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Identification
NameAmiloride
Accession NumberDB00594  (APRD00790, EXPT00514)
TypeSmall Molecule
GroupsApproved
DescriptionA pyrazine compound inhibiting sodium reabsorption through sodium channels in renal epithelial cells. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with diuretics to spare potassium loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705)
Structure
Thumb
Synonyms
3,5-Diamino-N-carbamimidoyl-6-chloropyrazine-2-carboxamide
Amilorid
Amilorida
Amiloridum
Amipramidin
Amipramidine
Amyloride
N-amidino-3,5-diamino-6-chloropyrazinecarboxamide
External Identifiers
  • MK 870
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Amiloride Hydrochloridetablet5 mg/1oralPhysicians Total Care, Inc.2005-01-28Not applicableUs
Amiloride Hydrochloride Tablets, USPtablet5 mgoralOrbus Pharma IncNot applicableNot applicableCanada
Amiloride Hydrocloridetablet5 mg/1oralPaddock Laboratories, LLC2009-04-06Not applicableUs
Midamortablet5.0 mgoralAa Pharma Inc2004-06-18Not applicableCanada
Midamor Tablets 5mgtablet5 mgoralOrbus Pharma Inc1981-12-312010-06-16Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Amiloride Hydrochloridetablet5 mg/1oralCarilion Materials Management1986-01-22Not applicableUs
Amiloride Hydrochloridetablet5 mg/1oralAv Kare, Inc.2012-03-28Not applicableUs
Amiloride Hydrochloridetablet5 mg/1oralZydus Pharmaceuticals (USA) Inc.2015-09-14Not applicableUs
Amiloride Hydrochloridetablet5 mg/1oralAv Pak2013-01-28Not applicableUs
Amiloride Hydrochloridetablet5 mg/1oralPar Pharmaceutical Inc.1986-01-22Not applicableUs
Amiloride Hydrochloridetablet5 mg/1oralRising Pharmaceuticals, Inc2009-05-01Not applicableUs
Amiloride Hydrochloridetablet5 mg/1oralGolden State Medical Supply, Inc.2015-08-31Not applicableUs
Amiloride Hydrochloridetablet5 mg/1oralCadila Healthcare Limited2015-09-14Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ArumilSharp & Dohme
KalurilAlphapharm
ModamideMerck
ModureticMerck
Brand mixtures
NameLabellerIngredients
Alti-amiloride HctzAltimed Pharma Inc.
Ami-hydro TabPro Doc Limitee
Amiloride Hydrochloride and HydrochlorothiazideMylan Pharmaceuticals Inc.
Apo-amilzide TabApotex Inc
ModuretPrempharm Inc
Mylan-amilazideMylan Pharmaceuticals Ulc
NovamilorTeva Canada Limited
Nu-amilzide 5/50 Mg TabNu Pharm Inc
Penta-amiloride Hctz TabletsPentapharm Ltd.
Riva-amilzide 5/50 mgLaboratoire Riva Inc
Salts
Name/CASStructureProperties
Amiloride hydrochloride
2016-88-8
Thumb
  • InChI Key: ACHKKGDWZVCSNH-UHFFFAOYSA-N
  • Monoisotopic Mass: 265.0245633
  • Average Mass: 266.09
DBSALT001807
Amiloride hydrochloride dihydrate
17440-83-4
Thumb
  • InChI Key: LTKVFMLMEYCWMK-UHFFFAOYSA-N
  • Monoisotopic Mass: 301.045692731
  • Average Mass: 302.119
DBSALT000270
Categories
UNII7DZO8EB0Z3
CAS number2609-46-3
WeightAverage: 229.627
Monoisotopic: 229.04788562
Chemical FormulaC6H8ClN7O
InChI KeyInChIKey=XSDQTOBWRPYKKA-UHFFFAOYSA-N
InChI
InChI=1S/C6H8ClN7O/c7-2-4(9)13-3(8)1(12-2)5(15)14-6(10)11/h(H4,8,9,13)(H4,10,11,14,15)
IUPAC Name
3,5-diamino-6-chloro-N-(diaminomethylidene)pyrazine-2-carboxamide
SMILES
NC(N)=NC(=O)C1=C(N)N=C(N)C(Cl)=N1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as pyrazinecarboxamides. These are compounds containing a pyrazine ring which bears a carboxamide.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassDiazines
Sub ClassPyrazines
Direct ParentPyrazinecarboxamides
Alternative Parents
Substituents
  • Pyrazinecarboxamide
  • Aminopyrazine
  • Acylguanidine
  • Imidolactam
  • Primary aromatic amine
  • Aryl halide
  • Aryl chloride
  • Heteroaromatic compound
  • Vinylogous amide
  • Guanidine
  • Carboxamide group
  • Azacycle
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Carboximidamide
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor use as adjunctive treatment with thiazide diuretics or other kaliuretic-diuretic agents in congestive heart failure or hypertension.
PharmacodynamicsAmiloride, an antikaliuretic-diuretic agent, is a pyrazine-carbonyl-guanidine that is unrelated chemically to other known antikaliuretic or diuretic agents. It is an antihypertensive, potassium-sparing diuretic that was first approved for use in 1967 and helps to treat hypertension and congestive heart failure. The drug is often used in conjunction with thiazide or loop diuretics. Due to its potassium-sparing capacities, hyperkalemia (high blood potassium levels) are occasionally observed in patients taking amiloride. The risk is high in concurrent use of ACE inhibitors or spironolactone. Patients are also advised not to use potassium-containing salt replacements.
Mechanism of actionAmiloride works by inhibiting sodium reabsorption in the distal convoluted tubules and collecting ducts in the kidneys by binding to the amiloride-sensitive sodium channels. This promotes the loss of sodium and water from the body, but without depleting potassium. Amiloride exerts its potassium sparing effect through the inhibition of sodium reabsorption at the distal convoluted tubule, cortical collecting tubule and collecting duct; this decreases the net negative potential of the tubular lumen and reduces both potassium and hydrogen secretion and their subsequent excretion. Amiloride is not an aldosterone antagonist and its effects are seen even in the absence of aldosterone.
Related Articles
AbsorptionReadily absorbed following oral administration.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Amiloride is not metabolized by the liver but is excreted unchanged by the kidneys.

Route of eliminationAmiloride HCl is not metabolized by the liver but is excreted unchanged by the kidneys. About 50 percent of a 20 mg dose of amiloride HCl is excreted in the urine and 40 percent in the stool within 72 hours.
