Explore a selection of our essential drug information below, or:
Identification
- Summary
Amiloride is a pyrizine compound used to treat hypertension and congestive heart failure.
- Brand Names
- Midamor
- Generic Name
- Amiloride
- DrugBank Accession Number
- DB00594
- Background
A 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)
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Amiloride (DB00594)
- Weight
- Average: 229.627
Monoisotopic: 229.04788562 - Chemical Formula
- C6H8ClN7O
- Synonyms
- 3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-carboxamide
- Amilorid
- Amilorida
- Amiloride
- Amiloridum
- Amipramidin
- Amipramidine
- Amyloride
- N-amidino-3,5-diamino-6-chloropyrazinecarboxamide
- External IDs
- MK 870
Pharmacology
- Indication
For use as adjunctive treatment with thiazide diuretics or other kaliuretic-diuretic agents in congestive heart failure or hypertension.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Ascites ••• ••••• Prevention of Calcium nephrolithiasis ••• ••••• Adjunct therapy in management of Congestive heart failure •••••••••••• •••••• Used in combination to manage High blood pressure (hypertension) Combination Product in combination with: Bendroflumethiazide (DB00436) •••••••••••• •••••• Used in combination to treat High blood pressure (hypertension) Combination Product in combination with: Timolol (DB00373), Hydrochlorothiazide (DB00999) •••••••••••• •••••• - Contraindications & Blackbox Warnings
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Amiloride, 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 action
Amiloride 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.
Target Actions Organism AAmiloride-sensitive sodium channel subunit alpha inhibitorHumans AAmiloride-sensitive sodium channel subunit beta inhibitorHumans AAmiloride-sensitive sodium channel subunit gamma inhibitorHumans AAmiloride-sensitive sodium channel subunit delta inhibitorHumans UDiamine oxidase [copper-containing] inhibitorHumans UAcid-sensing ion channel 2 inhibitorHumans UAcid-sensing ion channel 1 inhibitorHumans USodium/hydrogen exchanger 1 inhibitorHumans UUrokinase-type plasminogen activator inhibitorHumans - Absorption
Readily absorbed following oral administration.
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
Amiloride is not metabolized by the liver but is excreted unchanged by the kidneys.
- Route of elimination
Amiloride 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-life
Plasma half-life varies from 6 to 9 hours.
- Clearance
Not Available
- Adverse Effects
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No 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.
- Pathways
Pathway Category Amiloride Action Pathway Drug action - Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- 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 Amiloride 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 Amiloride is combined with Abaloparatide. Acebutolol The risk or severity of adverse effects can be increased when Amiloride is combined with Acebutolol. Aceclofenac The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Aceclofenac is combined with Amiloride. Acemetacin The therapeutic efficacy of Amiloride can be decreased when used in combination with Acemetacin. - Food Interactions
- Avoid drastic dietary changes.
- Avoid natural licorice.
- Avoid potassium-containing products.
- Take with food. Food reduces irritation.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Amiloride hydrochloride 7M458Q65S3 2016-88-8 ACHKKGDWZVCSNH-UHFFFAOYSA-N Amiloride hydrochloride dihydrate FZJ37245UC 17440-83-4 LTKVFMLMEYCWMK-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Arumil (Sharp & Dohme) / Kaluril (Alphapharm) / Modamide (Merck) / Moduretic (Merck)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Amiloride Hydrochloride Tablet 5 mg/1 Oral Physicians Total Care, Inc. 2005-01-28 Not applicable US 
Amiloride Hydrochloride Tablets, USP Tablet 5 mg Oral Orbus Pharma Inc Not applicable Not applicable Canada 
