Silva Lobo DS, Vallada HP, Knight J, Martins SS, Tavares H, Gentil V, Kennedy JL: Dopamine genes and pathological gambling in discordant sib-pairs. J Gambl Stud. 2007 Dec;23(4):421-33. Epub 2007 Mar 30. [Article]
- Fu W, Shen J, Luo X, Zhu W, Cheng J, Yu K, Briggs JM, Jin G, Chen K, Jiang H: Dopamine D1 receptor agonist and D2 receptor antagonist effects of the natural product (-)-stepholidine: molecular modeling and dynamics simulations. Biophys J. 2007 Sep 1;93(5):1431-41. Epub 2007 Apr 27. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase
- Specific Function
- Dopamine binding
- Gene Name
- DRD5
- Uniprot ID
- P21918
- Uniprot Name
- D(1B) dopamine receptor
- Molecular Weight
- 52950.5 Da
References
- Ostadali MR, Ahangari G, Eslami MB, Razavi A, Zarrindast MR, Ahmadkhaniha HR, Boulhari J: The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation
- Specific Function
- Dopamine neurotransmitter receptor activity, coupled via gi/go
- Gene Name
- DRD3
- Uniprot ID
- P35462
- Uniprot Name
- D(3) dopamine receptor
- Molecular Weight
- 44194.315 Da
References
- Ostadali MR, Ahangari G, Eslami MB, Razavi A, Zarrindast MR, Ahmadkhaniha HR, Boulhari J: The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General 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. Activated by dopamine, but also by epinephrine and norepinephrine, and by numerous synthetic agonists and drugs (PubMed:16423344, PubMed:27659709, PubMed:29051383, PubMed:9003072). Agonist binding triggers signaling via G proteins that inhibit adenylyl cyclase (PubMed:16423344, PubMed:27659709, PubMed:29051383, PubMed:7512953, PubMed:7643093). Modulates the circadian rhythm of contrast sensitivity by regulating the rhythmic expression of NPAS2 in the retinal ganglion cells (By similarity)
- Specific Function
- Dopamine binding
- Gene Name
- DRD4
- Uniprot ID
- P21917
- Uniprot Name
- D(4) dopamine receptor
- Molecular Weight
- 43900.84 Da
References
- Ostadali MR, Ahangari G, Eslami MB, Razavi A, Zarrindast MR, Ahmadkhaniha HR, Boulhari J: The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inducer
- General Function
- Mediates sodium- and chloride-dependent transport of dopamine (PubMed:10375632, PubMed:11093780, PubMed:1406597, PubMed:15505207, PubMed:19478460, PubMed:8302271). Also mediates sodium- and chloride-dependent transport of norepinephrine (also known as noradrenaline) (By similarity). Regulator of light-dependent retinal hyaloid vessel regression, downstream of OPN5 signaling (By similarity)
- Specific Function
- Amine binding
- Gene Name
- SLC6A3
- Uniprot ID
- Q01959
- Uniprot Name
- Sodium-dependent dopamine transporter
- Molecular Weight
- 68494.255 Da
References
- Ostadali MR, Ahangari G, Eslami MB, Razavi A, Zarrindast MR, Ahmadkhaniha HR, Boulhari J: The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Ligand
- General Function
- Catalyzes the hydroxylation of dopamine to noradrenaline (also known as norepinephrine), and is thus vital for regulation of these neurotransmitters
- Specific Function
- Catalytic activity
- Gene Name
- DBH
- Uniprot ID
- P09172
- Uniprot Name
- Dopamine beta-hydroxylase
- Molecular Weight
- 69064.45 Da
References
- Goldman JM, Cooper RL, Murr AS: Reproductive functions and hypothalamic catecholamines in response to the soil fumigant metam sodium: adaptations to extended exposures. Neurotoxicol Teratol. 2007 May-Jun;29(3):368-76. Epub 2006 Dec 6. [Article]
- Arboleda G, Huang TJ, Waters C, Verkhratsky A, Fernyhough P, Gibson RM: Insulin-like growth factor-1-dependent maintenance of neuronal metabolism through the phosphatidylinositol 3-kinase-Akt pathway is inhibited by C2-ceramide in CAD cells. Eur J Neurosci. 2007 May;25(10):3030-8. [Article]
- Garland EM, Black BK, Harris PA, Robertson D: Dopamine-beta-hydroxylase in postural tachycardia syndrome. Am J Physiol Heart Circ Physiol. 2007 Jul;293(1):H684-90. [Article]
- Pyatskowit JW, Prohaska JR: Rodent brain and heart catecholamine levels are altered by different models of copper deficiency. Comp Biochem Physiol C Toxicol Pharmacol. 2007 Mar;145(2):275-81. Epub 2007 Jan 12. [Article]
