Explore a selection of our essential drug information below, or:
Identification
- Summary
Minoxidil is an antihypertensive vasodilating agent used for resistant hypertension that is symptomatic or has caused end organ damage.
- Brand Names
- Loniten, Minox, Regoxidine, Rogaine
- Generic Name
- Minoxidil
- DrugBank Accession Number
- DB00350
- Background
A potent direct-acting peripheral vasodilator (vasodilator agents) that reduces peripheral resistance and produces a fall in blood pressure.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Minoxidil (DB00350)
- Weight
- Average: 209.2483
Monoisotopic: 209.127660127 - Chemical Formula
- C9H15N5O
- Synonyms
- 2,4-Diamino-6-piperidinopyrimidine 3-oxide
- 6-Piperidin-1-ylpyrimidine-2,4-diamine 3-oxide
- Minossidile
- Minoxidil
- Minoxidilum
- External IDs
- U-10,858
- U-10858
Pharmacology
- Indication
For the treatment of severe hypertension and in the topical treatment (regrowth) of androgenic alopecia in males and females and stabilisation of hair loss in patients with androgenic alopecia.
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 Treatment of Androgenic alopecia •••••••••••• Treatment of Severe, symptomatic hypertension •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Minoxidil is an orally effective direct acting peripheral vasodilator that reduces elevated systolic and diastolic blood pressure by decreasing peripheral vascular resistance. Minoxidil is also used topically to treat androgenetic alopecia. Microcirculatory blood flow in animals is enhanced or maintained in all systemic vascular beds. In man, forearm and renal vascular resistance decline; forearm blood flow increases while renal blood flow and glomerular filtration rate are preserved. The predominant site of minoxidil action is arterial. Venodilation does not occur with minoxidil; thus, postural hypotension is unusual with its administration. The antihypertensive activity of minoxidil is due to its sulphate metabolite, minoxidil sulfate.
- Mechanism of action
Minoxidil is thought to promote the survival of human dermal papillary cells (DPCs) or hair cells by activating both extracellular signal-regulated kinase (ERK) and Akt and by preventing cell death by increasing the ratio of BCl-2/Bax. Minoxidil may stimulate the growth of human hairs by prolonging anagen through these proliferative and anti-apoptotic effects on DPCs. Minoxidil, when used as a vasodilator, acts by opening adenosine triphosphate-sensitive potassium channels in vascular smooth muscle cells. This vasodilation may also improve the viability of hair cells or hair follicles.
Target Actions Organism AATP-sensitive inward rectifier potassium channel 1 inducerHumans URenin Not Available Humans UProstaglandin G/H synthase 1 inducerHumans - Absorption
Minoxidil is at least 90% absorbed from the GI tract in experimental animals and man.
- Volume of distribution
Not Available
- Protein binding
Minoxidil does not bind to plasma proteins.
- Metabolism
Approximately 90% of the administered drug is metabolized, predominantly by conjugation with glucuronic acid at the N-oxide position in the pyrimidine ring, but also by conversion to more polar products. Known metabolites exert much less pharmacologic effect than minoxidil itself.
- Route of elimination
Not Available
- Half-life
4.2 hours
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Oral LD50 in rats has ranged from 1321-3492 mg/kg; in mice, 2456-2648 mg/kg. Side effects include cardiovascular effects associated with hypotension such as sudden weight gain, rapid heart beat, faintness or dizziness.
- Pathways
- Not Available
- 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 softwareAbaloparatide The risk or severity of adverse effects can be increased when Minoxidil is combined with Abaloparatide. Acebutolol Minoxidil may increase the hypotensive activities of Acebutolol. Aceclofenac The therapeutic efficacy of Minoxidil can be decreased when used in combination with Aceclofenac. Acemetacin The therapeutic efficacy of Minoxidil can be decreased when used in combination with Acemetacin. Acetylsalicylic acid Acetylsalicylic acid may decrease the antihypertensive activities of Minoxidil. - Food Interactions
- Take with or without food. The absorption is unaffected by food.
