Identification
- Summary
Triamterene is a potassium-sparing diuretic used in the treatment of edema and in the management of hypertension.
- Brand Names
- Dyrenium, Maxzide
- Generic Name
- Triamterene
- DrugBank Accession Number
- DB00384
- Background
Triamterene (2,4,7-triamino-6-phenylpteridine) is a potassium-sparing diuretic that is used in the management of hypertension. It works by promoting the excretion of sodium ions and water while decreasing the potassium excretion in the distal part of the nephron in the kidneys by working on the lumenal side.2 Since it acts on the distal nephron where only a small fraction of sodium ion reabsorption occurs, triamterene is reported to have limited diuretic efficacy.11 Due to its effects on increased serum potassium levels, triamterene is associated with a risk of producing hyperkalemia. Triamterene is a weak antagonist of folic acid, and a photosensitizing drug.12
Triamterene was approved by the Food and Drug Administration in the U.S. in 1964.12 Currently, triamterene is used in the treatment of edema associated with various conditions as monotherapy and is approved for use with other diuretics to enhance diuretic and potassium-sparing effects.15 It is also found in a combination product with hydrochlorothiazide that is used for the management of hypertension or treatment of edema in patients who develop hypokalemia on hydrochlorothiazide alone.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Triamterene (DB00384)
- Weight
- Average: 253.2626
Monoisotopic: 253.107593387 - Chemical Formula
- C12H11N7
- Synonyms
- 6-phenylpteridine-2,4,7-triamine
- Teridin
- Triamteren
- Triamterena
- Triamtérène
- Triamterene
- Triamtereno
- Triamterenum
- External IDs
- NSC-77625
- SK&F 8542
- SK&F-8542
Pharmacology
- Indication
Triamterene is indicated for the treatment of edema associated with congestive heart failure, cirrhosis of the liver, and the nephrotic syndrome; also in steroid-induced edema, idiopathic edema, and edema due to secondary hyperaldosteronism.15
Triamterene in combination with hydrochlorothiazide is indicated for the managment of hypertension or treatment of edema in patients who develop hypokalemia following hydrochlorothiazide monotherapy, and in patients who require thiazide diuretic and in whom the development of hypokalemia cannot be risked.13 Triamterene allows the maintenance of potassium balance when given in combination with loop diuretics and thiazides.11
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat Edema Combination Product in combination with: Hydrochlorothiazide (DB00999) •••••••••••• ••••••••••• •••••• •• •••••••• ••••••••• •••••••• •••••• Treatment of Edema •••••••••••• •••••••• •••••• Treatment of Edema •••••••••••• •••••••• •••••• Treatment of Edema •••••••••••• •••••••• •••••• Treatment of Edema caused by secondary hyperaldosteronism •••••••••••• •••••••• •••••• - Contraindications & Blackbox Warnings
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Triamterene, a relatively weak, potassium-sparing diuretic and antihypertensive, is used in the management of hypertension and edema. It primarily works on the distal nephron in the kidneys; it acts from the late distal tubule to the collecting duct to inhibit Na+ reabsorption and decreasing K+ excretion.11 As triamterene tends to conserve potassium more strongly than promoting Na+ excretion, it can cause an increase in serum potassium, which may result in hyperkalemia potentially associated with cardiac irregularities.15 In healthy volunteers administered with oral triamterene, there was an increase in the renal clearnace of sodium and magnesium, and a decrease in the clearance of uric acid and creatinine5 due to its effect of reducing glomerular filtration renal plasma flow.13 Triamterene does not affect calcium excretion.13 In clinical trials, the use of triamterene in combination with hydrochlorothiazide resulted an enhanced blood pressure-lowering effects of hydrochlorothiazide.7
