Identification
- Summary
Bumetanide is a sulfamyl diuretic used to treat edema in congestive heart failure, hepatic and renal disease, and nephrotic syndrome.
- Brand Names
- Bumex, Burinex
- Generic Name
- Bumetanide
- DrugBank Accession Number
- DB00887
- Background
Bumetanide is a sulfamyl diuretic.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Bumetanide (DB00887)
- Weight
- Average: 364.416
Monoisotopic: 364.10929245 - Chemical Formula
- C17H20N2O5S
- Synonyms
- 3-(aminosulfonyl)-5-(butylamino)-4-phenoxybenzoic acid
- 3-butylamino-4-(phenoxy)-5-sulfamoylbenzoic acid
- 3-butylamino-4-phenoxy-5-sulfamoyl-benzoic acid
- 3-butylamino-4-phenoxy-5-sulfamoylbenzoic acid
- Bumetanida
- Bumetanide
- Bumetanidum
- External IDs
- CS 380
- RO 10-6338
- RO-10-6338
Pharmacology
- Indication
For the treatment of edema associated with congestive heart failure, hepatic and renal disease including the nephrotic syndrome.
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
Bumetanide is a loop diuretic of the sulfamyl category to treat heart failure. It is often used in patients in whom high doses of furosemide are ineffective. There is however no reason not to use bumetanide as a first choice drug. The main difference between the two substances is in bioavailability. Bumetanide has more predictable pharmacokinetic properties as well as clinical effect. In patients with normal renal function, bumetanide is 40 times more effective than furosemide.
- Mechanism of action
Bumetanide interferes with renal cAMP and/or inhibits the sodium-potassium ATPase pump. Bumetanide appears to block the active reabsorption of chloride and possibly sodium in the ascending loop of Henle, altering electrolyte transfer in the proximal tubule. This results in excretion of sodium, chloride, and water and, hence, diuresis.
Target Actions Organism ASolute carrier family 12 member 1 inhibitorHumans ASolute carrier family 12 member 2 inhibitorHumans ASolute carrier family 12 member 4 inhibitorHumans ASolute carrier family 12 member 5 inhibitorHumans UCystic fibrosis transmembrane conductance regulator antagonistHumans - Absorption
Bumetanide is completely absorbed (80%), and the absorption is not altered when taken with food. Bioavailability is almost complete.
- Volume of distribution
Not Available
- Protein binding
97%
- Metabolism
45% is secreted unchanged. Urinary and biliary metabolites are formed by oxidation of the N-butyl side chain.
- Route of elimination
Oral administration of carbon-14 labeled Bumex to human volunteers revealed that 81% of the administered radioactivity was excreted in the urine, 45% of it as unchanged drug. Biliary excretion of Bumex amounted to only 2% of the administered dose.
- Half-life
60-90 minutes
- Clearance
- 0.2 - 1.1 mL/min/kg [preterm and full-term neonates with respiratory disorders]
- 2.17 mL/min/kg [neonates receiving bumetanide for volume overload]
- 1.8 +/- 0.3 mL/min/kg [geriatric subjects]
- 2.9 +/- 0.2 mL/min/kg [younger subjects]
- 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
Overdosage can lead to acute profound water loss, volume and electrolyte depletion, dehydration, reduction of blood volume and circulatory collapse with a possibility of vascular thrombosis and embolism. Electrolyte depletion may be manifested by weakness, dizziness, mental confusion, anorexia, lethargy, vomiting and cramps. Treatment consists of replacement of fluid and electrolyte losses by careful monitoring of the urine and electrolyte output and serum electrolyte levels.
- Pathways
Pathway Category Bumetanide Action Pathway Drug action - Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Bumetanide may increase the excretion rate of Abacavir which could result in a lower serum level and potentially a reduction in efficacy. Abaloparatide The risk or severity of adverse effects can be increased when Bumetanide is combined with Abaloparatide. Acamprosate The excretion of Acamprosate can be decreased when combined with Bumetanide. Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Bumetanide. Acebutolol The risk or severity of adverse effects can be increased when Bumetanide is combined with Acebutolol. - Food Interactions
- Take with food. Food reduces irritation.
