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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyIdentification
- Name
- Dopamine
- Accession Number
- DB00988 (APRD00085)
- Type
- Small Molecule
- Groups
- Approved
- Description
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.
- Structure
Structure for Dopamine (DB00988)
- 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
- Product Ingredients
Ingredient UNII CAS InChI Key Dopamine hydrochloride 7L3E358N9L 62-31-7 CTENFNNZBMHDDG-UHFFFAOYSA-N - Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End 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 HCl Inj 4% Liquid 40 mg Intravenous International Medication Systems, Limited 1980-12-31 1997-08-15 Canada 
Dopamine Hydrochloride Injection, solution, concentrate 40 mg/1mL Intravenous General Injectables & Vaccines 2015-09-18 Not applicable US DOPamine Hydrochloride Injection, solution, concentrate 40 mg/1mL Intravenous Hospira, Inc. 2005-06-30 Not applicable US Dopamine Hydrochloride Injection, solution, concentrate 40 mg/1mL Intravenous General Injectables & Vaccines 2010-08-01 Not applicable US DOPamine Hydrochloride Injection, solution, concentrate 40 mg/1mL Intravenous Hospira, Inc. 2005-08-25 Not applicable US DOPamine Hydrochloride Injection, solution, concentrate 40 mg/1mL Intravenous Remedy Repack 2015-01-23 2016-02-05 US DOPamine Hydrochloride Injection, solution, concentrate 40 mg/1mL Intravenous Cardinal Health 1981-05-19 Not applicable US DOPamine HYDROCHLORIDE AND DEXTROSE Injection, solution 160 mg/100mL Intravenous Hospira, Inc. 2005-02-28 2009-06-01 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End 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 1990-09-30 Not applicable 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 1990-09-30 Not applicable US Dopamine HCl Injection, solution 80 mg/1mL Intravenous Cardinal Health 1990-09-30 Not applicable US Dopamine HCl Injection, solution 160 mg/1mL Intravenous American Regent 1990-09-30 Not applicable US Dopamine HCl Injection, solution 40 mg/1mL Intravenous Cardinal Health 1987-02-11 Not applicable US Dopamine Hydrochloride Injection 80 mg/1mL Intravenous West-Ward Pharmaceuticals Corp 2018-04-11 Not applicable US Dopamine Hydrochloride Injection 40 mg/1mL Intravenous West-Ward Pharmaceuticals Corp 2018-04-11 Not applicable US Dopamine Hydrochloride Injection, solution 40 mg/1mL Intravenous General Injectables & Vaccines 2010-07-01 2013-12-01 US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Dopamine HCl 0.8mg/ml Dextrose 5% Inj USP Dopamine hydrochloride (.8 mg) + Dextrose, unspecified form (50 mg) Solution Intravenous Baxter Laboratories 1992-12-31 Not applicable Canada Dopamine HCl 1.6mg/ml Dextrose 5% Inj USP Dopamine hydrochloride (1.6 mg) + Dextrose, unspecified form (50 mg) Solution Intravenous Baxter Laboratories 1990-12-31 Not applicable Canada Dopamine HCl 3.2mg/ml Dextrose 5% Inj USP Dopamine hydrochloride (3.2 mg) + Dextrose, unspecified form (50 mg) Solution Intravenous Baxter Laboratories 1990-12-31 Not applicable Canada Dopamine Hydrochloride and 5% Dextrose Injection USP Dopamine hydrochloride (3.2 mg) + Dextrose, unspecified form (50 mg) Solution Intravenous Hospira, Inc. 1991-12-31 Not applicable Canada Dopamine Hydrochloride and 5% Dextrose Injection USP Dopamine hydrochloride (0.8 mg) + Dextrose, unspecified form (50 mg) Solution Intravenous Hospira, Inc. 1986-12-31 Not applicable Canada Dopamine Hydrochloride and 5% Dextrose Injection USP Dopamine hydrochloride (1.6 mg) + Dextrose, unspecified form (50 mg) Solution Intravenous Hospira, Inc. 1986-12-31 