- LeBlanc J, Ducharme MB: Plasma dopamine and noradrenaline variations in response to stress. Physiol Behav. 2007 Jun 8;91(2-3):208-11. Epub 2007 Mar 2. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General 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 signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca(2+) ions from intracellular stores. Plays a role in the regulation of 5-hydroxytryptamine release and in the regulation of dopamine and 5-hydroxytryptamine metabolism. Plays a role in the regulation of dopamine and 5-hydroxytryptamine levels in the brain, and thereby affects neural activity, mood and behavior. Plays a role in the response to anxiogenic stimuli
- Specific Function
- G protein-coupled serotonin receptor activity
- Gene Name
- HTR1A
- Uniprot ID
- P08908
- Uniprot Name
- 5-hydroxytryptamine receptor 1A
- Molecular Weight
- 46106.335 Da
References
- Weber JT, Hayataka K, O'Connor MF, Parker KK: Rabbit cerebral cortex 5HT1a receptors. Comp Biochem Physiol C Pharmacol Toxicol Endocrinol. 1997 May;117(1):19-24. [Article]
- Toll L, Berzetei-Gurske IP, Polgar WE, Brandt SR, Adapa ID, Rodriguez L, Schwartz RW, Haggart D, O'Brien A, White A, Kennedy JM, Craymer K, Farrington L, Auh JS: Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications. NIDA Res Monogr. 1998 Mar;178:440-66. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General 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 is mediated by G proteins that stimulate adenylate cyclase
- Specific Function
- G protein-coupled serotonin receptor activity
- Gene Name
- HTR7
- Uniprot ID
- P34969
- Uniprot Name
- 5-hydroxytryptamine receptor 7
- Molecular Weight
- 53554.43 Da
References
- Lovenberg TW, Baron BM, de Lecea L, Miller JD, Prosser RA, Rea MA, Foye PE, Racke M, Slone AL, Siegel BW, et al.: A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms. Neuron. 1993 Sep;11(3):449-58. [Article]
- Shen Y, Monsma FJ Jr, Metcalf MA, Jose PA, Hamblin MW, Sibley DR: Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype. J Biol Chem. 1993 Aug 25;268(24):18200-4. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase
- Specific Function
- Arrestin family protein binding
Components:
References
- Hubner H, Haubmann C, Utz W, Gmeiner P: Conjugated enynes as nonaromatic catechol bioisosteres: synthesis, binding experiments, and computational studies of novel dopamine receptor agonists recognizing preferentially the D(3) subtype. J Med Chem. 2000 Feb 24;43(4):756-62. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Mediates sodium- and chloride-dependent transport of norepinephrine (also known as noradrenaline) (PubMed:2008212, PubMed:8125921). Can also mediate sodium- and chloride-dependent transport of dopamine (PubMed:11093780, PubMed:8125921)
- Specific Function
- Actin binding
- Gene Name
- SLC6A2
- Uniprot ID
- P23975
- Uniprot Name
- Sodium-dependent noradrenaline transporter
- Molecular Weight
- 69331.42 Da
References
- Rothman RB, Baumann MH, Dersch CM, Romero DV, Rice KC, Carroll FI, Partilla JS: Amphetamine-type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin. Synapse. 2001 Jan;39(1):32-41. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Serotonin transporter that cotransports serotonin with one Na(+) ion in exchange for one K(+) ion and possibly one proton in an overall electroneutral transport cycle. Transports serotonin across the plasma membrane from the extracellular compartment to the cytosol thus limiting serotonin intercellular signaling (PubMed:10407194, PubMed:12869649, PubMed:21730057, PubMed:27049939, PubMed:27756841, PubMed:34851672). Essential for serotonin homeostasis in the central nervous system. In the developing somatosensory cortex, acts in glutamatergic neurons to control serotonin uptake and its trophic functions accounting for proper spatial organization of cortical neurons and elaboration of sensory circuits. In the mature cortex, acts primarily in brainstem raphe neurons to mediate serotonin uptake from the synaptic cleft back into the pre-synaptic terminal thus terminating serotonin signaling at the synapse (By similarity). Modulates mucosal serotonin levels in the gastrointestinal tract through uptake and clearance of serotonin