Identification

Name
Triamterene
Accession Number
DB00384  (APRD00079)
Type
Small Molecule
Groups
Approved
Description

A pteridine that is used as a mild diuretic.

Structure
Thumb
Synonyms
  • 6-phenylpteridine-2,4,7-triamine
  • Teridin
  • Triamteren
  • Triamterena
  • Triamtérène
  • Triamterene
  • Triamtereno
  • Triamterenum
External IDs
NSC-77625 / SK&F 8542 / SK&F-8542
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DyreniumCapsule50 mg/1OralConcordia Pharmaceuticals Inc.1999-10-01Not applicableUs
DyreniumCapsule100 mg/1OralPhysicians Total Care, Inc.2004-06-152011-06-30Us
DyreniumCapsule100 mg/1OralWell Spring Pharmaceutical Corporation1999-01-012020-01-31Us65197 0003 01 nlmimage10 2e45975c
DyreniumCapsule100 mg/1OralConcordia Pharmaceuticals Inc.1999-01-01Not applicableUs
DyreniumCapsule50 mg/1OralWell Spring Pharmaceutical Corporation1999-10-012019-12-31Us
DyreniumCapsule50 mg/1OralCarilion Materials Management1999-10-01Not applicableUs65197 0002 01 nlmimage10 3315999c
Dyrenium 100Tablet100 mgOralGlaxosmithkline Inc1992-12-312002-07-03Canada
Dyrenium 50Tablet50 mgOralGlaxosmithkline Inc1992-12-312002-07-03Canada
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Apo TriazideTriamterene (50 mg) + Hydrochlorothiazide (25 mg)TabletOralApotex Corporation1984-12-31Not applicableCanada
DyazideTriamterene (37.5 mg/1) + Hydrochlorothiazide (25 mg/1)CapsuleOralPhysicians Total Care, Inc.2003-09-092011-06-30Us
DyazideTriamterene (37.5 mg/1) + Hydrochlorothiazide (25 mg/1)CapsuleOralGlaxosmithkline Inc1994-03-302018-02-23Us
DyazideTriamterene (37.5 mg/1) + Hydrochlorothiazide (25 mg/1)CapsuleOralCardinal Health1994-03-30Not applicableUs00007 3650 22 nlmimage10 4c192669
DyazideTriamterene (37.5 mg/1) + Hydrochlorothiazide (25 mg/1)CapsuleOralMckesson Rxpak Inc1994-03-30Not applicableUs
DyazideTriamterene (37.5 mg/1) + Hydrochlorothiazide (25 mg/1)CapsuleOralGlaxosmithkline Inc1994-03-30Not applicableUs0007 365020180810 16125 1bkzpqu
Dyazide TabTriamterene (50 mg) + Hydrochlorothiazide (25 mg)TabletOralSmithkline Beecham Pharma Division Of Smithkline Beecham Inc1992-12-312001-03-05Canada
MaxzideTriamterene (75 mg/1) + Hydrochlorothiazide (50 mg/1)TabletOralPhysicians Total Care, Inc.1988-05-132012-06-30Us
MaxzideTriamterene (75 mg/1) + Hydrochlorothiazide (50 mg/1)TabletOralMylan Pharmaceuticals Inc.1988-05-13Not applicableUs
Maxzide-25Triamterene (37.5 mg/1) + Hydrochlorothiazide (25 mg/1)TabletOralPhysicians Total Care, Inc.1988-05-132012-06-30Us
International/Other Brands
Diuteren (Kotobuki Seiyaku) / Dyrenium / Dytac (Mercury) / Riyazine (Ciiphar) / Triteren (Kyoto Yakuhin) / Urinis (Ying Yuan)
Categories
UNII
WS821Z52LQ
CAS number
396-01-0
Weight
Average: 253.2626
Monoisotopic: 253.107593387
Chemical Formula
C12H11N7
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

Pharmacology

Indication

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.