Not applicable Canada Dopamine Hydrochloride in Dextrose Dopamine hydrochloride (160 mg/100mL) + D-glucose monohydrate (5 g/100mL) Injection, solution Intravenous B. Braun Medical Inc. 2007-03-01 2012-09-01 US Dopamine Hydrochloride in Dextrose Dopamine hydrochloride (320 mg/100mL) + D-glucose monohydrate (5 g/100mL) Injection, solution Intravenous B. Braun Medical Inc. 2007-03-01 2012-09-01 US Dopamine Hydrochloride in Dextrose Dopamine hydrochloride (80 mg/100mL) + D-glucose monohydrate (5 g/100mL) Injection, solution Intravenous B. Braun Medical Inc. 2007-03-01 2012-09-01 US Dopamine Hydrochloride in Dextrose Dopamine hydrochloride (160 mg/100mL) + D-glucose monohydrate (5 g/100mL) Injection, solution Intravenous B. Braun Medical Inc. 2007-03-01 2012-09-01 US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End DOPamine Hydrochloride Dopamine hydrochloride (80 mg/1mL) Injection, solution, concentrate Intravenous Hospira 2008-07-21 2008-07-21 US DOPamine Hydrochloride and Dextrose Dopamine hydrochloride (80 mg/100mL) Injection, solution Intravenous Hospira, Inc. 2006-07-19 2006-07-19 US - International/Other Brands
- Intropin / Revimine
- Categories
- Adrenergic and Dopaminergic Agents
- Amines
- Autonomic Agents
- Biogenic Amines
- Biogenic Monoamines
- Cardiac Stimulants Excl. Cardiac Glycosides
- Cardiac Therapy
- Cardiotonic Agents
- Cardiovascular Agents
- Cardiovascular System
- Catecholamines
- COMT Substrates
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Dopamine Agents
- Dopamine Agonists
- Dopamine D1 Receptor Agonists
- Dopamine D2 Receptor Agonists
- Neurotransmitter Agents
- OCT2 Inhibitors
- OCT2 Substrates
- Peripheral Nervous System Agents
- Protective Agents
- Selective Beta 1-adrenergic Agonists
- Sympathomimetics
- UNII
- VTD58H1Z2X
- CAS number
- 51-61-6
- Weight
- Average: 153.1784
Monoisotopic: 153.078978601 - Chemical Formula
- C8H11NO2
- 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
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
- Associated Conditions
- Arrythmias
- Circulatory collapse and shock
- Feeling Anxious
- Hypotension caused by Trauma, endotoxic septicemia, Open-heart Surgery, Renal Failure, chronic cardiac decompensation, Myocardial Infarction
- Mental confusion
- Urine flow decreased caused by Trauma, endotoxic septicemia, Open-heart Surgery, Renal Failure, chronic cardiac decompensation, Myocardial Infarction
- Decreased cardiac output caused by Trauma, endotoxic septicemia, Open-heart Surgery, Renal Failure, chronic cardiac decompensation, Myocardial Infarction
- 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 actas as an agonist to the five dopamine receptor subtypes (D!, D2, D3, D4, D5).
Target Actions Organism AD(2) dopamine receptor agonistHuman AD(1A) dopamine receptor agonistHuman AD(1B) dopamine receptor agonistHuman AD(3) dopamine receptor agonistHuman AD(4) dopamine receptor agonistHuman ASodium-dependent dopamine transporter inducerHuman ADopamine beta-hydroxylase ligandHuman U5-hydroxytryptamine receptor 1A binderHuman U5-hydroxytryptamine receptor 7 binderHuman UD(1) dopamine receptor agonistHuman USodium-dependent noradrenaline transporter inhibitorHuman USodium-dependent serotonin transporter inhibitorHuman U5-hydroxytryptamine receptor 3A Not Available Human U5-hydroxytryptamine receptor 3B Not Available Human USuperoxide dismutase [Cu-Zn] Not Available Human USynaptic vesicular amine transporter Not Available Human - 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).
- 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
- 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.