in enterocytes. Required for enteric neurogenesis and gastrointestinal reflexes (By similarity). Regulates blood serotonin levels by ensuring rapid high affinity uptake of serotonin from plasma to platelets, where it is further stored in dense granules via vesicular monoamine transporters and then released upon stimulation (PubMed:17506858, PubMed:18317590). Mechanistically, the transport cycle starts with an outward-open conformation having Na1(+) and Cl(-) sites occupied. The binding of a second extracellular Na2(+) ion and serotonin substrate leads to structural changes to outward-occluded to inward-occluded to inward-open, where the Na2(+) ion and serotonin are released into the cytosol. Binding of intracellular K(+) ion induces conformational transitions to inward-occluded to outward-open and completes the cycle by releasing K(+) possibly together with a proton bound to Asp-98 into the extracellular compartment. Na1(+) and Cl(-) ions remain bound throughout the transport cycle (PubMed:10407194, PubMed:12869649, PubMed:21730057, PubMed:27049939, PubMed:27756841, PubMed:34851672). Additionally, displays serotonin-induced channel-like conductance for monovalent cations, mainly Na(+) ions. The channel activity is uncoupled from the transport cycle and may contribute to the membrane resting potential or excitability (By similarity)
- Specific Function
- Actin filament binding
- Gene Name
- SLC6A4
- Uniprot ID
- P31645
- Uniprot Name
- Sodium-dependent serotonin transporter
- Molecular Weight
- 70324.165 Da
References
- Rothman RB, Baumann MH, Dersch CM, Romero DV, Rice KC, Carroll FI, Partilla JS: Amphetamine-type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin. Synapse. 2001 Jan;39(1):32-41. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Forms serotonin (5-hydroxytryptamine/5-HT3)-activated cation-selective channel complexes, which when activated cause fast, depolarizing responses in neurons
- Specific Function
- Excitatory extracellular ligand-gated monoatomic ion channel activity
- Gene Name
- HTR3A
- Uniprot ID
- P46098
- Uniprot Name
- 5-hydroxytryptamine receptor 3A
- Molecular Weight
- 55279.835 Da
References
- Rusch D, Musset B, Wulf H, Schuster A, Raines DE: Subunit-dependent modulation of the 5-hydroxytryptamine type 3 receptor open-close equilibrium by n-alcohols. J Pharmacol Exp Ther. 2007 Jun;321(3):1069-74. Epub 2007 Mar 7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Forms serotonin (5-hydroxytryptamine/5-HT3)-activated cation-selective channel complexes, which when activated cause fast, depolarizing responses in neurons
- Specific Function
- Excitatory extracellular ligand-gated monoatomic ion channel activity
- Gene Name
- HTR3B
- Uniprot ID
- O95264
- Uniprot Name
- 5-hydroxytryptamine receptor 3B
- Molecular Weight
- 50291.3 Da
References
- Rusch D, Musset B, Wulf H, Schuster A, Raines DE: Subunit-dependent modulation of the 5-hydroxytryptamine type 3 receptor open-close equilibrium by n-alcohols. J Pharmacol Exp Ther. 2007 Jun;321(3):1069-74. Epub 2007 Mar 7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Destroys radicals which are normally produced within the cells and which are toxic to biological systems
- Specific Function
- Copper ion binding
- Gene Name
- SOD1
- Uniprot ID
- P00441
- Uniprot Name
- Superoxide dismutase [Cu-Zn]
- Molecular Weight
- 15935.685 Da
References
- Wright GS, Antonyuk SV, Kershaw NM, Strange RW, Samar Hasnain S: Ligand binding and aggregation of pathogenic SOD1. Nat Commun. 2013;4:1758. doi: 10.1038/ncomms2750. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Electrogenic antiporter that exchanges one cationic monoamine with two intravesicular protons across the membrane of secretory and synaptic vesicles. Uses the electrochemical proton gradient established by the V-type proton-pump ATPase to accumulate high concentrations of monoamines inside the vesicles prior to their release via exocytosis. Transports a variety of catecholamines such as dopamine, adrenaline and noradrenaline, histamine, and indolamines such as serotonin (PubMed:23363473, PubMed:8643547). Regulates the transvesicular monoaminergic gradient that determines the quantal size. Mediates somatodendritic dopamine release in hippocampal neurons, likely as part of a regulated secretory pathway that integrates retrograde synaptic signals (By similarity). Acts as a primary transporter for striatal dopamine loading ensuring impulse-dependent release of dopamine at the synaptic cleft (By similarity). Responsible for histamine and serotonin storage and subsequent corelease from mast cell granules (By similarity) (PubMed:8860238)