Half lifePlasma half-life varies from 6 to 9 hours.
ClearanceNot Available
ToxicityNo data are available in regard to overdosage in humans. The oral LD50 of amiloride hydrochloride (calculated as the base) is 56 mg/kg in mice and 36 to 85 mg/kg in rats, depending on the strain. The most likely signs and symptoms to be expected with overdosage are dehydration and electrolyte imbalance.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Amiloride Action PathwayDrug actionSMP00133
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9408
Blood Brain Barrier+0.7193
Caco-2 permeable-0.8957
P-glycoprotein substrateNon-substrate0.7207
P-glycoprotein inhibitor INon-inhibitor0.9282
P-glycoprotein inhibitor IINon-inhibitor0.9677
Renal organic cation transporterNon-inhibitor0.8122
CYP450 2C9 substrateNon-substrate0.8253
CYP450 2D6 substrateNon-substrate0.8778
CYP450 3A4 substrateNon-substrate0.6687
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9577
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9295
CYP450 3A4 inhibitorNon-inhibitor0.9733
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9605
Ames testAMES toxic0.9107
CarcinogenicityNon-carcinogens0.9119
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5469 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9838
hERG inhibition (predictor II)Non-inhibitor0.8945
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Par pharmaceutical inc
  • Sigmapharm laboratories llc
  • Paddock laboratories inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral
Tabletoral5 mg/1
Tabletoral5.0 mg
Tabletoral5 mg
Prices
Unit descriptionCostUnit
Amiloride hcl powder5.6USD g
Amiloride hcl 5 mg tablet1.49USD tablet
Midamor 5 mg tablet1.19USD tablet
Apo-Amiloride 5 mg Tablet0.28USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point240.5-241.5Cragoe, E.J., Jr.; US. Patent 3,313,813; April 11,1967; assigned to Merck 81 Co., Inc.
water solubilitySlightly solubleNot Available
logP-0.3Not Available
pKa8.7Not Available
Predicted Properties
PropertyValueSource
Water Solubility1.22 mg/mLALOGPS
logP-0.72ALOGPS
logP-0.89ChemAxon
logS-2.3ALOGPS
pKa (Strongest Acidic)16.46ChemAxon
pKa (Strongest Basic)3.29ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area159.29 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity56.69 m3·mol-1ChemAxon
Polarizability19.99 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis Reference

Cragoe, E.J., Jr.; US. Patent 3,313,813; April 11,1967; assigned to Merck 81 Co., Inc.

General ReferencesNot Available
External Links
ATC CodesC03DB01
AHFS Codes
  • 40:28.16
PDB Entries
FDA labelDownload (377 KB)
MSDSDownload (39.3 KB)
Interactions
Drug Interactions
Drug
AcebutololThe risk or severity of adverse effects can be increased when Amiloride is combined with Acebutolol.
AceclofenacAceclofenac may decrease the antihypertensive activities of Amiloride.
AcetazolamideThe risk or severity of adverse effects can be increased when Amiloride is combined with Acetazolamide.
AcetyldigitoxinThe therapeutic efficacy of Acetyldigitoxin can be decreased when used in combination with Amiloride.
Acetylsalicylic acidAcetylsalicylic acid may decrease the antihypertensive activities of Amiloride.
AdapaleneAdapalene may decrease the antihypertensive activities of Amiloride.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Amiloride.
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Amiloride.
AliskirenThe risk or severity of adverse effects can be increased when Amiloride is combined with Aliskiren.
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Amiloride.
AmlodipineThe risk or severity of adverse effects can be increased when Amlodipine is combined with Amiloride.
Ammonium chlorideThe risk or severity of adverse effects can be increased when Amiloride is combined with Ammonium chloride.
AmobarbitalAmobarbital may increase the hypotensive activities of Amiloride.
Amyl NitriteThe risk or severity of adverse effects can be increased when Amiloride is combined with Amyl Nitrite.
AntipyrineAntipyrine may decrease the antihypertensive activities of Amiloride.
ApraclonidineThe risk or severity of adverse effects can be increased when Amiloride is combined with Apraclonidine.
ApremilastApremilast may decrease the antihypertensive activities of Amiloride.
ArdeparinArdeparin may increase the hyperkalemic activities of Amiloride.
AripiprazoleAripiprazole may increase the hypotensive activities of Amiloride.
AtenololThe risk or severity of adverse effects can be increased when Atenolol is combined with Amiloride.
AzapropazoneAzapropazone may decrease the antihypertensive activities of Amiloride.
AzelastineAzelastine may decrease the antihypertensive activities of Amiloride.
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Amiloride is combined with Azilsartan medoxomil.
BalsalazideBalsalazide may decrease the antihypertensive activities of Amiloride.
BarbitalBarbital may increase the hypotensive activities of Amiloride.
BemiparinBemiparin may increase the hyperkalemic activities of Amiloride.
BenazeprilThe risk or severity of adverse effects can be increased when Benazepril is combined with Amiloride.
BendroflumethiazideThe risk or severity of adverse effects can be increased when Bendroflumethiazide is combined with Amiloride.
BenoxaprofenBenoxaprofen may decrease the antihypertensive activities of Amiloride.
BetaxololThe risk or severity of adverse effects can be increased when Betaxolol is combined with Amiloride.
BezitramideThe risk or severity of adverse effects can be increased when Bezitramide is combined with Amiloride.
BisoprololThe risk or severity of adverse effects can be increased when Amiloride is combined with Bisoprolol.
BretyliumThe risk or severity of adverse effects can be increased when Amiloride is combined with Bretylium.
BrimonidineThe risk or severity of adverse effects can be increased when Brimonidine is combined with Amiloride.
BromfenacBromfenac may decrease the antihypertensive activities of Amiloride.
BumetanideThe risk or severity of adverse effects can be increased when Amiloride is combined with Bumetanide.
BuprenorphineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Amiloride.
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Amiloride.
CanagliflozinCanagliflozin may increase the hyperkalemic activities of Amiloride.
CanagliflozinThe risk or severity of adverse effects can be increased when Amiloride is combined with Canagliflozin.
CandesartanThe risk or severity of adverse effects can be increased when Amiloride is combined with Candesartan.
CandoxatrilAmiloride may increase the hyperkalemic activities of Candoxatril.
CaptoprilThe risk or severity of adverse effects can be increased when Amiloride is combined with Captopril.
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Amiloride.
CarprofenCarprofen may decrease the antihypertensive activities of Amiloride.