- Mechanism of action
Triamterene inhibits the epithelial sodium channels (ENaC) located on the lumenal side in the late distal convoluted tubule and collecting tubule 6, which are transmembrane channels that normally promote sodium uptake and potassium secretion.7 In the late distal tubule to the collecting duct, sodium ions are actively reabsorbed via ENaC on the luminal membrane and are extruded out of the cell into the peritubular medium by a sodium-potassium exchange pump, the Na-K-ATPase,8 with water following passively.11 Triamterene exerts a diuretic effect on the distal renal tubule to inhibit the reabsorption of sodium ions in exchange for potassium and hydrogen ions and its natriuretic activity is limited by the amount of sodium reaching its site of action.13 Its action is antagonistic to that of adrenal mineralocorticoids, such as aldosterone, but it is not an inhibitor or antagonist of aldosterone.15 Triamterene maintains or increases sodium excretion, thereby increasing the excretion of water, and reducing the excess loss of potassium, hydrogen, and chloride ions by inhibiting the distal tubular exchange mechanism.13 Due to its diuretic effect, triamterene rapidly and reversibly reduces the lumen-negative transepithelial potential difference by almost completely abolishing Na+ conductance without altering K+ conductance.3 This reduces the driving force for potassium movement into the tubular lumen and thus decreases potassium excretion. 8 Triamterene is similar in action to amiloride but, unlike amiloride, increases the urinary excretion of magnesium.5
Target Actions Organism AAmiloride-sensitive sodium channel subunit gamma inhibitorHumans AAmiloride-sensitive sodium channel subunit alpha inhibitorHumans AAmiloride-sensitive sodium channel subunit beta inhibitorHumans UAmiloride-sensitive sodium channel subunit delta inhibitorHumans - Absorption
Triamterene is shown to be rapidly absorbed in the gastrointestinal tract 15,11 Its onset of action achiveved within 2 to 4 hours after oral ingestion 15 and its duration of action is 12-16 hours.11 It is reported that the diuretic effect of triamterene may not be observed for several days after administration.15 In a pharmacokinetic study, the oral bioavailability of triamterene was determined to be 52%.4 Following administration of a single oral dose to fasted healthy male volunteers, the mean AUC of triamterene was about 148.7 ng*hr/mL 13 and the mean peak plasma concentrations (Cmax) were 46.4 ng/mL reached at 1.1 hour after administration.13 In a limited study, administration of triamterene in combination with hydrochlorothiazide resulted in an increased bioavailability of triamterene by about 67% and a delay of up to 2 hours in the absorption of the drug.13 It is advised that triamterene is administered after meals; in a limited study, combination use of triamterene and hydrochlorothiazide with the consumption of a high-fat meal resulted in an increase in the mean bioavailability and peak serum concentrations of triamterene and its active sulfate metabolite, as well as a delay of up to 2 hours in the absorption of the active constituents.13
- Volume of distribution
In a pharmacolinetic study involving healthy volunteers receiving triamterene intravenously, the volumes of distribution of the central compartment of triamterene and its hydroxylated ester metabolite were 1.49 L/kg and 0.11 L/kg, respectively.1 Triamterene was found to cross the placental barrier and appear in the cord blood of animals.15
- Protein binding
67% bound to proteins. 15
- Metabolism
Triamterene undergoes phase I metabolism involving hydroxylation, via CYP1A2 activity, to form 4'-hydroxytriamterene. 4'-Hydroxytriamterene is further transformed in phase II metabolism mediated by cytosolic sulfotransferases to form the major metabolite, 4′-hydroxytriamterene sulfate, which retains a diuretic activity. 10,12 Both the plasma and urine levels of this metabolite greatly exceed triamterene levels 15 while the renal clearance of the sulfate conjugate was les than that of triamterene; this low renal clearance of the sulfate conjugate as compared with triamterene may be explained by the low unbound fraction of the metabolite in plasma.9