Amiloride Hydrocloride Tablet 5 mg/1 Oral KAISER FOUNDATION HOSPITALS 2017-09-07 2019-02-28 US Midamor Tablet 5.0 mg Oral Aa Pharma Inc 2004-06-18 Not applicable Canada Midamor Tablets 5mg Tablet 5 mg Oral Orbus Pharma Inc 1981-12-31 2010-06-16 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Amiloride Hydrochloride Tablet 5 mg/1 Oral Sigmapharm Laboratories, LLC 2021-06-14 Not applicable US Amiloride Hydrochloride Tablet 5 mg/1 Oral Golden State Medical Supply, Inc. 1986-01-22 Not applicable US Amiloride Hydrochloride Tablet 5 mg/1 Oral Rising Pharmaceuticals, Inc. 2009-05-01 2019-07-31 US Amiloride Hydrochloride Tablet 5 mg/1 Oral Zydus Pharmaceuticals USA Inc. 2015-09-14 2017-07-19 US Amiloride Hydrochloride Tablet 5 mg/1 Oral bryant ranch prepack 1986-01-22 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Aa-amilzide Amiloride hydrochloride (5 mg) + Hydrochlorothiazide (50 mg) Tablet Oral Aa Pharma Inc 1989-12-31 Not applicable Canada AA-Amilzide Tablet 50mg/5mg Amiloride hydrochloride (5 mg) + Hydrochlorothiazide (50 mg) Tablet Oral PHARMAFORTE SINGAPORE PTE LTD 2024-01-17 Not applicable Malaysia 
Alti-amiloride Hctz Amiloride hydrochloride (5 mg) + Hydrochlorothiazide (50 mg) Tablet Oral Altimed Pharma Inc. 1995-12-31 2004-08-03 Canada Ami-hydro Tab Amiloride hydrochloride (5 mg) + Hydrochlorothiazide (50 mg) Tablet Oral Pro Doc Limitee 1990-12-31 2017-05-05 Canada AMIDROTHIDE Amiloride (5 MG) + Hydrochlorothiazide (50 MG) Tablet Oral บริษัท โรงงานเภสัชกรรมแอตแลนติค จำกัด 1992-08-03 Not applicable Thailand 
Categories
- ATC Codes
- C03DB01 — Amiloride
- Drug Categories
- Acid Sensing Ion Channel Blockers
- Agents causing hyperkalemia
- Cardiovascular Agents
- Decreased Renal K+ Excretion
- Diuretics
- Epithelial Sodium Channel Blockers
- Hypotensive Agents
- Increased Diuresis
- Membrane Transport Modulators
- Natriuretic Agents
- OCT2 Inhibitors
- Potassium-Sparing Diuretics
- Pyrazines
- Sodium Channel Blockers
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as aminopyrazines. These are organic compounds containing an amino group attached to a pyrazine ring.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Diazines
- Sub Class
- Pyrazines
- Direct Parent
- Aminopyrazines
- Alternative Parents
- Imidolactams / Aryl chlorides / Heteroaromatic compounds / Propargyl-type 1,3-dipolar organic compounds / Carboximidamides / Azacyclic compounds / Primary amines / Organopnictogen compounds / Organooxygen compounds / Organochlorides show 2 more
- Substituents
- Amine / Aminopyrazine / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Azacycle / Carboximidamide / Heteroaromatic compound / Hydrocarbon derivative / Imidolactam show 11 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- pyrazines, monocarboxylic acid amide, organochlorine compound, guanidines, aromatic amine (CHEBI:2639) / a small molecule (CPD-10324)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 7DZO8EB0Z3
- CAS number
- 2609-46-3
- InChI Key
- 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-N-carbamimidoyl-6-chloropyrazine-2-carboxamide
- SMILES
- NC(=N)NC(=O)C1=NC(Cl)=C(N)N=C1N
References
- Synthesis Reference
Cragoe, E.J., Jr.; US. Patent 3,313,813; April 11,1967; assigned to Merck 81 Co., Inc.
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0014732
- KEGG Drug
- D07447
- KEGG Compound
- C06821
- PubChem Compound
- 16231
- PubChem Substance
- 46508156
- ChemSpider
- 15403
- BindingDB
- 16173
- 644
- ChEBI
- 2639
- ChEMBL
- CHEMBL945
- ZINC
- ZINC000004340269
- Therapeutic Targets Database
- DAP000187
- PharmGKB
- PA448368
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- AMR
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Amiloride
- PDB Entries
- 1f5l / 4ntx
- FDA label
- Download (377 KB)
- MSDS
- Download (39.3 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Active Not Recruiting Not Available Hypertension 1 somestatus stop reason just information to hide Not Available Completed Not Available Bone Fractures / Type 2 Diabetes Mellitus 1 somestatus stop reason just information to hide Not Available Completed Not Available Coronavirus Disease 2019 (COVID‑19) / COVID / Hypertension 1 somestatus stop reason just information to hide Not Available Completed Not Available Primary Aldosteronism / Primary Aldosteronism Due to Adrenal Hyperplasia (Bilateral) / Primary Aldosteronism Due to Aldosterone Producing Adenoma 1 somestatus stop reason just information to hide Not Available Completed Basic Science Physiological Conditions 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Par pharmaceutical inc
- Sigmapharm laboratories llc
- Paddock laboratories inc
- Packagers
- Kaiser Foundation Hospital
- Paddock Labs
- Par Pharmaceuticals
- Physicians Total Care Inc.