- Specific Function
- Monoamine transmembrane transporter activity
- Gene Name
- SLC18A2
- Uniprot ID
- Q05940
- Uniprot Name
- Synaptic vesicular amine transporter
- Molecular Weight
- 55712.075 Da
References
- Gonzalez AM, Walther D, Pazos A, Uhl GR: Synaptic vesicular monoamine transporter expression: distribution and pharmacologic profile. Brain Res Mol Brain Res. 1994 Mar;22(1-4):219-26. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Catalyzes the hydroxylation of dopamine to noradrenaline (also known as norepinephrine), and is thus vital for regulation of these neurotransmitters
- Specific Function
- Catalytic activity
- Gene Name
- DBH
- Uniprot ID
- P09172
- Uniprot Name
- Dopamine beta-hydroxylase
- Molecular Weight
- 69064.45 Da
References
- Goldman JM, Cooper RL, Murr AS: Reproductive functions and hypothalamic catecholamines in response to the soil fumigant metam sodium: adaptations to extended exposures. Neurotoxicol Teratol. 2007 May-Jun;29(3):368-76. Epub 2006 Dec 6. [Article]
- Arboleda G, Huang TJ, Waters C, Verkhratsky A, Fernyhough P, Gibson RM: Insulin-like growth factor-1-dependent maintenance of neuronal metabolism through the phosphatidylinositol 3-kinase-Akt pathway is inhibited by C2-ceramide in CAD cells. Eur J Neurosci. 2007 May;25(10):3030-8. [Article]
- Garland EM, Black BK, Harris PA, Robertson D: Dopamine-beta-hydroxylase in postural tachycardia syndrome. Am J Physiol Heart Circ Physiol. 2007 Jul;293(1):H684-90. [Article]
- Pyatskowit JW, Prohaska JR: Rodent brain and heart catecholamine levels are altered by different models of copper deficiency. Comp Biochem Physiol C Toxicol Pharmacol. 2007 Mar;145(2):275-81. Epub 2007 Jan 12. [Article]
- LeBlanc J, Ducharme MB: Plasma dopamine and noradrenaline variations in response to stress. Physiol Behav. 2007 Jun 8;91(2-3):208-11. Epub 2007 Mar 2. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Catalyzes the oxidative deamination of primary and some secondary amine such as neurotransmitters, with concomitant reduction of oxygen to hydrogen peroxide and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues (PubMed:18391214, PubMed:20493079, PubMed:24169519, PubMed:8316221). Preferentially oxidizes serotonin (PubMed:20493079, PubMed:24169519). Also catalyzes the oxidative deamination of kynuramine to 3-(2-aminophenyl)-3-oxopropanal that can spontaneously condense to 4-hydroxyquinoline (By similarity)
- Specific Function
- Aliphatic amine oxidase activity
- Gene Name
- MAOA
- Uniprot ID
- P21397
- Uniprot Name
- Amine oxidase [flavin-containing] A
- Molecular Weight
- 59681.27 Da
References
- Bortolato M, Chen K, Shih JC: Monoamine oxidase inactivation: from pathophysiology to therapeutics. Adv Drug Deliv Rev. 2008 Oct-Nov;60(13-14):1527-33. doi: 10.1016/j.addr.2008.06.002. Epub 2008 Jul 4. [Article]
- Kaludercic N, Carpi A, Menabo R, Di Lisa F, Paolocci N: Monoamine oxidases (MAO) in the pathogenesis of heart failure and ischemia/reperfusion injury. Biochim Biophys Acta. 2011 Jul;1813(7):1323-32. doi: 10.1016/j.bbamcr.2010.09.010. Epub 2010 Sep 24. [Article]
- Volavka J, Bilder R, Nolan K: Catecholamines and aggression: the role of COMT and MAO polymorphisms. Ann N Y Acad Sci. 2004 Dec;1036:393-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Catalyzes the oxidative deamination of primary and some secondary amines such as neurotransmitters, and exogenous amines including the tertiary amine, neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), with concomitant reduction of oxygen to hydrogen peroxide and participates in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues (PubMed:11049757, PubMed:11134050, PubMed:20493079, PubMed:8316221, PubMed:8665924). Preferentially degrades benzylamine and phenylethylamine (PubMed:11049757, PubMed:11134050, PubMed:20493079, PubMed:8316221, PubMed:8665924)