CarteololThe risk or severity of adverse effects can be increased when Carteolol is combined with Amiloride.
CarvedilolThe risk or severity of adverse effects can be increased when Amiloride is combined with Carvedilol.
CastanospermineCastanospermine may decrease the antihypertensive activities of Amiloride.
CelecoxibCelecoxib may decrease the antihypertensive activities of Amiloride.
CertoparinCertoparin may increase the hyperkalemic activities of Amiloride.
ChloroquineChloroquine may decrease the antihypertensive activities of Amiloride.
ChlorothiazideThe risk or severity of adverse effects can be increased when Amiloride is combined with Chlorothiazide.
ChlorthalidoneThe risk or severity of adverse effects can be increased when Chlorthalidone is combined with Amiloride.
CilazaprilThe risk or severity of adverse effects can be increased when Amiloride is combined with Cilazapril.
ClevidipineThe risk or severity of adverse effects can be increased when Amiloride is combined with Clevidipine.
ClonidineThe risk or severity of adverse effects can be increased when Clonidine is combined with Amiloride.
ClonixinClonixin may decrease the antihypertensive activities of Amiloride.
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Amiloride.
CyclosporineAmiloride may increase the hyperkalemic activities of Cyclosporine.
D-LimoneneD-Limonene may decrease the antihypertensive activities of Amiloride.
DalteparinDalteparin may increase the hyperkalemic activities of Amiloride.
DapagliflozinThe risk or severity of adverse effects can be increased when Amiloride is combined with Dapagliflozin.
DeslanosideThe therapeutic efficacy of Deslanoside can be decreased when used in combination with Amiloride.
DexmedetomidineThe risk or severity of adverse effects can be increased when Amiloride is combined with Dexmedetomidine.
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Amiloride.
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Amiloride.
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Amiloride.
DiclofenacDiclofenac may decrease the antihypertensive activities of Amiloride.
DiclofenamideThe risk or severity of adverse effects can be increased when Amiloride is combined with Diclofenamide.
DiflunisalDiflunisal may decrease the antihypertensive activities of Amiloride.
DigitoxinThe therapeutic efficacy of Digitoxin can be decreased when used in combination with Amiloride.
DigoxinThe therapeutic efficacy of Digoxin can be decreased when used in combination with Amiloride.
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Amiloride.
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Amiloride.
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Amiloride.
DiltiazemThe risk or severity of adverse effects can be increased when Diltiazem is combined with Amiloride.
DinutuximabThe risk or severity of adverse effects can be increased when Amiloride is combined with Dinutuximab.
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Amiloride.
DipyridamoleThe risk or severity of adverse effects can be increased when Amiloride is combined with Dipyridamole.
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Amiloride.
DoxazosinThe risk or severity of adverse effects can be increased when Doxazosin is combined with Amiloride.
DPDPEThe risk or severity of adverse effects can be increased when DPDPE is combined with Amiloride.
DrospirenoneDrospirenone may increase the hyperkalemic activities of Amiloride.
DroxicamDroxicam may decrease the antihypertensive activities of Amiloride.
DuloxetineAmiloride may increase the orthostatic hypotensive activities of Duloxetine.
EmpagliflozinThe risk or severity of adverse effects can be increased when Amiloride is combined with Empagliflozin.
EnalaprilThe risk or severity of adverse effects can be increased when Enalapril is combined with Amiloride.
EnalaprilatAmiloride may increase the hyperkalemic activities of Enalaprilat.
EnoxaparinEnoxaparin may increase the hyperkalemic activities of Amiloride.
EpirizoleEpirizole may decrease the antihypertensive activities of Amiloride.
EplerenoneThe risk or severity of adverse effects can be increased when Amiloride is combined with Eplerenone.
EprosartanThe risk or severity of adverse effects can be increased when Amiloride is combined with Eprosartan.
EsmololThe risk or severity of adverse effects can be increased when Esmolol is combined with Amiloride.
Etacrynic acidThe risk or severity of adverse effects can be increased when Amiloride is combined with Etacrynic acid.
EtanerceptEtanercept may decrease the antihypertensive activities of Amiloride.
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Amiloride.
EtodolacEtodolac may decrease the antihypertensive activities of Amiloride.
EtofenamateEtofenamate may decrease the antihypertensive activities of Amiloride.
EtoricoxibEtoricoxib may decrease the antihypertensive activities of Amiloride.
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Amiloride.
Evening primrose oilEvening primrose oil may decrease the antihypertensive activities of Amiloride.
exisulindexisulind may decrease the antihypertensive activities of Amiloride.
FelodipineThe risk or severity of adverse effects can be increased when Amiloride is combined with Felodipine.
FenbufenFenbufen may decrease the antihypertensive activities of Amiloride.
FenoprofenFenoprofen may decrease the antihypertensive activities of Amiloride.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Amiloride.
FloctafenineFloctafenine may decrease the antihypertensive activities of Amiloride.
FlunixinFlunixin may decrease the antihypertensive activities of Amiloride.
FlurbiprofenFlurbiprofen may decrease the antihypertensive activities of Amiloride.
ForasartanForasartan may increase the hyperkalemic activities of Amiloride.
FosinoprilThe risk or severity of adverse effects can be increased when Fosinopril is combined with Amiloride.
FurosemideThe risk or severity of adverse effects can be increased when Amiloride is combined with Furosemide.
GuanfacineThe risk or severity of adverse effects can be increased when Amiloride is combined with Guanfacine.
HeparinHeparin may increase the hyperkalemic activities of Amiloride.
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Amiloride.
HexobarbitalHexobarbital may increase the hypotensive activities of Amiloride.
HMPL-004HMPL-004 may decrease the antihypertensive activities of Amiloride.
HydralazineThe risk or severity of adverse effects can be increased when Amiloride is combined with Hydralazine.
HydrochlorothiazideThe risk or severity of adverse effects can be increased when Amiloride is combined with Hydrochlorothiazide.
HydrocodoneThe risk or severity of adverse effects can be increased when Hydrocodone is combined with Amiloride.
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Amiloride.
IbuprofenIbuprofen may decrease the antihypertensive activities of Amiloride.
IbuproxamIbuproxam may decrease the antihypertensive activities of Amiloride.
IcatibantIcatibant may decrease the antihypertensive activities of Amiloride.
IndapamideThe risk or severity of adverse effects can be increased when Amiloride is combined with Indapamide.
IndomethacinIndomethacin may decrease the antihypertensive activities of Amiloride.
IndoprofenIndoprofen may decrease the antihypertensive activities of Amiloride.