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 Images
- International/Other Brands
- Burinex (F. Hoffmann-La Roche Ltd.) / Fordiuran (LEO Pharma A/S) / Lunetoron (Daiichi Sankyo)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Bumex Tablet 0.5 mg/1 Oral Genentech, Inc. 1983-02-28 2007-10-31 US 
Bumex Tablet 1 mg/1 Oral Validus Pharmaceuticals LLC 1983-02-28 Not applicable US Bumex Tablet 1 mg/1 Oral Physicians Total Care, Inc. 1996-04-04 2011-05-31 US Bumex Tablet 0.5 mg/1 Oral Validus Pharmaceuticals LLC 1983-02-28 Not applicable US Bumex Tablet 1 mg/1 Oral Genentech, Inc. 1983-02-28 2008-06-30 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Bumetanide Tablet 1 mg/1 Oral Paragon Enterprises Inc 2016-11-16 2016-11-17 US Bumetanide Injection, solution 0.25 mg/1mL Intramuscular; Intravenous Hospira, Inc. 2006-07-06 Not applicable US Bumetanide Tablet 1 mg/1 Oral AvKARE, Inc. 2015-01-26 2018-09-17 US Bumetanide Tablet 0.5 mg/1 Oral Heritage Pharmaceuticals Inc. d/b/a Avet Pharmaceuticals Inc. 2019-06-01 Not applicable US Bumetanide Tablet 0.5 mg/1 Oral Taro Pharmaceuticals U.S.A., Inc. 2023-07-24 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image BURINEX TABLET 1 mg Bumetanide (1 mg) + Bumetanide (1.0 mg) Tablet Oral ZUELLIG PHARMA PTE. LTD. 1988-03-05 Not applicable Singapore 
BURINEX TABLET 1 mg Bumetanide (1 mg) + Bumetanide (1.0 mg) Tablet Oral ZUELLIG PHARMA PTE. LTD. 1988-03-05 Not applicable Singapore - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Bumex Bumetanide (1 mg/1) Tablet Oral Physicians Total Care, Inc. 1996-04-04 2011-05-31 US
Categories
- ATC Codes
- G01AE10 — Combinations of sulfonamides
- G01AE — Sulfonamides
- G01A — ANTIINFECTIVES AND ANTISEPTICS, EXCL. COMBINATIONS WITH CORTICOSTEROIDS
- G01 — GYNECOLOGICAL ANTIINFECTIVES AND ANTISEPTICS
- G — GENITO URINARY SYSTEM AND SEX HORMONES
- C03CB — Sulfonamides and potassium in combination
- C03C — HIGH-CEILING DIURETICS
- C03 — DIURETICS
- C — CARDIOVASCULAR SYSTEM
- C03EB — High-ceiling diuretics and potassium-sparing agents
- C03E — DIURETICS AND POTASSIUM-SPARING AGENTS IN COMBINATION
- C03 — DIURETICS
- C — CARDIOVASCULAR SYSTEM
- Drug Categories
- Acids, Carbocyclic
- Agents Causing Muscle Toxicity
- Amides
- Aminobenzoates
- Benzene Derivatives
- Benzoates
- Cardiovascular Agents
- Diuretics
- Drugs causing inadvertant photosensitivity
- Drugs that are Mainly Renally Excreted
- Genito Urinary System and Sex Hormones
- Gynecological Antiinfectives and Antiseptics
- High-Ceiling Diuretics
- High-Ceiling Diuretics and Potassium-Sparing Agents
- Hyperglycemia-Associated Agents
- Hypotensive Agents
- Increased Diuresis at Loop of Henle
- Membrane Transport Modulators
- meta-Aminobenzoates
- Natriuretic Agents
- Nephrotoxic agents
- Non Potassium Sparing Diuretics
- OAT1/SLC22A6 inhibitors
- OAT3/SLC22A8 Inhibitors
- OAT3/SLC22A8 Substrates
- Photosensitizing Agents
- Sodium Potassium Chloride Symporter Inhibitors
- Sulfonamides
- Sulfones
- Sulfur Compounds
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as diphenylethers. These are aromatic compounds containing two benzene rings linked to each other through an ether group.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Diphenylethers