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 Minoxidil sulfate HM46T3593Q 210357-39-4 AGMYAAIWWVATKU-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Alostil (McNeil) / Apo-Gain (Apotex) / Avogain / Lipogaine / Lonolox (Pfizer) / Minodyl / Minoximen (Menarini) / Mintop (Dr. Reddy's) / Normoxidil / Regaine (McNeil) / Rogaine (Johnson & Johnson) / Theroxidil (Ei) / Tricoxidil / Vanarex
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Loniten Tablet 2.5 mg/1 Oral Pharmacia & Upjohn Inc 1979-11-01 2005-10-31 US 
Loniten Tablet 10 mg/1 Oral Pharmacia & Upjohn Inc 1979-11-01 2005-06-30 US Loniten 10mg Tablet 10 mg Oral Pfizer Canada Ulc 1980-12-31 Not applicable Canada 
Loniten 2.5mg Tablet 2.5 mg Oral Pfizer Canada Ulc 1980-12-31 Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Minoxidil Tablet 10 mg/1 Oral AvKARE 2013-08-01 Not applicable US Minoxidil Tablet 2.5 mg/1 Oral Remedy Repack 2011-01-13 2013-10-30 US Minoxidil Tablet 10 mg/1 Oral Golden State Medical Supply, Inc. 1988-11-14 Not applicable US Minoxidil Tablet 2.5 mg/1 Oral Avera McKennan Hospital 2015-08-21 2017-05-24 US 
Minoxidil Tablet 2.5 mg/1 Oral Ncs Health Care Of Ky, Inc Dba Vangard Labs 1988-11-14 Not applicable US - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image 2% Minoxidil hair growth oil Liquid 2 g/100mL Topical EUbizrival LLC 2023-11-02 Not applicable US 2% Minoxidil Hair regrowth serum Spray 2 g/100mL Topical good manager holdings inc. 2023-03-01 Not applicable US 3RX Minoxidil HAIR REGROWTH TREATMENT FOR MEN Liquid 5 g/100mL Topical Shenzhen Youbente E-commerce Co., Ltd 2024-06-18 Not applicable US 5% Minoxidil Oil 5 g/100mL Topical Shenzhen Lancity Information Technology Co., Ltd 2023-12-22 Not applicable US 5% Minoxidil Beard Growth Serum Liquid 5 g/100mL Topical Shenzhen Huiyuan Trading Co., Ltd. 2024-03-13 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image 5% Minoxidil Hair Growth Serum Minoxidil (5 g/100mL) + Biotin (0.3 g/100mL) + Caffeine (0.2 g/100mL) + Nicotinamide (0.2 g/100mL) Liquid Topical Guangzhou Ariel Biotech Co., Ltd. 2024-09-23 Not applicable US 5%Minoxidil Hair Growth Serum Minoxidil (5 g/100mL) + Biotin (0.3 g/100mL) + Caffeine (0.2 g/100mL) + Nicotinamide (0.2 g/100mL) Liquid Topical Guangzhou Binsi Clothing Co.,Ltd. 2024-05-30 Not applicable US Bakumokon 5% Minoxidil Minoxidil (5 mg/100mg) + Dutasteride (0.1 mg/100mg) + Oxytocin (0.01 mg/100mg) Liquid Topical DS LABORATORIES, INC. 2015-02-09 2017-10-19 US Bakumokon 7% Minoxidil Sulfate Minoxidil sulfate (7 mg/100mg) + Dutasteride (0.1 mg/100mg) + Oxytocin (0.01 mg/100mg) Liquid Topical DS LABORATORIES, INC. 2015-02-09 2017-10-11 US Cream Minoxidil (6 g/30g) + Glycerin (7.5 g/30g) + Hyaluronic acid (4.5 g/30g) + Tocopherol (7.5 g/30g) Cream Cutaneous Shantou Youjia E-Commerce Co., Ltd. 2024-02-01 2024-12-31 US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image 3RX Minoxidil HAIR REGROWTH TREATMENT FOR MEN Minoxidil (5 g/100mL) Liquid Topical Shenzhen Youbente E-commerce Co., Ltd 2024-06-18 Not applicable US 5% Minoxidil Hair growth foam Minoxidil (5 mg/100mL) Aerosol, foam Topical good manager holdings inc. 2023-03-02 Not applicable US 5% Minoxidil Hair Growth Serum Minoxidil (5 g/100mL) + Biotin (0.3 g/100mL) + Caffeine (0.2 g/100mL) + Nicotinamide (0.2 g/100mL) Liquid Topical Guangzhou Ariel Biotech Co., Ltd. 2024-09-23 Not applicable US 5% Minoxidil Topical serum Minoxidil (5 g/100mL) Liquid Topical Shenzhen Xiaomai Manufacturing Co., Ltd. 2024-01-29 Not applicable US 5% Minoxidil Topical Solution Minoxidil (5 g/100mL) Solution Topical Flpharmaceuticals LLC 2022-01-19 Not applicable US
Categories
- ATC Codes
- D11AX01 — Minoxidil
- D11AX — Other dermatologicals
- D11A — OTHER DERMATOLOGICAL PREPARATIONS
- D11 — OTHER DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- Drug Categories
- Antihypertensive Agents
- Antihypertensive Agents Indicated for Hypertension
- Arteriolar Smooth Muscle, Agents Acting On
- Arteriolar Vasodilation
- Arteriolar Vasodilator
- Cardiovascular Agents
- Dermatologicals
- Direct Vasodilators
- Hypotensive Agents
- Misc. Skin and Mucous Membrane Agents
- Piperidines
- Potassium Channel Opener
- Pyrimidine Derivatives
- Pyrimidines
- UGT1A1 Substrates
- Vasodilating Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as dialkylarylamines. These are aliphatic aromatic amines in which the amino group is linked to two aliphatic chains and one aromatic group.