- Specific Function
- Aliphatic amine oxidase activity
- Gene Name
- MAOB
- Uniprot ID
- P27338
- Uniprot Name
- Amine oxidase [flavin-containing] B
- Molecular Weight
- 58762.475 Da
References
- Bortolato M, Chen K, Shih JC: Monoamine oxidase inactivation: from pathophysiology to therapeutics. Adv Drug Deliv Rev. 2008 Oct-Nov;60(13-14):1527-33. doi: 10.1016/j.addr.2008.06.002. Epub 2008 Jul 4. [Article]
- Kaludercic N, Carpi A, Menabo R, Di Lisa F, Paolocci N: Monoamine oxidases (MAO) in the pathogenesis of heart failure and ischemia/reperfusion injury. Biochim Biophys Acta. 2011 Jul;1813(7):1323-32. doi: 10.1016/j.bbamcr.2010.09.010. Epub 2010 Sep 24. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Catalyzes the O-methylation, and thereby the inactivation, of catecholamine neurotransmitters and catechol hormones. Also shortens the biological half-lives of certain neuroactive drugs, like L-DOPA, alpha-methyl DOPA and isoproterenol
- Specific Function
- Catechol o-methyltransferase activity
- Gene Name
- COMT
- Uniprot ID
- P21964
- Uniprot Name
- Catechol O-methyltransferase
- Molecular Weight
- 30036.77 Da
References
- Ittiwut R, Listman JB, Ittiwut C, Cubells JF, Weiss RD, Brady K, Oslin D, Farrer LA, Kranzler HR, Gelernter J: Association between polymorphisms in catechol-O-methyltransferase (COMT) and cocaine-induced paranoia in European-American and African-American populations. Am J Med Genet B Neuropsychiatr Genet. 2011 Sep;156B(6):651-60. doi: 10.1002/ajmg.b.31205. Epub 2011 Jun 8. [Article]
- Boot E, Booij J, Abeling N, Meijer J, da Silva Alves F, Zinkstok J, Baas F, Linszen D, van Amelsvoort T: Dopamine metabolism in adults with 22q11 deletion syndrome, with and without schizophrenia--relationship with COMT Val(1)(0)(8)/(1)(5)(8)Met polymorphism, gender and symptomatology. J Psychopharmacol. 2011 Jul;25(7):888-95. doi: 10.1177/0269881111400644. Epub 2011 Mar 29. [Article]
- Volavka J, Bilder R, Nolan K: Catecholamines and aggression: the role of COMT and MAO polymorphisms. Ann N Y Acad Sci. 2004 Dec;1036:393-8. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Electrogenic voltage-dependent transporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics (PubMed:9260930, PubMed:9687576). Functions as a Na(+)-independent, bidirectional uniporter (PubMed:21128598, PubMed:9687576). Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient (PubMed:15212162, PubMed:9260930, PubMed:9687576). However, may also engage electroneutral cation exchange when saturating concentrations of cation substrates are reached (By similarity). Predominantly expressed at the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds by hepatic and renal clearance from the blood flow (PubMed:15783073). Implicated in monoamine neurotransmitters uptake such as histamine, dopamine, adrenaline/epinephrine, noradrenaline/norepinephrine, serotonin and tyramine, thereby supporting a physiological role in the central nervous system by regulating interstitial concentrations of neurotransmitters (PubMed:16581093, PubMed:17460754, PubMed:9687576). Also capable of transporting dopaminergic neuromodulators cyclo(his-pro), salsolinol and N-methyl-salsolinol, thereby involved in the maintenance of dopaminergic cell integrity in the central nervous system (PubMed:17460754). Mediates the bidirectional transport of acetylcholine (ACh) at the apical membrane of ciliated cell in airway epithelium, thereby playing a role in luminal release of ACh from bronchial epithelium (PubMed:15817714). Also transports guanidine and endogenous monoamines such as vitamin B1/thiamine, creatinine and N-1-methylnicotinamide (NMN) (PubMed:12089365, PubMed:15212162, PubMed:17072098, PubMed:24961373, PubMed:9260930). Mediates the uptake and efflux of quaternary ammonium compound choline (PubMed:9260930). Mediates the bidirectional transport of polyamine agmatine and the uptake of polyamines putrescine and spermidine (PubMed:12538837, PubMed:21128598). Able to transport non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) (PubMed:11907186). Also involved in the uptake of xenobiotic 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) (PubMed:12395288, PubMed:16394027). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