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- Route of elimination
Triamterene and its metabolites are excreted by the kidney by filtration and tubular secretion.14 Upon oral ingestion, somewhat less than 50% of the oral dose reaches the urine.15 About 20% of an oral dose appears unchanged in the urine, 70% as the sulphate ester of hydroxytriamterene and 10% as free hydroxytriamterene and triamterene glucuronide.14
- Half-life
The half-life of the drug in plasma ranges from 1.5 to 2 hours.14 In a pharmacokinetic study involving healthy volunteers, the terminal half-lives for triamterene and 4′-hydroxytriamterene sulfate were 255 ± 42 and 188 ± 70 minutes, respectively, after intravenous infusion of the parent drug.1,12
- Clearance
The total plasma clearance was 4.5 l/min and renal plasma clearance was 0.22 l/kg following intravenous administration of triamterene in healthy volunteers.1
- Adverse Effects
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Acute oral LD50 of triamterene in rats is 400 mg/kg and 285-380 mg/kg in mice.15,MSDS There has been a case of reversible acute renal failure following ingestion of 50 combination pills containing 50 mg triamterene and 25 mg hydrochlorothiazide. Symptoms of overdose, such as nausea, vomiting, gastrointestinal disturbances, weakness, and hypotension, are related to electrolyte imbalances, such as hyperkalemia. As there is no specific antidote, emesis and gastric lavage should be use to induce immediate evacuation of the stomach and careful evaluation of the electrolyte pattern and fluid balance should be made. Dialysis may be somewhat effective in case of an overdosage.15
In a carciongenicity study in male and female mice administered with triamterene at the highst dosage level, there was an increased incidence of hepatocellular neoplasia, primarily adenomas. However, this was not a dose-dependent phenomenon and there was no statistically significant difference from control incidence at any dose level. In bacterial assays, there was no demonstrated mutagenic potential of triamterene. In in vitro assay using Chinese hamster ovary (CHO) cells with or without metabolic activation, there were no chromosomal aberrations. Studies evaluating the effects of triamterene on reproductive system or fertility have not been conducted. It is advised that the use of triamterene is avoided during pregnancy. As triamterene has been detected in human breast milk, triamterene should be used when nursing is ceased.15
- Pathways
Pathway Category Triamterene 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 Triamterene 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 Triamterene is combined with Abaloparatide. Abametapir The serum concentration of Triamterene can be increased when it is combined with Abametapir. Abatacept The metabolism of Triamterene can be increased when combined with Abatacept. Abiraterone The serum concentration of Triamterene can be increased when it is combined with Abiraterone. - Food Interactions
- Avoid potassium-containing products. The risk of hyperkalemia can be increased with the intake of potassium supplementation or potassium-rich foods.
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
- Diuteren (Kotobuki Seiyaku) / Dytac (Mercury) / Riyazine (Ciiphar) / Triteren (Kyoto Yakuhin) / Urinis (Ying Yuan)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Dyrenium Capsule 100 mg/1 Oral Concordia Pharmaceuticals Inc. 1999-01-01 Not applicable US 
Dyrenium Capsule 100 mg/1 Oral Physicians Total Care, Inc. 2004-06-15 2011-06-30 US Dyrenium Capsule 50 mg/1 Oral Concordia Pharmaceuticals Inc. 1999-10-01 Not applicable US Dyrenium Capsule 100 mg/1 Oral Well Spring Pharmaceutical Corporation 1999-01-01 2020-01-31 US 