IrbesartanThe risk or severity of adverse effects can be increased when Amiloride is combined with Irbesartan.
Isosorbide DinitrateThe risk or severity of adverse effects can be increased when Amiloride is combined with Isosorbide Dinitrate.
Isosorbide MononitrateThe risk or severity of adverse effects can be increased when Amiloride is combined with Isosorbide Mononitrate.
IsoxicamIsoxicam may decrease the antihypertensive activities of Amiloride.
IsoxsuprineThe risk or severity of adverse effects can be increased when Amiloride is combined with Isoxsuprine.
IsradipineThe risk or severity of adverse effects can be increased when Isradipine is combined with Amiloride.
KebuzoneKebuzone may decrease the antihypertensive activities of Amiloride.
KetobemidoneThe risk or severity of adverse effects can be increased when Ketobemidone is combined with Amiloride.
KetoprofenKetoprofen may decrease the antihypertensive activities of Amiloride.
KetorolacKetorolac may decrease the antihypertensive activities of Amiloride.
LabetalolThe risk or severity of adverse effects can be increased when Amiloride is combined with Labetalol.
LeflunomideLeflunomide may decrease the antihypertensive activities of Amiloride.
LevobunololThe risk or severity of adverse effects can be increased when Amiloride is combined with Levobunolol.
LevodopaAmiloride may increase the orthostatic hypotensive activities of Levodopa.
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Amiloride.
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Amiloride.
LisinoprilThe risk or severity of adverse effects can be increased when Amiloride is combined with Lisinopril.
LofentanilThe risk or severity of adverse effects can be increased when Lofentanil is combined with Amiloride.
LornoxicamLornoxicam may decrease the antihypertensive activities of Amiloride.
LosartanThe risk or severity of adverse effects can be increased when Amiloride is combined with Losartan.
LoxoprofenLoxoprofen may decrease the antihypertensive activities of Amiloride.
LumiracoxibLumiracoxib may decrease the antihypertensive activities of Amiloride.
Magnesium salicylateMagnesium salicylate may decrease the antihypertensive activities of Amiloride.
MannitolThe risk or severity of adverse effects can be increased when Amiloride is combined with Mannitol.
MasoprocolMasoprocol may decrease the antihypertensive activities of Amiloride.
MecamylamineThe risk or severity of adverse effects can be increased when Amiloride is combined with Mecamylamine.
Meclofenamic acidMeclofenamic acid may decrease the antihypertensive activities of Amiloride.
Mefenamic acidMefenamic acid may decrease the antihypertensive activities of Amiloride.
MeloxicamMeloxicam may decrease the antihypertensive activities of Amiloride.
MesalazineMesalazine may decrease the antihypertensive activities of Amiloride.
MetamizoleMetamizole may decrease the antihypertensive activities of Amiloride.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Amiloride.
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Amiloride.
MethazolamideThe risk or severity of adverse effects can be increased when Amiloride is combined with Methazolamide.
MethohexitalMethohexital may increase the hypotensive activities of Amiloride.
MethyclothiazideThe risk or severity of adverse effects can be increased when Methyclothiazide is combined with Amiloride.
MethyldopaThe risk or severity of adverse effects can be increased when Amiloride is combined with Methyldopa.
MethylphenobarbitalMethylphenobarbital may increase the hypotensive activities of Amiloride.
MetipranololThe risk or severity of adverse effects can be increased when Amiloride is combined with Metipranolol.
MetolazoneThe risk or severity of adverse effects can be increased when Metolazone is combined with Amiloride.
MetoprololThe risk or severity of adverse effects can be increased when Metoprolol is combined with Amiloride.
MinoxidilThe risk or severity of adverse effects can be increased when Minoxidil is combined with Amiloride.
MoexiprilThe risk or severity of adverse effects can be increased when Amiloride is combined with Moexipril.
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Amiloride.
Mycophenolate mofetilMycophenolate mofetil may decrease the antihypertensive activities of Amiloride.
Mycophenolic acidMycophenolic acid may decrease the antihypertensive activities of Amiloride.
NabumetoneNabumetone may decrease the antihypertensive activities of Amiloride.
NadololThe risk or severity of adverse effects can be increased when Amiloride is combined with Nadolol.
NadroparinNadroparin may increase the hyperkalemic activities of Amiloride.
NaftifineNaftifine may decrease the antihypertensive activities of Amiloride.
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Amiloride.
NaproxenNaproxen may decrease the antihypertensive activities of Amiloride.
NCX 4016NCX 4016 may decrease the antihypertensive activities of Amiloride.
NebivololThe risk or severity of adverse effects can be increased when Amiloride is combined with Nebivolol.
NepafenacNepafenac may decrease the antihypertensive activities of Amiloride.
NesiritideThe risk or severity of adverse effects can be increased when Amiloride is combined with Nesiritide.
NicardipineThe risk or severity of adverse effects can be increased when Amiloride is combined with Nicardipine.
NicorandilNicorandil may increase the hypotensive activities of Amiloride.
NifedipineThe risk or severity of adverse effects can be increased when Amiloride is combined with Nifedipine.
Niflumic AcidNiflumic Acid may decrease the antihypertensive activities of Amiloride.
NimesulideNimesulide may decrease the antihypertensive activities of Amiloride.
NimodipineThe risk or severity of adverse effects can be increased when Nimodipine is combined with Amiloride.
NisoldipineThe risk or severity of adverse effects can be increased when Nisoldipine is combined with Amiloride.
NitroglycerinThe risk or severity of adverse effects can be increased when Amiloride is combined with Nitroglycerin.
NitroprussideThe risk or severity of adverse effects can be increased when Nitroprusside is combined with Amiloride.
NormethadoneThe risk or severity of adverse effects can be increased when Normethadone is combined with Amiloride.
OlmesartanThe risk or severity of adverse effects can be increased when Olmesartan is combined with Amiloride.
OlopatadineOlopatadine may decrease the antihypertensive activities of Amiloride.
OlsalazineOlsalazine may decrease the antihypertensive activities of Amiloride.
OmapatrilatAmiloride may increase the hyperkalemic activities of Omapatrilat.
OpiumThe risk or severity of adverse effects can be increased when Opium is combined with Amiloride.
OrgoteinOrgotein may decrease the antihypertensive activities of Amiloride.
OuabainThe therapeutic efficacy of Ouabain can be decreased when used in combination with Amiloride.
OxaprozinOxaprozin may decrease the antihypertensive activities of Amiloride.