- Specific Function
- Acetylcholine transmembrane transporter activity
- Gene Name
- SLC22A2
- Uniprot ID
- O15244
- Uniprot Name
- Solute carrier family 22 member 2
- Molecular Weight
- 62579.99 Da
References
- 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]
- 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]
- Urakami Y, Okuda M, Masuda S, Akazawa M, Saito H, Inui K: Distinct characteristics of organic cation transporters, OCT1 and OCT2, in the basolateral membrane of renal tubules. Pharm Res. 2001 Nov;18(11):1528-34. [Article]
- 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]
- 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]
- Verhaagh S, Schweifer N, Barlow DP, Zwart R: Cloning of the mouse and human solute carrier 22a3 (Slc22a3/SLC22A3) identifies a conserved cluster of three organic cation transporters on mouse chromosome 17 and human 6q26-q27. Genomics. 1999 Jan 15;55(2):209-18. [Article]
- Grundemann D, Liebich G, Kiefer N, Koster S, Schomig E: Selective substrates for non-neuronal monoamine transporters. Mol Pharmacol. 1999 Jul;56(1):1-10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Electrogenic voltage-dependent transporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics (PubMed:11388889, PubMed:11408531, PubMed:12439218, PubMed:12719534, PubMed:15389554, PubMed:16263091, PubMed:16272756, PubMed:16581093, PubMed:19536068, PubMed:21128598, PubMed:23680637, PubMed:24961373, PubMed:34040533, PubMed:9187257, PubMed:9260930, PubMed:9655880). Functions as a pH- and Na(+)-independent, bidirectional transporter (By similarity). Cation cellular uptake or release is driven by the electrochemical potential (i.e. membrane potential and concentration gradient) and substrate selectivity (By similarity). Hydrophobicity is a major requirement for recognition in polyvalent substrates and inhibitors (By similarity). Primarily expressed at the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds by hepatic and renal clearance from the blood flow (By similarity). Most likely functions as an uptake carrier in enterocytes contributing to the intestinal elimination of organic cations from the systemic circulation (PubMed:16263091). Transports endogenous monoamines such as N-1-methylnicotinamide (NMN), guanidine, histamine, neurotransmitters dopamine, serotonin and adrenaline (PubMed:12439218, PubMed:24961373, PubMed:35469921, PubMed:9260930). Also transports natural polyamines such as spermidine, agmatine and putrescine at low affinity, but relatively high turnover (PubMed:21128598). Involved in the hepatic uptake of vitamin B1/thiamine, hence regulating hepatic lipid and energy metabolism (PubMed:24961373). Mediates the bidirectional transport of acetylcholine (ACh) at the apical membrane of ciliated cell in airway epithelium, thereby playing a role in luminal release of ACh from bronchial epithelium (PubMed:15817714). Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with lower efficency (PubMed:17460754). Also capable of transporting non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) (PubMed:11907186). May contribute to the transport of cationic compounds in testes across the blood-testis-barrier (Probable). Also involved in the uptake of xenobiotics tributylmethylammonium (TBuMA), quinidine, N-methyl-quinine (NMQ), N-methyl-quinidine (NMQD) N-(4,4-azo-n-pentyl)-quinuclidine (APQ), azidoprocainamide methoiodide (AMP), N-(4,4-azo-n-pentyl)-21-deoxyajmalinium (APDA) and 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) (PubMed:11408531, PubMed:15389554, PubMed:35469921, PubMed:9260930)
- Specific Function
- (r)-carnitine transmembrane transporter activity
- Gene Name
- SLC22A1
- Uniprot ID
- O15245
- Uniprot Name
- Solute carrier family 22 member 1
- Molecular Weight
- 61153.345 Da
References
- Bednarczyk D, Ekins S, Wikel JH, Wright SH: Influence of molecular structure on substrate binding to the human organic cation transporter, hOCT1. Mol Pharmacol. 2003 Mar;63(3):489-98. [Article]