- Direct Parent
- Diphenylethers
- Alternative Parents
- Aminobenzenesulfonamides / Diarylethers / Aminobenzoic acids / Benzenesulfonyl compounds / Benzoic acids / Phenylalkylamines / Aniline and substituted anilines / Phenoxy compounds / Phenol ethers / Benzoyl derivatives show 9 more
- Substituents
- Amine / Amino acid / Amino acid or derivatives / Aminobenzenesulfonamide / Aminobenzoic acid / Aminobenzoic acid or derivatives / Aminosulfonyl compound / Aniline or substituted anilines / Aromatic homomonocyclic compound / Benzenesulfonamide show 27 more
- Molecular Framework
- Aromatic homomonocyclic compounds
- External Descriptors
- sulfonamide, benzoic acids, amino acid (CHEBI:3213)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 0Y2S3XUQ5H
- CAS number
- 28395-03-1
- InChI Key
- MAEIEVLCKWDQJH-UHFFFAOYSA-N
- InChI
- InChI=1S/C17H20N2O5S/c1-2-3-9-19-14-10-12(17(20)21)11-15(25(18,22)23)16(14)24-13-7-5-4-6-8-13/h4-8,10-11,19H,2-3,9H2,1H3,(H,20,21)(H2,18,22,23)
- IUPAC Name
- 3-(butylamino)-4-phenoxy-5-sulfamoylbenzoic acid
- SMILES
- CCCCNC1=C(OC2=CC=CC=C2)C(=CC(=C1)C(O)=O)S(N)(=O)=O
References
- Synthesis Reference
Felt, P.W.; US. Patent 3,634,583; January 11, 1972; assigned to Lovens Kemiske Fabrik Produktionsaktieselskab, Denmark.
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0015024
- KEGG Drug
- D00247
- PubChem Compound
- 2471
- PubChem Substance
- 46508147
- ChemSpider
- 2377
- BindingDB
- 25903
- 1808
- ChEBI
- 3213
- ChEMBL
- CHEMBL1072
- ZINC
- ZINC000003813061
- Therapeutic Targets Database
- DAP000361
- PharmGKB
- PA448682
- PDBe Ligand
- 82U
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Bumetanide
- PDB Entries
- 7s1x / 7s1y / 7smp
- FDA label
- Download (206 KB)
- MSDS
- Download (72.8 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Treatment Heart Failure 1 4 Recruiting Treatment Acute Heart Failure (AHF) / Diuretics Drug Reactions 1 4 Recruiting Treatment Chronic Kidney Disease (CKD) / Hypertension 1 4 Recruiting Treatment Congestive Heart Failure (CHF) 1 4 Recruiting Treatment Heart Failure With Preserved Ejection Fraction (HFpEF) 1
Pharmacoeconomics
- Manufacturers
- Baxter healthcare corp anesthesia and critical care
- Bedford laboratories div ben venue laboratories inc
- Hospira inc
- Teva parenteral medicines inc
- Validus pharmaceuticals inc
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- Sandoz inc
- Packagers
- Advanced Pharmaceutical Services Inc.
- Amerisource Health Services Corp.
- Baxter International Inc.
- Bedford Labs
- Ben Venue Laboratories Inc.
- Cardinal Health
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Eon Labs
- F Hoffmann-La Roche Ltd.
- Heartland Repack Services LLC
- Hospira Inc.
- Ivax Pharmaceuticals
- Major Pharmaceuticals
- Mckesson Corp.
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Neuman Distributors Inc.
- Nucare Pharmaceuticals Inc.
- PD-Rx Pharmaceuticals Inc.
- Pharmaceutical Utilization Management Program VA Inc.
- Physicians Total Care Inc.
- Sandhills Packaging Inc.
- Teva Pharmaceutical Industries Ltd.
- UDL Laboratories
- Vangard Labs Inc.