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Amiloride.
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Amiloride.
OxyphenbutazoneOxyphenbutazone may decrease the antihypertensive activities of Amiloride.
PapaverineThe risk or severity of adverse effects can be increased when Amiloride is combined with Papaverine.
ParecoxibParecoxib may decrease the antihypertensive activities of Amiloride.
ParnaparinParnaparin may increase the hyperkalemic activities of Amiloride.
PenbutololThe risk or severity of adverse effects can be increased when Amiloride is combined with Penbutolol.
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Amiloride.
PentobarbitalPentobarbital may increase the hypotensive activities of Amiloride.
PerindoprilThe risk or severity of adverse effects can be increased when Amiloride is combined with Perindopril.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Amiloride.
PhenobarbitalPhenobarbital may increase the hypotensive activities of Amiloride.
PhenylbutazonePhenylbutazone may decrease the antihypertensive activities of Amiloride.
PimecrolimusPimecrolimus may decrease the antihypertensive activities of Amiloride.
PindololThe risk or severity of adverse effects can be increased when Amiloride is combined with Pindolol.
PirfenidonePirfenidone may decrease the antihypertensive activities of Amiloride.
PiroxicamPiroxicam may decrease the antihypertensive activities of Amiloride.
PrazosinThe risk or severity of adverse effects can be increased when Prazosin is combined with Amiloride.
PrimidonePrimidone may increase the hypotensive activities of Amiloride.
PropacetamolPropacetamol may decrease the antihypertensive activities of Amiloride.
PropranololThe risk or severity of adverse effects can be increased when Propranolol is combined with Amiloride.
PTC299PTC299 may decrease the antihypertensive activities of Amiloride.
QuetiapineThe risk or severity of adverse effects can be increased when Amiloride is combined with Quetiapine.
QuinaprilThe risk or severity of adverse effects can be increased when Amiloride is combined with Quinapril.
QuinidineThe therapeutic efficacy of Quinidine can be decreased when used in combination with Amiloride.
RamiprilThe risk or severity of adverse effects can be increased when Ramipril is combined with Amiloride.
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Amiloride.
RescinnamineAmiloride may increase the hyperkalemic activities of Rescinnamine.
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Amiloride.
ResveratrolResveratrol may decrease the antihypertensive activities of Amiloride.
ReviparinReviparin may increase the hyperkalemic activities of Amiloride.
RiociguatThe risk or severity of adverse effects can be increased when Amiloride is combined with Riociguat.
RisperidoneAmiloride may increase the hypotensive activities of Risperidone.
RofecoxibRofecoxib may decrease the antihypertensive activities of Amiloride.
SalicylamideSalicylamide may decrease the antihypertensive activities of Amiloride.
Salicylic acidSalicylic acid may decrease the antihypertensive activities of Amiloride.
SalsalateSalsalate may decrease the antihypertensive activities of Amiloride.
SaprisartanSaprisartan may increase the hyperkalemic activities of Amiloride.
SaralasinSaralasin may increase the hyperkalemic activities of Amiloride.
SecobarbitalSecobarbital may increase the hypotensive activities of Amiloride.
SeratrodastSeratrodast may decrease the antihypertensive activities of Amiloride.
SotalolThe risk or severity of adverse effects can be increased when Sotalol is combined with Amiloride.
SpiraprilAmiloride may increase the hyperkalemic activities of Spirapril.
SpironolactoneAmiloride may increase the hyperkalemic activities of Spironolactone.
SpironolactoneThe risk or severity of adverse effects can be increased when Spironolactone is combined with Amiloride.
SRT501SRT501 may decrease the antihypertensive activities of Amiloride.
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Amiloride.
SulfasalazineSulfasalazine may decrease the antihypertensive activities of Amiloride.
SulindacSulindac may decrease the antihypertensive activities of Amiloride.
SuprofenSuprofen may decrease the antihypertensive activities of Amiloride.
TacrolimusAmiloride may increase the hyperkalemic activities of Tacrolimus.
TapentadolThe risk or severity of adverse effects can be increased when Tapentadol is combined with Amiloride.
TasosartanTasosartan may increase the hyperkalemic activities of Amiloride.
TelmisartanThe risk or severity of adverse effects can be increased when Amiloride is combined with Telmisartan.
TemocaprilAmiloride may increase the hyperkalemic activities of Temocapril.
TenoxicamTenoxicam may decrease the antihypertensive activities of Amiloride.
TepoxalinTepoxalin may decrease the antihypertensive activities of Amiloride.
TerazosinThe risk or severity of adverse effects can be increased when Amiloride is combined with Terazosin.
TeriflunomideTeriflunomide may decrease the antihypertensive activities of Amiloride.
ThiamylalThiamylal may increase the hypotensive activities of Amiloride.
ThiopentalThiopental may increase the hypotensive activities of Amiloride.
Tiaprofenic acidTiaprofenic acid may decrease the antihypertensive activities of Amiloride.
TimololThe risk or severity of adverse effects can be increased when Timolol is combined with Amiloride.
TinzaparinTinzaparin may increase the hyperkalemic activities of Amiloride.
TizanidineThe risk or severity of adverse effects can be increased when Amiloride is combined with Tizanidine.
Tolfenamic AcidTolfenamic Acid may decrease the antihypertensive activities of Amiloride.
TolmetinTolmetin may decrease the antihypertensive activities of Amiloride.
TolvaptanTolvaptan may increase the hyperkalemic activities of Amiloride.
TorasemideThe risk or severity of adverse effects can be increased when Torasemide is combined with Amiloride.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Amiloride.
TrandolaprilThe risk or severity of adverse effects can be increased when Trandolapril is combined with Amiloride.
TranilastTranilast may decrease the antihypertensive activities of Amiloride.
TriamtereneThe risk or severity of adverse effects can be increased when Triamterene is combined with Amiloride.
Trisalicylate-cholineTrisalicylate-choline may decrease the antihypertensive activities of Amiloride.
ValdecoxibValdecoxib may decrease the antihypertensive activities of Amiloride.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Amiloride.
VerapamilThe risk or severity of adverse effects can be increased when Amiloride is combined with Verapamil.
ZaltoprofenZaltoprofen may decrease the antihypertensive activities of Amiloride.
ZileutonZileuton may decrease the antihypertensive activities of Amiloride.
ZomepiracZomepirac may decrease the antihypertensive activities of Amiloride.
Food Interactions
  • Avoid drastic changes in dietary habit.
  • Avoid natural licorice.