- Zhang L, Schaner ME, Giacomini KM: Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa). J Pharmacol Exp Ther. 1998 Jul;286(1):354-61. [Article]
- Urakami Y, Okuda M, Masuda S, Akazawa M, Saito H, Inui K: Distinct characteristics of organic cation transporters, OCT1 and OCT2, in the basolateral membrane of renal tubules. Pharm Res. 2001 Nov;18(11):1528-34. [Article]
- 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]
- 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]
- Boxberger KH, Hagenbuch B, Lampe JN: Common drugs inhibit human organic cation transporter 1 (OCT1)-mediated neurotransmitter uptake. Drug Metab Dispos. 2014 Jun;42(6):990-5. doi: 10.1124/dmd.113.055095. Epub 2014 Mar 31. [Article]
- Grundemann D, Liebich G, Kiefer N, Koster S, Schomig E: Selective substrates for non-neuronal monoamine transporters. Mol Pharmacol. 1999 Jul;56(1):1-10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Electrogenic voltage-dependent transporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics (PubMed:10196521, PubMed:10966924, PubMed:12538837, PubMed:17460754, PubMed:20858707). Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient (PubMed:10966924). Functions as a Na(+)- and Cl(-)-independent, bidirectional uniporter (PubMed:12538837). Implicated in monoamine neurotransmitters uptake such as dopamine, adrenaline/epinephrine, noradrenaline/norepinephrine, histamine, serotonin and tyramine, thereby supporting a role in homeostatic regulation of aminergic neurotransmission in the brain (PubMed:10196521, PubMed:16581093, PubMed:20858707). Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with low efficiency (PubMed:17460754). May be involved in the uptake and disposition of cationic compounds by renal clearance from the blood flow (PubMed:10966924). May contribute to regulate the transport of cationic compounds in testis across the blood-testis-barrier (Probable). Mediates the transport of polyamine spermidine and putrescine (By similarity). Mediates the bidirectional transport of polyamine agmatine (PubMed:12538837). Also transports guanidine (PubMed:10966924). May also mediate intracellular transport of organic cations, thereby playing a role in amine metabolism and intracellular signaling (By similarity)
- Specific Function
- Monoamine transmembrane transporter activity
- Gene Name
- SLC22A3
- Uniprot ID
- O75751
- Uniprot Name
- Solute carrier family 22 member 3
- Molecular Weight
- 61279.485 Da
References
- 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]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General 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 (PubMed:10454528, PubMed:10525100, PubMed:10966938, PubMed:17509700, PubMed:20722056, PubMed:33124720). Also transports organic cations such as tetraethylammonium (TEA) without the involvement of sodium. Relative uptake activity ratio of carnitine to TEA is 11.3 (PubMed:10454528, PubMed:10525100, PubMed:10966938). In intestinal epithelia, transports the quorum-sensing pentapeptide CSF (competence and sporulation factor) from Bacillus Subtilis wich induces cytoprotective heat shock proteins contributing to intestinal homeostasis (PubMed:18005709). May also contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
- Specific Function
- (r)-carnitine transmembrane transporter activity
- Gene Name
- SLC22A5
- Uniprot ID
- O76082
- Uniprot Name
- Organic cation/carnitine transporter 2
- Molecular Weight
- 62751.08 Da
References
- 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]
- 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
- Transcription factor that binds to the octamer motif (5'-ATTTGCAT-3'). Forms a trimeric complex with SOX2 or SOX15 on DNA and controls the expression of a number of genes involved in embryonic development such as YES1, FGF4, UTF1 and ZFP206. Critical for early embryogenesis and for embryonic stem cell pluripotency
- Specific Function
- Dna binding
- Gene Name
- POU5F1
- Uniprot ID
- Q01860
- Uniprot Name
- POU domain, class 5, transcription factor 1
- Molecular Weight
- 38570.415 Da
References
- 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 September 15, 2024 04:51