- Affected organisms
- Humans and other mammals
- Pathways
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction Abiraterone The serum concentration of Dopamine can be increased when it is combined with Abiraterone. Acebutolol The risk or severity of adverse effects can be increased when Dopamine is combined with Acebutolol. Acetaminophen Acetaminophen may decrease the excretion rate of Dopamine which could result in a higher serum level. Acetyl sulfisoxazole The metabolism of Dopamine can be decreased when combined with Acetyl sulfisoxazole. Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Dopamine which could result in a higher serum level. Agmatine The serum concentration of Agmatine can be increased when it is combined with Dopamine. Alprazolam Alprazolam may decrease the excretion rate of Dopamine which could result in a higher serum level. Amiloride The serum concentration of Dopamine can be increased when it is combined with Amiloride. Amitriptyline Dopamine may decrease the excretion rate of Amitriptyline which could result in a higher serum level. Amlodipine Amlodipine may decrease the excretion rate of Dopamine which could result in a higher serum level. - Food Interactions
- Not Available
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. [PubMed:17237217]
- Giuliano F, Allard J: Dopamine and male sexual function. Eur Urol. 2001 Dec;40(6):601-8. [PubMed:11805404]
- Giuliano F, Allard J: Dopamine and sexual function. Int J Impot Res. 2001 Aug;13 Suppl 3:S18-28. [PubMed:11477488]
- 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. [PubMed:9858756]
- 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. [PubMed:14561867]
- External Links
- Human Metabolome Database
- HMDB0000073
- KEGG Drug
- D07870
- KEGG Compound
- C03758
- PubChem Compound
- 681
- PubChem Substance
- 46506043
- ChemSpider
- 661
- BindingDB
- 55121
- ChEBI
- 18243
- ChEMBL
- CHEMBL59
- Therapeutic Targets Database
- DAP000212
- PharmGKB
- PA449396
- IUPHAR
- 940
- Guide to Pharmacology
- GtP Drug Page
- HET
- LDP
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Dopamine
- ATC Codes
- C01CA04 — Dopamine
- AHFS Codes
- 12:12.08.08 — Selective Beta 1-adrenergic Agonists
- PDB Entries
- 2a3r / 2qmz / 2vq5 / 3nk2 / 4a7v / 4dtz / 4du2 / 4dub / 4xp1 / 5log … show 2 more
- MSDS
- Download (72.1 KB)
Clinical Trials
- Clinical Trials
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 160 mg/1mL Injection, solution Intravenous 40 mg/1mL Injection, solution Intravenous 80 mg/1mL Solution Intravenous Liquid Intravenous 40 mg Injection Intravenous 40 mg/1mL Injection Intravenous 80 mg/1mL 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 Intravenous 40 mg - 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
Taxonomy
- 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
- Catecholamine / Phenethylamine / 2-arylethylamine / 1-hydroxy-4-unsubstituted benzenoid / 1-hydroxy-2-unsubstituted benzenoid / Aralkylamine / Monocyclic benzene moiety / Amine / Hydrocarbon derivative / Primary amine
- Molecular Framework
- Aromatic homomonocyclic compounds
- External Descriptors
- catecholamine (CHEBI:18243) / Biogenic amines, Tyramine derivatives, Dopamine (C03758)
Targets
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Potassium channel regulator activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
- Gene Name
- DRD2
- Uniprot ID
- P14416
- Uniprot Name
- D(2) dopamine receptor
- Molecular Weight
- 50618.91 Da
References
- 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. [PubMed:17301410]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- G-protein coupled amine receptor activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
- Gene Name
- DRD1
- Uniprot ID
- P21728
- Uniprot Name
- D(1A) dopamine receptor
- Molecular Weight
- 49292.765 Da
References
- 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. [PubMed:17301410]
- 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. [PubMed:17455212]
- 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. [PubMed:17449449]
- 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. [PubMed:17394052]
- 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. [PubMed:17468175]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- G-protein coupled amine receptor activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
- Gene Name
- DRD5
- Uniprot ID
- P21918
- Uniprot Name
- D(1B) dopamine receptor
- Molecular Weight
- 52950.5 Da
References
- 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. [PubMed:17301410]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- G-protein coupled amine receptor activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
- Gene Name
- DRD3
- Uniprot ID
- P35462
- Uniprot Name
- D(3) dopamine receptor
- Molecular Weight
- 44224.335 Da
References
- 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. [PubMed:17301410]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Sh3 domain binding
- Specific Function
- Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins ...