  • Avoid salt substitutes containing potassium.
  • Take with food to reduce irritation.

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 membrane of epithelial cells. Plays an essential role in electrolyte and blood pressure homeostasis, but also in airway surface liquid homeostasis, which is important for proper clearance of mucus. C...
Gene Name:
SCNN1A
Uniprot ID:
P37088
Molecular Weight:
75703.08 Da
References
  1. Kelly O, Lin C, Ramkumar M, Saxena NC, Kleyman TR, Eaton DC: Characterization of an amiloride binding region in the alpha-subunit of ENaC. Am J Physiol Renal Physiol. 2003 Dec;285(6):F1279-90. Epub 2003 Aug 19. [PubMed:12928313 ]
  2. Ji HL, Benos DJ: Degenerin sites mediate proton activation of deltabetagamma-epithelial sodium channel. J Biol Chem. 2004 Jun 25;279(26):26939-47. Epub 2004 Apr 14. [PubMed:15084585 ]
  3. Otulakowski G, Duan W, Gandhi S, O'brodovich H: Steroid and oxygen effects on eIF4F complex, mTOR, and ENaC translation in fetal lung epithelia. Am J Respir Cell Mol Biol. 2007 Oct;37(4):457-66. Epub 2007 Jun 7. [PubMed:17556672 ]
  4. 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 membrane of epithelial cells. Plays an essential role in electrolyte and blood pressure homeostasis, but also in airway surface liquid homeostasis, which is important for proper clearance of mucus. C...
Gene Name:
SCNN1B
Uniprot ID:
P51168
Molecular Weight:
72658.485 Da
References
  1. Lebowitz J, An B, Edinger RS, Zeidel ML, Johnson JP: Effect of altered Na+ entry on expression of apical and basolateral transport proteins in A6 epithelia. Am J Physiol Renal Physiol. 2003 Sep;285(3):F524-31. Epub 2003 May 13. [PubMed:12746257 ]
  2. Planes C, Leyvraz C, Uchida T, Angelova MA, Vuagniaux G, Hummler E, Matthay M, Clerici C, Rossier B: In vitro and in vivo regulation of transepithelial lung alveolar sodium transport by serine proteases. Am J Physiol Lung Cell Mol Physiol. 2005 Jun;288(6):L1099-109. Epub 2005 Jan 28. [PubMed:15681398 ]
  3. Yamagata T, Yamagata Y, Nishimoto T, Nakanishi M, Nakanishi H, Minakata Y, Mune M, Yukawa S: The impact of phorbol ester on the regulation of amiloride-sensitive epithelial sodium channel in alveolar type ii epithelial cells. Exp Lung Res. 2002 Oct-Nov;28(7):543-62. [PubMed:12396248 ]
  4. Brooks HL, Allred AJ, Beutler KT, Coffman TM, Knepper MA: Targeted proteomic profiling of renal Na(+) transporter and channel abundances in angiotensin II type 1a receptor knockout mice. Hypertension. 2002 Feb;39(2 Pt 2):470-3. [PubMed:11882592 ]
  5. Kamide K, Tanaka C, Takiuchi S, Miwa Y, Yoshii M, Horio T, Kawano Y, Miyata T: Six missense mutations of the epithelial sodium channel beta and gamma subunits in Japanese hypertensives. Hypertens Res. 2004 May;27(5):333-8. [PubMed:15198480 ]
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 membrane of epithelial cells. Plays an essential role in electrolyte and blood pressure homeostasis, but also in airway surface liquid homeostasis, which is important for proper clearance of mucus. C...
Gene Name:
SCNN1G
Uniprot ID:
P51170
Molecular Weight:
74269.62 Da
References
  1. Viemann M, Peter M, Lopez-Siguero JP, Simic-Schleicher G, Sippell WG: Evidence for genetic heterogeneity of pseudohypoaldosteronism type 1: identification of a novel mutation in the human mineralocorticoid receptor in one sporadic case and no mutations in two autosomal dominant kindreds. J Clin Endocrinol Metab. 2001 May;86(5):2056-9. [PubMed:11344206 ]
  2. Iwai N, Baba S, Mannami T, Katsuya T, Higaki J, Ogihara T, Ogata J: Association of sodium channel gamma-subunit promoter variant with blood pressure. Hypertension. 2001 Jul;38(1):86-9. [PubMed:11463765 ]
  3. Yamagata T, Yamagata Y, Nishimoto T, Nakanishi M, Nakanishi H, Minakata Y, Mune M, Yukawa S: The impact of phorbol ester on the regulation of amiloride-sensitive epithelial sodium channel in alveolar type ii epithelial cells. Exp Lung Res. 2002 Oct-Nov;28(7):543-62. [PubMed:12396248 ]
  4. Akcay A, Yavuz T, Semiz S, Bundak R, Demirdoven M: Pseudohypoaldosteronism type 1 and respiratory distress syndrome. J Pediatr Endocrinol Metab. 2002 Nov-Dec;15(9):1557-61. [PubMed:12503866 ]
  5. Ludwig M, Bidlingmaier F, Reissinger A: Pseudohypoaldosteronism type 1 and the genes encoding prostasin, alpha-spectrin, and Nedd4. Int J Mol Med. 2004 Dec;14(6):1101-4. [PubMed:15547682 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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 membrane of epithelial cells. Controls the reabsorption of sodium in kidney, colon, lung and sweat glands. Also plays a role in taste perception.
Gene Name:
SCNN1D
Uniprot ID:
P51172
Molecular Weight:
70214.195 Da
References
  1. Yamamura H, Ugawa S, Ueda T, Nagao M, Shimada S: Protons activate the delta-subunit of the epithelial Na+ channel in humans. J Biol Chem. 2004 Mar 26;279(13):12529-34. Epub 2004 Jan 15. [PubMed:14726523 ]
  2. Ji HL, Bishop LR, Anderson SJ, Fuller CM, Benos DJ: The role of Pre-H2 domains of alpha- and delta-epithelial Na+ channels in ion permeation, conductance, and amiloride sensitivity. J Biol Chem. 2004 Feb 27;279(9):8428-40. Epub 2003 Dec 2. [PubMed:14660613 ]
  3. Ji HL, Su XF, Kedar S, Li J, Barbry P, Smith PR, Matalon S, Benos DJ: Delta-subunit confers novel biophysical features to alpha beta gamma-human epithelial sodium channel (ENaC) via a physical interaction. J Biol Chem. 2006 Mar 24;281(12):8233-41. Epub 2006 Jan 19. [PubMed:16423824 ]
  4. Yamamura H, Ugawa S, Ueda T, Nagao M, Shimada S: Icilin activates the delta-subunit of the human epithelial Na+ channel. Mol Pharmacol. 2005 Oct;68(4):1142-7. Epub 2005 Jul 20. [PubMed:16033954 ]
  5. Yamamura H, Ugawa S, Ueda T, Shimada S: Evans blue is a specific antagonist of the human epithelial Na+ channel delta-subunit. J Pharmacol Exp Ther. 2005 Nov;315(2):965-9. Epub 2005 Aug 17. [PubMed:16107516 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Zinc ion binding
Specific Function:
Catalyzes the degradation of compounds such as putrescine, histamine, spermine, and spermidine, substances involved in allergic and immune responses, cell proliferation, tissue differentiation, tumor formation, and possibly apoptosis. Placental DAO is thought to play a role in the regulation of the female reproductive function.