Dyrenium Capsule 50 mg/1 Oral Carilion Materials Management 1999-10-01 Not applicable US 
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Triamterene Capsule 50 mg/1 Oral TruPharma LLC 2018-12-12 Not applicable US Triamterene Capsule 50 mg/1 Oral Prasco Laboratories 2019-08-13 Not applicable US Triamterene Capsule 100 mg/1 Oral Prasco Laboratories 2019-08-13 Not applicable US Triamterene Capsule 100 mg/1 Oral TruPharma LLC 2018-12-12 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Apo Triazide Triamterene (50 mg) + Hydrochlorothiazide (25 mg) Tablet Oral Apotex Corporation 1984-12-31 Not applicable Canada 
APO-TRIAZIDE TABLET Triamterene (50 mg) + Hydrochlorothiazide (25 mg) Tablet Oral PHARMAFORTE SINGAPORE PTE LTD 1991-11-09 Not applicable Singapore 
DOCITEREN Triamterene (25 mg/1) + Hydrochlorothiazide (12.5 mg/1) + Propranolol hydrochloride (80 mg/1) Tablet 2006-07-01 Not applicable Germany 
Dyazide Triamterene (37.5 mg/1) + Hydrochlorothiazide (25 mg/1) Capsule Oral GlaxoSmithKline LLC 1994-03-30 2021-09-30 US 
Dyazide Triamterene (37.5 mg/1) + Hydrochlorothiazide (25 mg/1) Capsule Oral Physicians Total Care, Inc. 2003-09-09 2011-06-30 US
Categories
- ATC Codes
- C03DB02 — Triamterene
- Drug Categories
- Agents causing hyperkalemia
- Cardiovascular Agents
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 Substrates
- Decreased Renal K+ Excretion
- Diuretics
- Drugs causing inadvertant photosensitivity
- Epithelial Sodium Channel Blockers
- Heterocyclic Compounds, Fused-Ring
- Hypotensive Agents
- Increased Diuresis
- Membrane Transport Modulators
- Natriuretic Agents
- Nephrotoxic agents
- Photosensitizing Agents
- Potassium-Sparing Diuretics
- Pteridines
- Sodium Channel Blockers
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as pteridines and derivatives. These are polycyclic aromatic compounds containing a pteridine moiety, which consists of a pyrimidine fused to a pyrazine ring to form pyrimido(4,5-b)pyrazine.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Pteridines and derivatives
- Sub Class
- Not Available
- Direct Parent
- Pteridines and derivatives
- Alternative Parents
- Aminopyrimidines and derivatives / Aminopyrazines / Imidolactams / Benzene and substituted derivatives / Heteroaromatic compounds / Azacyclic compounds / Primary amines / Organopnictogen compounds / Hydrocarbon derivatives
- Substituents
- Amine / Aminopyrazine / Aminopyrimidine / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Heteroaromatic compound / Hydrocarbon derivative / Imidolactam / Monocyclic benzene moiety
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- WS821Z52LQ
- CAS number
- 396-01-0
- InChI Key
- FNYLWPVRPXGIIP-UHFFFAOYSA-N
- InChI
- InChI=1S/C12H11N7/c13-9-7(6-4-2-1-3-5-6)16-8-10(14)18-12(15)19-11(8)17-9/h1-5H,(H6,13,14,15,17,18,19)
- IUPAC Name
- 6-phenylpteridine-2,4,7-triamine
- SMILES
- NC1=NC(N)=C2N=C(C(N)=NC2=N1)C1=CC=CC=C1
References
- Synthesis Reference
Frederic J. Nugent, John K. C. Yen, "Process for preparing the combination products of triamterene and hydrochlorothiazide." U.S. Patent US4804540, issued July, 1987.
US4804540- General References
- Gilfrich HJ, Kremer G, Mohrke W, Mutschler E, Volger KD: Pharmacokinetics of triamterene after i.v. administration to man: determination of bioavailability. Eur J Clin Pharmacol. 1983;25(2):237-41. [Article]
- BABA WI, TUDHOPE GR, WILSON GM: Triamterene, a new diuretic drug. I. Studies in normal men and in adrenalectomized rats. Br Med J. 1962 Sep 22;2(5307):756-60. doi: 10.1136/bmj.2.5307.756. [Article]
- Knauf H, Wais U, Lubcke R, Albiez G: On the mechanism of action of triamterene: effects on transport of Na+, K+, and H+/HCO3- -ions. Eur J Clin Invest. 1976 Jan 30;6(1):43-50. [Article]
- Mutschler E, Gilfrich HJ, Knauf H, Mohrke W, Volger KD: Pharmacokinetics of triamterene. Clin Exp Hypertens A. 1983;5(2):249-69. [Article]