Associated Conditions
Pharmacodynamics

Triamterene, a relatively weak, potassium-sparing diuretic and antihypertensive, is used in the management of hypokalemia. Triamterene is similar in action to amiloride but, unlike amiloride, increases the urinary excretion of magnesium.

Mechanism of action

Triamterene inhibits the epithelial sodium channels on principal cells in the late distal convoluted tubule and collecting tubule, which are responsible for 1-2% of total sodium reabsorption. As sodium reabsorption is inhibited, this increases the osmolarity in the nephron lumen and decreases the osmolarity of the interstitium. Since sodium concentration is the main driving force for water reabsorption, triamterene can achieve a modest amount of diuresis by decreasing the osmotic gradient necessary for water reabsorption from lumen to interstitium. Triamterene also has a potassium-sparing effect. Normally, the process of potassium excretion is driven by the electrochemical gradient produced by sodium reabsorption. As sodium is reabsorbed, it leaves a negative potential in the lumen, while producing a positive potential in the principal cell. This potential promotes potassium excretion through apical potassium channels. By inhibiting sodium reabsorption, triamterene also inhibits potassium excretion.

TargetActionsOrganism
AAmiloride-sensitive sodium channel subunit gamma
inhibitor
Human
AAmiloride-sensitive sodium channel subunit alpha
inhibitor
Human
AAmiloride-sensitive sodium channel subunit beta
inhibitor
Human
UAmiloride-sensitive sodium channel subunit delta
inhibitor
Human
Absorption

Rapidly absorbed, with somewhat less than 50% of the oral dose reaching the urine.

Volume of distribution
Not Available
Protein binding

55-67% (93% for the OH-TA-ester metabolite)

Metabolism

Triamterene is primarily metabolized to the sulfate conjugate of hydroxytriamterene. Both the plasma and urine levels of this metabolite greatly exceed triamterene levels.

Route of elimination
Not Available
Half life

255 minutes (188 minutes for OH-TA-ester metabolite) after IV administration.

Clearance
  • 4.5 l/min [total plasma clearance]
  • 0.22 l/kg [renal plasma clearance]
Toxicity

In the event of overdosage it can be theorized that electrolyte imbalance would be the major concern, with particular attention to possible hyperkalemia. Other symptoms that might be seen would be nausea and vomiting, other G.I. disturbances, and weakness. It is conceivable that some hypotension could occur. The oral LD50 in mice is 380 mg/kg.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Triamterene Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Triamterene.
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic AcidThe risk or severity of hyperkalemia can be increased when Triamterene is combined with 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
1-benzylimidazoleThe risk or severity of hypertension can be increased when Triamterene is combined with 1-benzylimidazole.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of hypertension can be increased when Triamterene is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of hypertension can be increased when Triamterene is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3-isobutyl-1-methyl-7H-xanthineThe serum concentration of 3-isobutyl-1-methyl-7H-xanthine can be increased when it is combined with Triamterene.
3,4-MethylenedioxyamphetamineThe risk or severity of hypertension can be increased when Triamterene is combined with 3,4-Methylenedioxyamphetamine.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of hypertension can be increased when Triamterene is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-MethoxyamphetamineThe risk or severity of hypertension can be increased when Triamterene is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamineThe risk or severity of hypertension can be increased when Triamterene is combined with 5-methoxy-N,N-dimethyltryptamine.
Food Interactions
Not Available