Gene Name:
AOC1
Uniprot ID:
P19801
Molecular Weight:
85377.1 Da
References
  1. Padiglia A, Medda R, Lorrai A, Murgia B, Pedersen JZ, Finazzi Agro A, Floris G: Interaction of Pig Kidney and Lentil Seedling Copper-Containing Amine Oxidases with Guanidinium Compounds. J Enzyme Inhib. 1999 Nov;15(1):91-100. [PubMed:10938536 ]
  2. Padiglia A, Medda R, Lorrai A, Murgia B, Pedersen JZ, Agro AF, Floris G: Interaction of pig kidney and lentil seedling copper-containing amine oxidases with guanidinium compounds. J Enzyme Inhib. 2000;15(1):91-100. [PubMed:10850957 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Ligand-gated sodium channel activity
Specific Function:
Cation channel with high affinity for sodium, which is gated by extracellular protons and inhibited by the diuretic amiloride. Also permeable for Li(+) and K(+). Generates a biphasic current with a fast inactivating and a slow sustained phase. Heteromeric channel assembly seems to modulate.
Gene Name:
ASIC2
Uniprot ID:
Q16515
Molecular Weight:
57708.515 Da
References
  1. Berdiev BK, Xia J, McLean LA, Markert JM, Gillespie GY, Mapstone TB, Naren AP, Jovov B, Bubien JK, Ji HL, Fuller CM, Kirk KL, Benos DJ: Acid-sensing ion channels in malignant gliomas. J Biol Chem. 2003 Apr 25;278(17):15023-34. Epub 2003 Feb 12. [PubMed:12584187 ]
  2. Ugawa S, Yamamoto T, Ueda T, Ishida Y, Inagaki A, Nishigaki M, Shimada S: Amiloride-insensitive currents of the acid-sensing ion channel-2a (ASIC2a)/ASIC2b heteromeric sour-taste receptor channel. J Neurosci. 2003 May 1;23(9):3616-22. [PubMed:12736332 ]
  3. Ugawa S: Identification of sour-taste receptor genes. Anat Sci Int. 2003 Dec;78(4):205-10. [PubMed:14686475 ]
  4. Peng BG, Ahmad S, Chen S, Chen P, Price MP, Lin X: Acid-sensing ion channel 2 contributes a major component to acid-evoked excitatory responses in spiral ganglion neurons and plays a role in noise susceptibility of mice. J Neurosci. 2004 Nov 10;24(45):10167-75. [PubMed:15537887 ]
  5. Vila-Carriles WH, Kovacs GG, Jovov B, Zhou ZH, Pahwa AK, Colby G, Esimai O, Gillespie GY, Mapstone TB, Markert JM, Fuller CM, Bubien JK, Benos DJ: Surface expression of ASIC2 inhibits the amiloride-sensitive current and migration of glioma cells. J Biol Chem. 2006 Jul 14;281(28):19220-32. Epub 2006 May 16. [PubMed:16704974 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Ligand-gated sodium channel activity
Specific Function:
Isoform 2 and isoform 3 function as proton-gated sodium channels; they are activated by a drop of the extracellular pH and then become rapidly desensitized. The channel generates a biphasic current with a fast inactivating and a slow sustained phase. Has high selectivity for sodium ions and can also transport lithium ions with high efficiency. Isoform 2 can also transport potassium, but with lo...
Gene Name:
ASIC1
Uniprot ID:
P78348
Molecular Weight:
59908.915 Da
References
  1. Petruska JC, Napaporn J, Johnson RD, Cooper BY: Chemical responsiveness and histochemical phenotype of electrophysiologically classified cells of the adult rat dorsal root ganglion. Neuroscience. 2002;115(1):15-30. [PubMed:12401318 ]
  2. Jones NG, Slater R, Cadiou H, McNaughton P, McMahon SB: Acid-induced pain and its modulation in humans. J Neurosci. 2004 Dec 1;24(48):10974-9. [PubMed:15574747 ]
  3. Sugiura T, Dang K, Lamb K, Bielefeldt K, Gebhart GF: Acid-sensing properties in rat gastric sensory neurons from normal and ulcerated stomach. J Neurosci. 2005 Mar 9;25(10):2617-27. [PubMed:15758172 ]
  4. Wang W, Duan B, Xu H, Xu L, Xu TL: Calcium-permeable acid-sensing ion channel is a molecular target of the neurotoxic metal ion lead. J Biol Chem. 2006 Feb 3;281(5):2497-505. Epub 2005 Nov 29. [PubMed:16319075 ]
  5. Xiong ZG, Chu XP, Simon RP: Ca2+ -permeable acid-sensing ion channels and ischemic brain injury. J Membr Biol. 2006 Jan;209(1):59-68. Epub 2006 Apr 17. [PubMed:16685601 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Solute:proton antiporter activity
Specific Function:
Involved in pH regulation to eliminate acids generated by active metabolism or to counter adverse environmental conditions. Major proton extruding system driven by the inward sodium ion chemical gradient. Plays an important role in signal transduction.