- Walker BR, Hoppe RC, Alexander F: Effect of triamterene on the renal clearance of calcium, magnesium, phosphate, and uric acid in man. Clin Pharmacol Ther. 1972 Mar-Apr;13(2):245-50. [Article]
- Knauf H, Wais U, Albiez G, Lubcke R: [Inhibition of the exchange of Na+ for K+ and and H+ by triamterene (in epithelia)(author's transl)]. Arzneimittelforschung. 1976 Apr;26(4):484-6. [Article]
- Tu W, Decker BS, He Z, Erdel BL, Eckert GJ, Hellman RN, Murray MD, Oates JA, Pratt JH: Triamterene Enhances the Blood Pressure Lowering Effect of Hydrochlorothiazide in Patients with Hypertension. J Gen Intern Med. 2016 Jan;31(1):30-6. doi: 10.1007/s11606-015-3469-1. [Article]
- Horisberger JD, Giebisch G: Potassium-sparing diuretics. Ren Physiol. 1987;10(3-4):198-220. [Article]
- Hasegawa J, Lin ET, Williams RL, Sorgel F, Benet LZ: Pharmacokinetics of triamterene and its metabolite in man. J Pharmacokinet Biopharm. 1982 Oct;10(5):507-23. [Article]
- Fuhr U, Kober S, Zaigler M, Mutschler E, Spahn-Langguth H: Rate-limiting biotransformation of triamterene is mediated by CYP1A2. Int J Clin Pharmacol Ther. 2005 Jul;43(7):327-34. [Article]
- 28. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 352-353, 356). Edinburgh: Elsevier/Churchill Livingstone. [ISBN:978-0-7020-3471-8]
- Triamterene - International Agency for Research on Cancer (IARC) Monographs [Link]
- DYAZIDE (hydrochlorothiazide and triamterene) - FDA Label [Link]
- PRO-TRIAZIDE (Triamterene 50 mg and Hydrochlorothiazide 25 mg) - Product Monograph [Link]
- DailyMed Label: DYRENIUM (triamterene) oral capsules [Link]
- External Links
- Human Metabolome Database
- HMDB0001940
- KEGG Drug
- D00386
- PubChem Compound
- 5546
- PubChem Substance
- 46507623
- ChemSpider
- 5345
- BindingDB
- 6644
- 10763
- ChEBI
- 9671
- ChEMBL
- CHEMBL585
- ZINC
- ZINC000000120286
- Therapeutic Targets Database
- DAP000575
- PharmGKB
- PA451752
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- DX2
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Triamterene
- PDB Entries
- 3jq7
- MSDS
- Download (73.5 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 Unknown Status Treatment Proteinuria 1 3 Completed Not Available Cardiac Arrest / Cardiovascular Disease (CVD) / Hypertension / Sudden Cardiac Death 1 3 Completed Prevention Atherosclerosis / Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Diabetes Mellitus / High Cholesterol / Hypertension / Type 2 Diabetes Mellitus 1 Not Available Active Not Recruiting Not Available Hypertension 1 Not Available Completed Not Available Coronavirus Disease 2019 (COVID‑19) / COVID / Hypertension 1
Pharmacoeconomics
- Manufacturers
- Wellspring pharmaceutical corp
- Packagers
- Advanced Pharmaceutical Services Inc.
- Amerisource Health Services Corp.
- Apotex Inc.
- Apotheca Inc.
- A-S Medication Solutions LLC
- Atlantic Biologicals Corporation
- Barr Pharmaceuticals
- Bryant Ranch Prepack
- Cardinal Health
- Central Texas Community Health Centers
- Comprehensive Consultant Services Inc.
- Corepharma LLC
- Dept Health Central Pharmacy
- DHHS Program Support Center Supply Service Center
- Direct Dispensing Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Duramed
- GlaxoSmithKline Inc.
- Golden State Medical Supply Inc.
- Group Health Cooperative
- H.J. Harkins Co. Inc.
- Heartland Repack Services LLC
- Ivax Pharmaceuticals
- Kaiser Foundation Hospital
- Liberty Pharmaceuticals
- Major Pharmaceuticals
- Medvantx Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Neuman Distributors Inc.
- Nucare Pharmaceuticals Inc.
- Palmetto Pharmaceuticals Inc.
- PCA LLC
- PD-Rx Pharmaceuticals Inc.
- Pharmaceutical Utilization Management Program VA Inc.
- Pharmacy Service Center
- Physicians Total Care Inc.
- Pliva Inc.
- Preferred Pharmaceuticals Inc.
- Prepackage Specialists
- Prepak Systems Inc.
- Qualitest
- Rebel Distributors Corp.
- Remedy Repack
- Resource Optimization and Innovation LLC
- Sandhills Packaging Inc.