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
  1. 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. [PubMed:6628507]
External Links
Human Metabolome Database
HMDB0001940
KEGG Drug
D00386
PubChem Compound
5546
PubChem Substance
46507623
ChemSpider
5345
BindingDB
6644
ChEBI
9671
ChEMBL
CHEMBL585
Therapeutic Targets Database
DAP000575
PharmGKB
PA451752
IUPHAR
4329
Guide to Pharmacology
GtP Drug Page
HET
DX2
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Triamterene
ATC Codes
C03DB02 — Triamterene
AHFS Codes
  • 40:28.16 — Potassium-sparing Diuretics
PDB Entries
3jq7
MSDS
Download (73.5 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedNot AvailableCardiovascular Disease (CVD) / Death, Sudden,Cardiac / Heart Arrest / Heart Diseases / High Blood Pressure (Hypertension)1
3CompletedPreventionAtherosclerosis / Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Diabetes Mellitus (DM) / High Blood Pressure (Hypertension) / High Cholesterol / Type 2 Diabetes Mellitus1
4RecruitingTreatmentProteinuria1
Not AvailableUnknown StatusBasic ScienceDiabetic Nephropathies / High Blood Pressure (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
FormRouteStrength
CapsuleOral100 mg/1
CapsuleOral50 mg/1
TabletOral100 mg
TabletOral50 mg
TabletOral
CapsuleOral
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)316 °CPhysProp
water solubility48.2 mg/LNot Available
logP0.98HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.963 mg/mLALOGPS
logP1.21ALOGPS
logP1.11ChemAxon
logS-2.4ALOGPS
pKa (Strongest Acidic)15.88ChemAxon
pKa (Strongest Basic)3.11ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area129.62 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity75.13 m3·mol-1ChemAxon
Polarizability25.9 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.8735
Caco-2 permeable+0.7017
P-glycoprotein substrateNon-substrate0.6269
P-glycoprotein inhibitor INon-inhibitor0.8782
P-glycoprotein inhibitor IINon-inhibitor0.8814
Renal organic cation transporterNon-inhibitor0.8437
CYP450 2C9 substrateNon-substrate0.8949
CYP450 2D6 substrateNon-substrate0.8892
CYP450 3A4 substrateNon-substrate0.7542
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.831
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6161
Ames testNon AMES toxic0.8934
CarcinogenicityNon-carcinogens0.9092
BiodegradationNot ready biodegradable0.9959
Rat acute toxicity2.7706 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9604
hERG inhibition (predictor II)Non-inhibitor0.6829
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
GC-MS Spectrum - CI-BGC-MSsplash10-0udi-0090000000-c8bbcf103f5a3fdfebb5
MS/MS Spectrum - CI-B (Unknown) , PositiveLC-MS/MSsplash10-0udi-0090000000-c8bbcf103f5a3fdfebb5
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0udr-0090000000-007b38b2c4832f349909
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-000i-0590000000-b0551f41584c039101f6
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-00kf-0910000000-6428faa965a39a470ea5
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0udi-0090000000-c1e38db82ca2bfb168b7
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0udi-0090000000-e0b752d624dade8793ef
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0udi-0090000000-4c12cffcdf72d196b590
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0f79-0190000000-e63d14e64b8206d5c635
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0f79-0970000000-a69efa072a4b5fca0463
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0uxu-0910000000-f8ece9e1491b71df0c70
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0uxu-3900000000-946796a2530a51263ccd
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0f79-9600000000-59b671ef134dd8106331
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0gw0-9200000000-3451a9c6dc2b3f4b6e3b
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0udi-0190000000-425707e7729440a5bdb4
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0udi-0190000000-32f8b6872d5877d00316
1H NMR Spectrum1D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot Applicable

Taxonomy

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
Pteridine / Aminopyrazine / Aminopyrimidine / Monocyclic benzene moiety / Pyrazine / Pyrimidine / Benzenoid / Imidolactam / Heteroaromatic compound / Azacycle
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
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
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. 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. [PubMed:12827214]
  4. 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. [PubMed:8772124]
  5. 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. [PubMed:11509829]
Kind
Protein
Organism
Human
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
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. 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. [PubMed:8772124]
  4. 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. [PubMed:11509829]
  5. 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
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
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. 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. [PubMed:8772124]
  4. 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. [PubMed:11509829]
Kind
Protein
Organism
Human
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
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. 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. [PubMed:11509829]

Enzymes

Kind
Protein
Organism
Human
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
  1. 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]
  2. 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. [PubMed:16035375]

Drug created on June 13, 2005 07:24 / Updated on December 18, 2018 09:07