Gene Name:
SLC9A1
Uniprot ID:
P19634
Molecular Weight:
90762.13 Da
References
  1. Lee MG, Ahn W, Choi JY, Luo X, Seo JT, Schultheis PJ, Shull GE, Kim KH, Muallem S: Na(+)-dependent transporters mediate HCO(3)(-) salvage across the luminal membrane of the main pancreatic duct. J Clin Invest. 2000 Jun;105(11):1651-8. [PubMed:10841524 ]
  2. Konstantinou-Tegou A, Kaloyianni M, Bourikas D, Koliakos G: The effect of leptin on Na(+)-H(+) antiport (NHE 1) activity of obese and normal subjects erythrocytes. Mol Cell Endocrinol. 2001 Oct 25;183(1-2):11-8. [PubMed:11604219 ]
  3. Serrani RE, Mujica G, Gioia IA, Corchs JL: Neonatal red blood cells: amiloride-insensitive Na+-H+ transport isoform would express Na+-Li+ exchange. Acta Physiol Pharmacol Bulg. 2000;25(3-4):71-4. [PubMed:11688549 ]
  4. Cuthbert AW, Supuran CT, MacVinish LJ: Bicarbonate-dependent chloride secretion in Calu-3 epithelia in response to 7,8-benzoquinoline. J Physiol. 2003 Aug 15;551(Pt 1):79-92. Epub 2003 Jul 18. [PubMed:12872009 ]
  5. Furukawa O, Bi LC, Guth PH, Engel E, Hirokawa M, Kaunitz JD: NHE3 inhibition activates duodenal bicarbonate secretion in the rat. Am J Physiol Gastrointest Liver Physiol. 2004 Jan;286(1):G102-9. Epub 2003 Jul 24. [PubMed:12881227 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Serine-type endopeptidase activity
Specific Function:
Specifically cleaves the zymogen plasminogen to form the active enzyme plasmin.
Gene Name:
PLAU
Uniprot ID:
P00749
Molecular Weight:
48507.09 Da
References
  1. Vakili J, Standker L, Detheux M, Vassart G, Forssmann WG, Parmentier M: Urokinase plasminogen activator and plasmin efficiently convert hemofiltrate CC chemokine 1 into its active. J Immunol. 2001 Sep 15;167(6):3406-13. [PubMed:11544332 ]
  2. Jankun J, Skrzypczak-Jankun E: Binding site of amiloride to urokinase plasminogen activator depends on species. Int J Mol Med. 2001 Oct;8(4):365-71. [PubMed:11562773 ]
  3. Luikart S, Masri M, Wahl D, Hinkel T, Beck JM, Gyetko MR, Gupta P, Oegema T: Urokinase is required for the formation of mactinin, an alpha-actinin fragment that promotes monocyte/macrophage maturation. Biochim Biophys Acta. 2002 Aug 19;1591(1-3):99-107. [PubMed:12183060 ]
  4. Chen YX, O'Brien ER: Ethyl isopropyl amiloride inhibits smooth muscle cell proliferation and migration by inducing apoptosis and antagonizing urokinase plasminogen activator activity. Can J Physiol Pharmacol. 2003 Jul;81(7):730-9. [PubMed:12897821 ]
  5. Cejkova J, Cejka C, Zvarova J: Effects of inhibition of urokinase-type plasminogen activator (u-PA) by amiloride in the cornea and tear fluid of eyes irradiated with UVB. Acta Histochem. 2005;107(1):77-86. Epub 2005 Mar 4. [PubMed:15866288 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Zinc ion binding
Specific Function:
Catalyzes the degradation of compounds such as putrescine, histamine, spermine, and spermidine, substances involved in allergic and immune responses, cell proliferation, tissue differentiation, tumor formation, and possibly apoptosis. Placental DAO is thought to play a role in the regulation of the female reproductive function.
Gene Name:
AOC1
Uniprot ID:
P19801
Molecular Weight:
85377.1 Da
References
  1. Padiglia A, Medda R, Lorrai A, Murgia B, Pedersen JZ, Finazzi Agro A, Floris G: Interaction of Pig Kidney and Lentil Seedling Copper-Containing Amine Oxidases with Guanidinium Compounds. J Enzyme Inhib. 1999 Nov;15(1):91-100. [PubMed:10938536 ]
  2. Padiglia A, Medda R, Lorrai A, Murgia B, Pedersen JZ, Agro AF, Floris G: Interaction of pig kidney and lentil seedling copper-containing amine oxidases with guanidinium compounds. J Enzyme Inhib. 2000;15(1):91-100. [PubMed:10850957 ]
Kind
Protein
Organism
Pig
Pharmacological action
unknown
Actions
inhibitor
General Function:
Zinc ion binding
Specific Function:
Catalyzes the degradation of compounds such as putrescine, histamine, spermine, and spermidine, substances involved in allergic and immune responses, cell proliferation, tissue differentiation, tumor formation, and possibly apoptosis.
Gene Name:
AOC1
Uniprot ID:
Q9TRC7
Molecular Weight:
85474.24 Da
References
  1. Padiglia A, Medda R, Lorrai A, Murgia B, Pedersen JZ, Finazzi Agro A, Floris G: Interaction of Pig Kidney and Lentil Seedling Copper-Containing Amine Oxidases with Guanidinium Compounds. J Enzyme Inhib. 1999 Nov;15(1):91-100. [PubMed:10938536 ]
  2. Padiglia A, Medda R, Lorrai A, Murgia B, Pedersen JZ, Agro AF, Floris G: Interaction of pig kidney and lentil seedling copper-containing amine oxidases with guanidinium compounds. J Enzyme Inhib. 2000;15(1):91-100. [PubMed:10850957 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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, creatinine, amantadine, memantine, acriflavine, 4-[4-(dimethylamino)-styryl]-N-methylpyridinium ASP, amiloride, metformin, N-1-methylnicotinamide (NMN), tetraethylammonium (TEA), 1-methyl-4-phenylpyridiniu...
Gene Name:
SLC22A2
Uniprot ID:
O15244
Molecular Weight:
62579.99 Da
References
  1. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine...
Gene Name:
SLC22A1
Uniprot ID:
O15245
Molecular Weight:
61153.345 Da
References
  1. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Symporter activity
Specific Function:
Sodium-ion dependent, low affinity carnitine transporter. Probably transports one sodium ion with one molecule of carnitine. Also transports organic cations such as tetraethylammonium (TEA) without the involvement of sodium. Relative uptake activity ratio of carnitine to TEA is 1.78. A key substrate of this transporter seems to be ergothioneine (ET).
Gene Name:
SLC22A4
Uniprot ID:
Q9H015
Molecular Weight:
62154.48 Da
References
  1. Wu X, George RL, Huang W, Wang H, Conway SJ, Leibach FH, Ganapathy V: Structural and functional characteristics and tissue distribution pattern of rat OCTN1, an organic cation transporter, cloned from placenta. Biochim Biophys Acta. 2000 Jun 1;1466(1-2):315-27. [PubMed:10825452 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23