- Sandoz
- Southwood Pharmaceuticals
- Stat Scripts LLC
- Tya Pharmaceuticals
- UDL Laboratories
- Va Cmop Dallas
- Vangard Labs Inc.
- Watson Pharmaceuticals
- Wellspring Pharmaceutical
- Dosage Forms
Form Route Strength Tablet Capsule Oral 100 mg/1 Capsule Oral 50 mg/1 Tablet Oral 100 mg Tablet Oral 50 mg Tablet, film coated Oral Capsule, liquid filled Oral Capsule Oral Tablet Oral - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 316 °C PhysProp water solubility Very slightly soluble in water (<0.1%) IARC monograph, DYAZIDE (hydrochlorothiazide and triamterene) Label logP 0.98 HANSCH,C ET AL. (1995) - Predicted Properties
Property Value Source Water Solubility 0.963 mg/mL ALOGPS logP 1.21 ALOGPS logP 1.11 Chemaxon logS -2.4 ALOGPS pKa (Strongest Acidic) 15.88 Chemaxon pKa (Strongest Basic) 1.86 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 7 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 129.62 Å2 Chemaxon Rotatable Bond Count 1 Chemaxon Refractivity 75.13 m3·mol-1 Chemaxon Polarizability 25.9 Å3 Chemaxon Number of Rings 3 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 + 1.0 Blood Brain Barrier + 0.8735 Caco-2 permeable + 0.7017 P-glycoprotein substrate Non-substrate 0.6269 P-glycoprotein inhibitor I Non-inhibitor 0.8782 P-glycoprotein inhibitor II Non-inhibitor 0.8814 Renal organic cation transporter Non-inhibitor 0.8437 CYP450 2C9 substrate Non-substrate 0.8949 CYP450 2D6 substrate Non-substrate 0.8892 CYP450 3A4 substrate Non-substrate 0.7542 CYP450 1A2 substrate Inhibitor 0.9107 CYP450 2C9 inhibitor Non-inhibitor 0.907 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.831 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6161 Ames test Non AMES toxic 0.8934 Carcinogenicity Non-carcinogens 0.9092 Biodegradation Not ready biodegradable 0.9959 Rat acute toxicity 2.7706 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9604 hERG inhibition (predictor II) Non-inhibitor 0.6829
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 167.3285169 predictedDarkChem Lite v0.1.0 [M-H]- 167.0904169 predictedDarkChem Lite v0.1.0 [M-H]- 166.6125169 predictedDarkChem Lite v0.1.0 [M-H]- 155.81523 predictedDeepCCS 1.0 (2019) [M+H]+ 166.5691169 predictedDarkChem Lite v0.1.0 [M+H]+ 166.7296169 predictedDarkChem Lite v0.1.0 [M+H]+ 167.0409169 predictedDarkChem Lite v0.1.0 [M+H]+ 158.2108 predictedDeepCCS 1.0 (2019) [M+Na]+ 167.1691169 predictedDarkChem Lite v0.1.0 [M+Na]+ 177.5534834 predictedDarkChem Lite v0.1.0 [M+Na]+ 167.4868169 predictedDarkChem Lite v0.1.0 [M+Na]+ 164.21397 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Ww domain binding
- Specific Function
- Sodium permeable non-voltage-sensitive ion channel inhibited by the diuretic amiloride. Mediates the electrodiffusion of the luminal sodium (and water, which follows osmotically) through the apical...
- Gene Name
- SCNN1G
- Uniprot ID
- P51170
- Uniprot Name
- Amiloride-sensitive sodium channel subunit gamma
- Molecular Weight
- 74269.62 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Hiraoka Y, Taniguchi T, Tanaka T, Okada K, Kanamaru H, Muramatsu I: Pharmacological characterization of unique prazosin-binding sites in human kidney. Naunyn Schmiedebergs Arch Pharmacol. 2003 Jul;368(1):49-56. Epub 2003 Jun 25. [Article]
- Busch AE, Suessbrich H, Kunzelmann K, Hipper A, Greger R, Waldegger S, Mutschler E, Lindemann B, Lang F: Blockade of epithelial Na+ channels by triamterenes - underlying mechanisms and molecular basis. Pflugers Arch. 1996 Sep;432(5):760-6. [Article]
- Wagner CA, Ott M, Klingel K, Beck S, Melzig J, Friedrich B, Wild KN, Broer S, Moschen I, Albers A, Waldegger S, Tummler B, Egan ME, Geibel JP, Kandolf R, Lang F: Effects of the serine/threonine kinase SGK1 on the epithelial Na(+) channel (ENaC) and CFTR: implications for cystic fibrosis. Cell Physiol Biochem. 2001;11(4):209-18. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Ww domain binding
- Specific Function
- Sodium permeable non-voltage-sensitive ion channel inhibited by the diuretic amiloride. Mediates the electrodiffusion of the luminal sodium (and water, which follows osmotically) through the apical...