- Gene Name
- DRD4
- Uniprot ID
- P21917
- Uniprot Name
- D(4) dopamine receptor
- Molecular Weight
- 48359.86 Da
References
- 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. [PubMed:17301410]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Inducer
- General Function
- Monoamine transmembrane transporter activity
- Specific Function
- Amine transporter. Terminates the action of dopamine by its high affinity sodium-dependent reuptake into presynaptic terminals.
- Gene Name
- SLC6A3
- Uniprot ID
- Q01959
- Uniprot Name
- Sodium-dependent dopamine transporter
- Molecular Weight
- 68494.255 Da
References
- 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. [PubMed:17301410]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Ligand
- General Function
- L-ascorbic acid binding
- Specific Function
- Conversion of dopamine to noradrenaline.
- 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. [PubMed:17258889]
- 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. [PubMed:17561816]
- 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. [PubMed:17625104]
- 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. [PubMed:17287146]
- 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. [PubMed:17433386]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
- Gene Name
- HTR1A
- Uniprot ID
- P08908
- Uniprot Name
- 5-hydroxytryptamine receptor 1A
- Molecular Weight
- 46106.335 Da
References
- 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. [PubMed:9185324]
- 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. [PubMed:9686407]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Serotonin receptor activity
- Specific Function
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
- Gene Name
- HTR7
- Uniprot ID
- P34969
- Uniprot Name
- 5-hydroxytryptamine receptor 7
- Molecular Weight
- 53554.43 Da
References
- 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. [PubMed:8398139]
- 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. [PubMed:8394362]
- Kind
- Protein group
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- G-protein coupled amine receptor activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
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. [PubMed:10691700]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- 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
- 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. [PubMed:11071707]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Serotonin:sodium symporter activity
- Specific Function
- Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into t...
- Gene Name
- SLC6A4
- Uniprot ID
- P31645
- Uniprot Name
- Sodium-dependent serotonin transporter
- Molecular Weight
- 70324.165 Da
References
- 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. [PubMed:11071707]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- General Function
- Voltage-gated potassium channel activity
- Specific Function
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gate...
- Gene Name
- HTR3A
- Uniprot ID
- P46098
- Uniprot Name
- 5-hydroxytryptamine receptor 3A
- Molecular Weight
- 55279.835 Da
References
- 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. [PubMed:17360702]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- General Function
- Serotonin-activated cation-selective channel activity
- Specific Function
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gate...
- Gene Name
- 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. [PubMed:17360702]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- General Function
- Zinc ion binding
- Specific Function
- Destroys radicals which are normally produced within the cells and which are toxic to biological systems.
- 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. [PubMed:23612299]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- 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
- 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. [PubMed:7912402]
Enzymes
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Serotonin binding
- Specific Function
- Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral...
- 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. [PubMed:18652859]
- 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. [PubMed:20869994]
- 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. [PubMed:15817751]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Primary amine oxidase activity
- Specific Function
- Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral...
- 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. [PubMed:18652859]
- 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. [PubMed:20869994]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- O-methyltransferase activity
- Specific 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-DOP...
- 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. [PubMed:21656904]
- 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. [PubMed:21447540]
- 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. [PubMed:15817751]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- L-ascorbic acid binding
- Specific Function
- Conversion of dopamine to noradrenaline.
- 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. [PubMed:17258889]
- 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. [PubMed:17561816]
- 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. [PubMed:17625104]
- 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. [PubMed:17287146]
- 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. [PubMed:17433386]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Transporters
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- 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. [PubMed:12089365]
- 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. [PubMed:9830022]
- 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. [PubMed:11758759]
- 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. [PubMed:9687576]
- 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. [PubMed:9812985]
- 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. [PubMed:9933568]
- 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. [PubMed:10385678]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- 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. [PubMed:12606755]
- 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. [PubMed:9655880]
- 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. [PubMed:11758759]
- 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. [PubMed:8898084]
- 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. [PubMed:9776363]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- 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
- 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. [PubMed:9830022]
- Kind
- Protein
- Organism
- Human
- 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
- 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. [PubMed:11160873]
- 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. [PubMed:10454528]
- Kind
- Protein
- Organism
- Human
- 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
- 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. [PubMed:20402963]
Drug created on June 13, 2005 07:24 / Updated on September 21, 2018 00:07