- Qualitest
- Rising Pharmaceuticals
- Sigmapharm Laboratories LLC
- Spectrum Pharmaceuticals
- Dosage Forms
Form Route Strength Tablet Oral Tablet Oral 5 mg/1 Tablet Oral Tablet Oral 5 mg Tablet, film coated Oral Tablet Oral 5.0 mg Tablet Oral 5 mg Tablet - Prices
Unit description Cost Unit Amiloride hcl powder 5.6USD g Amiloride hcl 5 mg tablet 1.49USD tablet Midamor 5 mg tablet 1.19USD tablet Apo-Amiloride 5 mg Tablet 0.28USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 240.5-241.5 Cragoe, E.J., Jr.; US. Patent 3,313,813; April 11,1967; assigned to Merck 81 Co., Inc. water solubility Slightly soluble Not Available logP -0.3 Not Available pKa 8.7 Not Available - Predicted Properties
Property Value Source Water Solubility 0.616 mg/mL ALOGPS logP -0.48 ALOGPS logP -0.5 Chemaxon logS -2.6 ALOGPS pKa (Strongest Acidic) 11.43 Chemaxon pKa (Strongest Basic) 7.35 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 7 Chemaxon Hydrogen Donor Count 5 Chemaxon Polar Surface Area 156.79 Å2 Chemaxon Rotatable Bond Count 1 Chemaxon Refractivity 67.18 m3·mol-1 Chemaxon Polarizability 20 Å3 Chemaxon Number of Rings 1 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9408 Blood Brain Barrier + 0.7193 Caco-2 permeable - 0.8957 P-glycoprotein substrate Non-substrate 0.7207 P-glycoprotein inhibitor I Non-inhibitor 0.9282 P-glycoprotein inhibitor II Non-inhibitor 0.9677 Renal organic cation transporter Non-inhibitor 0.8122 CYP450 2C9 substrate Non-substrate 0.8253 CYP450 2D6 substrate Non-substrate 0.8778 CYP450 3A4 substrate Non-substrate 0.6687 CYP450 1A2 substrate Inhibitor 0.9107 CYP450 2C9 inhibitor Non-inhibitor 0.9577 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.9295 CYP450 3A4 inhibitor Non-inhibitor 0.9733 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9605 Ames test AMES toxic 0.9107 Carcinogenicity Non-carcinogens 0.9119 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.5469 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9838 hERG inhibition (predictor II) Non-inhibitor 0.8945
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 147.1949878 predictedDarkChem Lite v0.1.0 [M-H]- 149.99571 predictedDeepCCS 1.0 (2019) [M+H]+ 147.8307878 predictedDarkChem Lite v0.1.0 [M+H]+ 152.35371 predictedDeepCCS 1.0 (2019) [M+Na]+ 147.0313878 predictedDarkChem Lite v0.1.0 [M+Na]+ 158.44685 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General 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. Controls the reabsorption of sodium in kidney, colon, lung and eccrine sweat glands. Also plays a role in taste perception
- Specific Function
- ligand-gated sodium channel activity
- Gene Name
- SCNN1A
- Uniprot ID
- P37088
- Uniprot Name
- Amiloride-sensitive sodium channel subunit alpha
- Molecular Weight
- 75703.08 Da
References
- 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. [Article]
- 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. [Article]
- 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. [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
- 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. Controls the reabsorption of sodium in kidney, colon, lung and sweat glands. Also plays a role in taste perception
- Specific Function
- ligand-gated sodium channel activity
- Gene Name
- SCNN1B
- Uniprot ID
- P51168
- Uniprot Name
- Amiloride-sensitive sodium channel subunit beta
- Molecular Weight
- 72658.485 Da
References
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General 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. Controls the reabsorption of sodium in kidney, colon, lung and sweat glands. Also plays a role in taste perception
- Specific Function
- ligand-gated sodium channel activity
- Gene Name
- SCNN1G
- Uniprot ID
- P51170
- Uniprot Name
- Amiloride-sensitive sodium channel subunit gamma
- Molecular Weight
- 74269.62 Da
References
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General 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
- Specific Function
- ligand-gated sodium channel activity
- Gene Name
- SCNN1D
- Uniprot ID
- P51172
- Uniprot Name
- Amiloride-sensitive sodium channel subunit delta
- Molecular Weight
- 87849.205 Da
References
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Catalyzes the oxidative deamination of primary amines to the corresponding aldehydes with the concomitant production of hydrogen peroxide and ammonia (PubMed:12072962, PubMed:19764817, PubMed:239684, PubMed:8144586). Its preferred substrates are the diamines histamine and 1-methylhistamine and it could therefore play a role in allergic and immune responses (PubMed:12072962). Has a broad specificity for diamines and can also act on cadaverine and putrescine, two products of amino acid catabolism (PubMed:12072962). It could also act on polyamines, like spermidine and spermine though less efficiently, and regulate various biological processes (PubMed:12072962, PubMed:239684)
- Specific Function
- calcium ion binding