- Gene Name
- SCNN1A
- Uniprot ID
- P37088
- Uniprot Name
- Amiloride-sensitive sodium channel subunit alpha
- Molecular Weight
- 75703.08 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Busch AE, Suessbrich H, Kunzelmann K, Hipper A, Greger R, Waldegger S, Mutschler E, Lindemann B, Lang F: Blockade of epithelial Na+ channels by triamterenes - underlying mechanisms and molecular basis. Pflugers Arch. 1996 Sep;432(5):760-6. [Article]
- Wagner CA, Ott M, Klingel K, Beck S, Melzig J, Friedrich B, Wild KN, Broer S, Moschen I, Albers A, Waldegger S, Tummler B, Egan ME, Geibel JP, Kandolf R, Lang F: Effects of the serine/threonine kinase SGK1 on the epithelial Na(+) channel (ENaC) and CFTR: implications for cystic fibrosis. Cell Physiol Biochem. 2001;11(4):209-18. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Ww domain binding
- Specific Function
- Sodium permeable non-voltage-sensitive ion channel inhibited by the diuretic amiloride. Mediates the electrodiffusion of the luminal sodium (and water, which follows osmotically) through the apical...
- Gene Name
- SCNN1B
- Uniprot ID
- P51168
- Uniprot Name
- Amiloride-sensitive sodium channel subunit beta
- Molecular Weight
- 72658.485 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Busch AE, Suessbrich H, Kunzelmann K, Hipper A, Greger R, Waldegger S, Mutschler E, Lindemann B, Lang F: Blockade of epithelial Na+ channels by triamterenes - underlying mechanisms and molecular basis. Pflugers Arch. 1996 Sep;432(5):760-6. [Article]
- Wagner CA, Ott M, Klingel K, Beck S, Melzig J, Friedrich B, Wild KN, Broer S, Moschen I, Albers A, Waldegger S, Tummler B, Egan ME, Geibel JP, Kandolf R, Lang F: Effects of the serine/threonine kinase SGK1 on the epithelial Na(+) channel (ENaC) and CFTR: implications for cystic fibrosis. Cell Physiol Biochem. 2001;11(4):209-18. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Ligand-gated sodium channel activity
- Specific Function
- Sodium permeable non-voltage-sensitive ion channel inhibited by the diuretic amiloride. Mediates the electrodiffusion of the luminal sodium (and water, which follows osmotically) through the apical...
- Gene Name
- SCNN1D
- Uniprot ID
- P51172
- Uniprot Name
- Amiloride-sensitive sodium channel subunit delta
- Molecular Weight
- 70214.195 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Wagner CA, Ott M, Klingel K, Beck S, Melzig J, Friedrich B, Wild KN, Broer S, Moschen I, Albers A, Waldegger S, Tummler B, Egan ME, Geibel JP, Kandolf R, Lang F: Effects of the serine/threonine kinase SGK1 on the epithelial Na(+) channel (ENaC) and CFTR: implications for cystic fibrosis. Cell Physiol Biochem. 2001;11(4):209-18. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- Curator comments
- Data supported only by in vitro studies.
- 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
- Fuhr U, Kober S, Zaigler M, Mutschler E, Spahn-Langguth H: Rate-limiting biotransformation of triamterene is mediated by CYP1A2. Int J Clin Pharmacol Ther. 2005 Jul;43(7):327-34. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55