- Dosage Forms
Form Route Strength Tablet Oral 1.000 mg Injection Intramuscular; Intravenous 0.25 mg/1mL Injection, solution Intramuscular; Intravenous 0.25 mg/1mL Injection, solution Intravenous 0.25 mg/1mL Tablet Oral .5 mg/1 Tablet Oral 0.5 mg/1 Tablet Oral 2 mg/1 Tablet Oral 1 mg/1 Capsule Tablet Oral 1 mg Tablet Oral 5 mg Tablet Oral 2 mg Injection, solution Intravenous 0.5 mg/ml Injection Intramuscular; Intravenous 0.5 mg/ml Injection Intramuscular; Intravenous Tablet Oral 1 mg Tablet Oral Solution Intravenous 0.5000 mg Tablet Oral 1.00 mg - Prices
Unit description Cost Unit Bumex 2 mg tablet 1.65USD tablet Bumetanide 2 mg tablet 1.04USD tablet Bumex 1 mg tablet 0.98USD tablet Bumex 0.5 mg tablet 0.7USD tablet Bumetanide 1 mg tablet 0.51USD tablet Bumetanide 0.5 mg tablet 0.38USD tablet Bumetanide 0.25 mg/ml vial 0.25USD 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) 230-231 Felt, P.W.; US. Patent 3,634,583; January 11, 1972; assigned to Lovens Kemiske Fabrik Produktionsaktieselskab, Denmark. water solubility >20 mg/mL (in base) Not Available logP 2.6 Not Available - Predicted Properties
Property Value Source Water Solubility 0.0257 mg/mL ALOGPS logP 3.44 ALOGPS logP 2.42 Chemaxon logS -4.2 ALOGPS pKa (Strongest Acidic) 4.69 Chemaxon pKa (Strongest Basic) 2.7 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 118.72 Å2 Chemaxon Rotatable Bond Count 8 Chemaxon Refractivity 95.78 m3·mol-1 Chemaxon Polarizability 37.21 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9967 Blood Brain Barrier - 0.6636 Caco-2 permeable - 0.6492 P-glycoprotein substrate Non-substrate 0.509 P-glycoprotein inhibitor I Non-inhibitor 0.8765 P-glycoprotein inhibitor II Non-inhibitor 0.8103 Renal organic cation transporter Non-inhibitor 0.8966 CYP450 2C9 substrate Non-substrate 0.6368 CYP450 2D6 substrate Non-substrate 0.7656 CYP450 3A4 substrate Non-substrate 0.6059 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.9071 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7344 Ames test Non AMES toxic 0.6794 Carcinogenicity Non-carcinogens 0.7294 Biodegradation Not ready biodegradable 0.9837 Rat acute toxicity 1.8148 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9319 hERG inhibition (predictor II) Non-inhibitor 0.8591
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 202.1862591 predictedDarkChem Lite v0.1.0 [M-H]- 201.1089591 predictedDarkChem Lite v0.1.0 [M-H]- 182.65544 predictedDeepCCS 1.0 (2019) [M+H]+ 202.6577591 predictedDarkChem Lite v0.1.0 [M+H]+ 202.0907591 predictedDarkChem Lite v0.1.0 [M+H]+ 185.03035 predictedDeepCCS 1.0 (2019) [M+Na]+ 202.2088591 predictedDarkChem Lite v0.1.0 [M+Na]+ 201.4214591 predictedDarkChem Lite v0.1.0 [M+Na]+ 193.31616 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
- Inhibitor
- General Function
- Sodium:potassium:chloride symporter activity
- Specific Function
- Electrically silent transporter system. Mediates sodium and chloride reabsorption. Plays a vital role in the regulation of ionic balance and cell volume.
- Gene Name
- SLC12A1
- Uniprot ID
- Q13621
- Uniprot Name
- Solute carrier family 12 member 1
- Molecular Weight
- 121449.13 Da
References
- Thakker RV: Chloride channels in renal disease. Adv Nephrol Necker Hosp. 1999;29:289-98. [Article]
- Karolyi L, Koch MC, Grzeschik KH, Seyberth HW: The molecular genetic approach to "Bartter's syndrome". J Mol Med (Berl). 1998 Apr;76(5):317-25. [Article]
- Thakker RV: The role of renal chloride channel mutations in kidney stone disease and nephrocalcinosis. Curr Opin Nephrol Hypertens. 1998 Jul;7(4):385-8. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Long P, Mercer A, Begum R, Stephens GJ, Sihra TS, Jovanovic JN: Nerve Terminal GABAA Receptors Activate Ca2+/Calmodulin-dependent Signaling to Inhibit Voltage-gated Ca2+ Influx and Glutamate Release. J Biol Chem. 2009 Mar 27;284(13):8726-37. doi: 10.1074/jbc.M805322200. Epub 2009 Jan 13. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Sodium:potassium:chloride symporter activity
- Specific Function
- Electrically silent transporter system. Mediates sodium and chloride reabsorption. Plays a vital role in the regulation of ionic balance and cell volume.