- Gene Name
- AOC1
- Uniprot ID
- P19801
- Uniprot Name
- Diamine oxidase [copper-containing]
- Molecular Weight
- 85377.1 Da
References
- 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. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General 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
- Specific Function
- ligand-gated sodium channel activity
- Gene Name
- ASIC2
- Uniprot ID
- Q16515
- Uniprot Name
- Acid-sensing ion channel 2
- Molecular Weight
- 57708.515 Da
References
- 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. [Article]
- 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. [Article]
- Ugawa S: Identification of sour-taste receptor genes. Anat Sci Int. 2003 Dec;78(4):205-10. [Article]
- 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. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General 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 lower efficiency. It is nearly impermeable to the larger rubidium and cesium ions. Isoform 3 can also transport calcium ions. Mediates glutamate-independent Ca(2+) entry into neurons upon acidosis. This Ca(2+) overloading is toxic for cortical neurons and may be in part responsible for ischemic brain injury. Heteromeric channel assembly seems to modulate channel properties. Functions as a postsynaptic proton receptor that influences intracellular Ca(2+) concentration and calmodulin-dependent protein kinase II phosphorylation and thereby the density of dendritic spines. Modulates activity in the circuits underlying innate fear
- Specific Function
- ligand-gated sodium channel activity
- Gene Name
- ASIC1
- Uniprot ID
- P78348
- Uniprot Name
- Acid-sensing ion channel 1
- Molecular Weight
- 59908.915 Da
References
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Electroneutral Na(+) /H(+) antiporter that extrudes Na(+) in exchange for external protons driven by the inward sodium ion chemical gradient, protecting cells from acidification that occurs from metabolism (PubMed:11350981, PubMed:11532004, PubMed:14680478, PubMed:15035633, PubMed:15677483, PubMed:17073455, PubMed:17493937, PubMed:22020933, PubMed:27650500, PubMed:32130622, PubMed:7110335, PubMed:7603840). Exchanges intracellular H(+) ions for extracellular Na(+) in 1:1 stoichiometry (By similarity). Plays a key role in maintening intracellular pH neutral and cell volume, and thus is important for cell growth, proliferation, migration and survival (PubMed:12947095, PubMed:15096511, PubMed:22020933, PubMed:8901634). In addition, can transport lithium Li(+) and functions also as a Na(+)/Li(+) antiporter (PubMed:7603840). SLC9A1 also functions in membrane anchoring and organization of scaffolding complexes that coordinate signaling inputs (PubMed:15096511)
- Specific Function
- calcium-dependent protein binding
- Gene Name
- SLC9A1
- Uniprot ID
- P19634
- Uniprot Name
- Sodium/hydrogen exchanger 1
- Molecular Weight
- 90762.13 Da
References
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Specifically cleaves the zymogen plasminogen to form the active enzyme plasmin
- Specific Function
- serine-type endopeptidase activity
- Gene Name
- PLAU
- Uniprot ID
- P00749
- Uniprot Name
- Urokinase-type plasminogen activator
- Molecular Weight
- 48523.13 Da
References
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Catalyzes the oxidative deamination of primary amines to the corresponding aldehydes with the concomitant production of hydrogen peroxide and ammonia (PubMed:12072962, PubMed:19764817, PubMed:239684, PubMed:8144586). Its preferred substrates are the diamines histamine and 1-methylhistamine and it could therefore play a role in allergic and immune responses (PubMed:12072962). Has a broad specificity for diamines and can also act on cadaverine and putrescine, two products of amino acid catabolism (PubMed:12072962). It could also act on polyamines, like spermidine and spermine though less efficiently, and regulate various biological processes (PubMed:12072962, PubMed:239684)
- Specific Function
- calcium ion binding
- Gene Name
- AOC1
- Uniprot ID
- P19801
- Uniprot Name
- Diamine oxidase [copper-containing]
- Molecular Weight
- 85377.1 Da
References
- 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. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Pig
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Catalyzes the oxidative deamination of primary amines to the corresponding aldehydes with the concomitant production of hydrogen peroxide and ammonia (PubMed:1457410, PubMed:8144586). Its preferred substrates in vitro are the diamines histamine and 1-methylhistamine and it could therefore play a role in allergic and immune responses (By similarity). Has a broad specificity for diamines and can also act on cadaverine and putrescine, two products of amino acid catabolism (PubMed:8144586). It could also act on polyamines, like spermidine and spermine though less efficiently, and regulate various biological processes (By similarity).