- Gene Name
- SLC12A2
- Uniprot ID
- P55011
- Uniprot Name
- Solute carrier family 12 member 2
- Molecular Weight
- 131445.825 Da
References
- Panet R, Marcus M, Atlan H: Overexpression of the Na(+)/K(+)/Cl(-) cotransporter gene induces cell proliferation and phenotypic transformation in mouse fibroblasts. J Cell Physiol. 2000 Jan;182(1):109-18. [Article]
- Evans RL, Park K, Turner RJ, Watson GE, Nguyen HV, Dennett MR, Hand AR, Flagella M, Shull GE, Melvin JE: Severe impairment of salivation in Na+/K+/2Cl- cotransporter (NKCC1)-deficient mice. J Biol Chem. 2000 Sep 1;275(35):26720-6. [Article]
- Wall SM, Fischer MP, Mehta P, Hassell KA, Park SJ: Contribution of the Na+-K+-2Cl- cotransporter NKCC1 to Cl- secretion in rat OMCD. Am J Physiol Renal Physiol. 2001 May;280(5):F913-21. [Article]
- Akar F, Jiang G, Paul RJ, O'Neill WC: Contractile regulation of the Na(+)-K(+)-2Cl(-) cotransporter in vascular smooth muscle. Am J Physiol Cell Physiol. 2001 Aug;281(2):C579-84. [Article]
- Jiang G, Klein JD, O'Neill WC: Growth factors stimulate the Na-K-2Cl cotransporter NKCC1 through a novel Cl(-)-dependent mechanism. Am J Physiol Cell Physiol. 2001 Dec;281(6):C1948-53. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Protein kinase binding
- Specific Function
- Mediates electroneutral potassium-chloride cotransport when activated by cell swelling. May contribute to cell volume homeostasis in single cells. May be involved in the regulation of basolateral C...
- Gene Name
- SLC12A4
- Uniprot ID
- Q9UP95
- Uniprot Name
- Solute carrier family 12 member 4
- Molecular Weight
- 120648.73 Da
References
- Jean-Xavier C, Pflieger JF, Liabeuf S, Vinay L: Inhibitory postsynaptic potentials in lumbar motoneurons remain depolarizing after neonatal spinal cord transection in the rat. J Neurophysiol. 2006 Nov;96(5):2274-81. Epub 2006 Jun 28. [Article]
- Reid KH, Guo SZ, Iyer VG: Agents which block potassium-chloride cotransport prevent sound-triggered seizures in post-ischemic audiogenic seizure-prone rats. Brain Res. 2000 May 2;864(1):134-7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Protein kinase binding
- Specific Function
- Mediates electroneutral potassium-chloride cotransport in mature neurons. Transport occurs under isotonic conditions, but is activated 20-fold by cell swelling. Important for Cl(-) homeostasis in n...
- Gene Name
- SLC12A5
- Uniprot ID
- Q9H2X9
- Uniprot Name
- Solute carrier family 12 member 5
- Molecular Weight
- 126182.49 Da
References
- Reid KH, Guo SZ, Iyer VG: Agents which block potassium-chloride cotransport prevent sound-triggered seizures in post-ischemic audiogenic seizure-prone rats. Brain Res. 2000 May 2;864(1):134-7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Pdz domain binding
- Specific Function
- Involved in the transport of chloride ions. May regulate bicarbonate secretion and salvage in epithelial cells by regulating the SLC4A7 transporter. Can inhibit the chloride channel activity of ANO...
- Gene Name
- CFTR
- Uniprot ID
- P13569
- Uniprot Name
- Cystic fibrosis transmembrane conductance regulator
- Molecular Weight
- 168139.895 Da
References
- Reddy MM, Quinton PM: Bumetanide blocks CFTR GCl in the native sweat duct. Am J Physiol. 1999 Jan;276(1 Pt 1):C231-7. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Prostaglandin-endoperoxide synthase activity
- Specific Function
- Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and...
- Gene Name
- PTGS2
- Uniprot ID
- P35354
- Uniprot Name
- Prostaglandin G/H synthase 2
- Molecular Weight
- 68995.625 Da
References
- Cheng HF, Wang JL, Zhang MZ, McKanna JA, Harris RC: Role of p38 in the regulation of renal cortical cyclooxygenase-2 expression by extracellular chloride. J Clin Invest. 2000 Sep;106(5):681-8. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Virus receptor activity
- Specific Function
- The hepatic sodium/bile acid uptake system exhibits broad substrate specificity and transports various non-bile acid organic compounds as well. It is strictly dependent on the extracellular presenc...