- Specific Function
- copper ion binding
- Gene Name
- AOC1
- Uniprot ID
- Q9TRC7
- Uniprot Name
- Amiloride-sensitive amine oxidase [copper-containing]
- Molecular Weight
- 85474.24 Da
References
- 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. [Article]
- 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. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Electrogenic voltage-dependent transporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics (PubMed:9260930, PubMed:9687576). Functions as a Na(+)-independent, bidirectional uniporter (PubMed:21128598, PubMed:9687576). Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient (PubMed:15212162, PubMed:9260930, PubMed:9687576). However, may also engage electroneutral cation exchange when saturating concentrations of cation substrates are reached (By similarity). Predominantly expressed at the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds by hepatic and renal clearance from the blood flow (PubMed:15783073). Implicated in monoamine neurotransmitters uptake such as histamine, dopamine, adrenaline/epinephrine, noradrenaline/norepinephrine, serotonin and tyramine, thereby supporting a physiological role in the central nervous system by regulating interstitial concentrations of neurotransmitters (PubMed:16581093, PubMed:17460754, PubMed:9687576). Also capable of transporting dopaminergic neuromodulators cyclo(his-pro), salsolinol and N-methyl-salsolinol, thereby involved in the maintenance of dopaminergic cell integrity in the central nervous system (PubMed:17460754). Mediates the bidirectional transport of acetylcholine (ACh) at the apical membrane of ciliated cell in airway epithelium, thereby playing a role in luminal release of ACh from bronchial epithelium (PubMed:15817714). Also transports guanidine and endogenous monoamines such as vitamin B1/thiamine, creatinine and N-1-methylnicotinamide (NMN) (PubMed:12089365, PubMed:15212162, PubMed:17072098, PubMed:24961373, PubMed:9260930). Mediates the uptake and efflux of quaternary ammonium compound choline (PubMed:9260930). Mediates the bidirectional transport of polyamine agmatine and the uptake of polyamines putrescine and spermidine (PubMed:12538837, PubMed:21128598). Able to transport non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) (PubMed:11907186). Also involved in the uptake of xenobiotic 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) (PubMed:12395288, PubMed:16394027). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
- Specific Function
- acetylcholine transmembrane transporter activity
- Gene Name
- SLC22A2
- Uniprot ID
- O15244
- Uniprot Name
- Solute carrier family 22 member 2
- Molecular Weight
- 62579.99 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Transporter that mediates the transport of endogenous and microbial zwitterions and organic cations (PubMed:10215651, PubMed:15107849, PubMed:15795384, PubMed:16729965, PubMed:20601551, PubMed:22206629, PubMed:22569296, PubMed:29530864). Functions as a Na(+)-dependent and pH-dependent high affinity microbial symporter of potent food-derived antioxidant ergothioeine (PubMed:15795384, PubMed:29530864, PubMed:33124720). Transports one sodium ion with one ergothioeine molecule (By similarity). Involved in the absorption of ergothioneine from the luminal/apical side of the small intestine and renal tubular cells, and into non-parenchymal liver cells, thereby contributing to maintain steady-state ergothioneine level in the body (PubMed:20601551). Also mediates the bidirectional transport of acetycholine, although the exact transport mechanism has not been fully identified yet (PubMed:22206629). Most likely exports anti-inflammatory acetylcholine in non-neuronal tissues, thereby contributing to the non-neuronal cholinergic system (PubMed:22206629, PubMed:22569296). Displays a general physiological role linked to better survival by controlling inflammation and oxidative stress, which may be related to ergothioneine and acetycholine transports (PubMed:15795384, PubMed:22206629). May also function as a low-affinity Na(+)-dependent transporter of L-carnitine through the mitochondrial membrane, thereby maintaining intracellular carnitine homeostasis (PubMed:10215651, PubMed:15107849, PubMed:16729965). May contribute to regulate the transport of cationic compounds in testis across the blood-testis-barrier (PubMed:35307651)
- Specific Function
- acetylcholine transmembrane transporter activity
- Gene Name
- SLC22A4
- Uniprot ID
- Q9H015
- Uniprot Name
- Solute carrier family 22 member 4
- Molecular Weight
- 62154.48 Da
References
- 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. [Article]
Drug created at June 13, 2005 13:24 / Updated at October 13, 2024 03:36