- Gene Name
- SLC10A1
- Uniprot ID
- Q14973
- Uniprot Name
- Sodium/bile acid cotransporter
- Molecular Weight
- 38118.64 Da
References
- Hagenbuch B, Stieger B, Foguet M, Lubbert H, Meier PJ: Functional expression cloning and characterization of the hepatocyte Na+/bile acid cotransport system. Proc Natl Acad Sci U S A. 1991 Dec 1;88(23):10629-33. [Article]
- Platte HD, Honscha W, Schuh K, Petzinger E: Functional characterization of the hepatic sodium-dependent taurocholate transporter stably transfected into an immortalized liver-derived cell line and V79 fibroblasts. Eur J Cell Biol. 1996 May;70(1):54-60. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- Curator comments
- Substrate activity was investigated in vitro.
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one ...
- Gene Name
- SLC22A6
- Uniprot ID
- Q4U2R8
- Uniprot Name
- Solute carrier family 22 member 6
- Molecular Weight
- 61815.78 Da
References
- Race JE, Grassl SM, Williams WJ, Holtzman EJ: Molecular cloning and characterization of two novel human renal organic anion transporters (hOAT1 and hOAT3). Biochem Biophys Res Commun. 1999 Feb 16;255(2):508-14. [Article]
- Uwai Y, Saito H, Hashimoto Y, Inui KI: Interaction and transport of thiazide diuretics, loop diuretics, and acetazolamide via rat renal organic anion transporter rOAT1. J Pharmacol Exp Ther. 2000 Oct;295(1):261-5. [Article]
- VanWert AL, Gionfriddo MR, Sweet DH: Organic anion transporters: discovery, pharmacology, regulation and roles in pathophysiology. Biopharm Drug Dispos. 2010 Jan;31(1):1-71. doi: 10.1002/bdd.693. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
- Gene Name
- SLC22A8
- Uniprot ID
- Q8TCC7
- Uniprot Name
- Solute carrier family 22 member 8
- Molecular Weight
- 59855.585 Da
References
- Cha SH, Sekine T, Fukushima JI, Kanai Y, Kobayashi Y, Goya T, Endou H: Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney. Mol Pharmacol. 2001 May;59(5):1277-86. [Article]
- Kusuhara H, Sekine T, Utsunomiya-Tate N, Tsuda M, Kojima R, Cha SH, Sugiyama Y, Kanai Y, Endou H: Molecular cloning and characterization of a new multispecific organic anion transporter from rat brain. J Biol Chem. 1999 May 7;274(19):13675-80. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates saturable uptake of estrone sulfate, dehydroepiandrosterone sulfate and related compounds.
- Gene Name
- SLC22A11
- Uniprot ID
- Q9NSA0
- Uniprot Name
- Solute carrier family 22 member 11
- Molecular Weight
- 59970.945 Da
References
- Cha SH, Sekine T, Kusuhara H, Yu E, Kim JY, Kim DK, Sugiyama Y, Kanai Y, Endou H: Molecular cloning and characterization of multispecific organic anion transporter 4 expressed in the placenta. J Biol Chem. 2000 Feb 11;275(6):4507-12. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates sodium-independent multispecific organic anion transport. Transport of prostaglandin E2, prostaglandin F2, tetracycline, bumetanide, estrone sulfate, glutarate, dehydroepiandrosterone sulf...
- Gene Name
- SLC22A7
- Uniprot ID
- Q9Y694
- Uniprot Name
- Solute carrier family 22 member 7
- Molecular Weight
- 60025.025 Da
References
- Sekine T, Cha SH, Tsuda M, Apiwattanakul N, Nakajima N, Kanai Y, Endou H: Identification of multispecific organic anion transporter 2 expressed predominantly in the liver. FEBS Lett. 1998 Jun 12;429(2):179-82. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
- Gene Name
- SLCO1A2
- Uniprot ID
- P46721
- Uniprot Name
- Solute carrier organic anion transporter family member 1A2
- Molecular Weight
- 74144.105 Da
References
- Horz JA, Honscha W, Petzinger E: Bumetanide is not transported by the Ntcp or by the oatp: evidence for a third organic anion transporter in rat liver cells. Biochim Biophys Acta. 1996 Apr 19;1300(2):114-8. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55