- Kingdom
- Organic compounds
- Super Class
- Organic nitrogen compounds
- Class
- Organonitrogen compounds
- Sub Class
- Amines
- Direct Parent
- Dialkylarylamines
- Alternative Parents
- Aminopyrimidines and derivatives / Piperidines / Imidolactams / Heteroaromatic compounds / Azacyclic compounds / Primary amines / Organopnictogen compounds / Organic oxides / Hydrocarbon derivatives
- Substituents
- Aminopyrimidine / Aromatic heteromonocyclic compound / Azacycle / Dialkylarylamine / Heteroaromatic compound / Hydrocarbon derivative / Imidolactam / Organic oxide / Organic oxygen compound / Organoheterocyclic compound
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- piperidines, aminopyrimidine, pyrimidine N-oxide (CHEBI:6942)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 5965120SH1
- CAS number
- 38304-91-5
- InChI Key
- ZFMITUMMTDLWHR-UHFFFAOYSA-N
- InChI
- InChI=1S/C9H15N5O/c10-7-6-8(12-9(11)14(7)15)13-4-2-1-3-5-13/h6H,1-5,10H2,(H2,11,12)
- IUPAC Name
- 2,6-diamino-4-(piperidin-1-yl)pyrimidin-1-ium-1-olate
- SMILES
- NC1=CC(=NC(N)=[N+]1[O-])N1CCCCC1
References
- Synthesis Reference
Paul S. Uster, Yolanda P. Quinn, "Non-crystalline minoxidil composition, its production and application." U.S. Patent US4828837, issued March, 1985.
US4828837- General References
- Olsen EA, Whiting D, Bergfeld W, Miller J, Hordinsky M, Wanser R, Zhang P, Kohut B: A multicenter, randomized, placebo-controlled, double-blind clinical trial of a novel formulation of 5% minoxidil topical foam versus placebo in the treatment of androgenetic alopecia in men. J Am Acad Dermatol. 2007 Nov;57(5):767-74. Epub 2007 Aug 29. [Article]
- External Links
- Human Metabolome Database
- HMDB0014494
- KEGG Drug
- D00418
- PubChem Compound
- 4201
- PubChem Substance
- 46508344
- ChemSpider
- 10438564
- BindingDB
- 50237593
- 6984
- ChEBI
- 6942
- ChEMBL
- CHEMBL802
- ZINC
- ZINC000000001735
- Therapeutic Targets Database
- DAP000143
- PharmGKB
- PA450521
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- MXD
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Minoxidil
- PDB Entries
- 3b6h / 4k7a
- FDA label
- Download (145 KB)
- MSDS
- Download (73.5 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 Treatment Androgenetic Alopecia (AGA) 1 somestatus stop reason just information to hide Not Available Completed Not Available Alopecia / Female Pattern Hair Loss 1 somestatus stop reason just information to hide Not Available Completed Not Available Androgenetic Alopecia (AGA) 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 Treatment Female Pattern Hair Loss, Androgenic Alopecia 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Johnson and johnson group consumer companies
- Actavis mid atlantic llc
- Bausch and lomb pharmaceuticals inc
- Copley pharmaceutical inc
- Hi tech pharmacal co inc
- Novex pharma
- Perrigo co
- Sight pharmaceuticals inc
- Teva pharmaceuticals usa inc
- Wockhardt eu operations (swiss) ag
- Avacor products llc
- L perrigo co
- Perrigo new york inc
- Harmony laboratories
- Pharmacia and upjohn co
- Quantum pharmics ltd
- Mutual pharmaceutical co inc
- Par pharmaceutical inc
- Royce laboratories inc
- Usl pharma inc
- Watson laboratories inc
- Packagers
- Amerisource Health Services Corp.
- Atlantic Biologicals Corporation
- Comprehensive Consultant Services Inc.
- Dept Health Central Pharmacy
- Heartland Repack Services LLC
- Johnson & Johnson Healthcare
- Kaiser Foundation Hospital
- Major Pharmaceuticals
- Medisca Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Mutual Pharmaceutical Co.
- Nucare Pharmaceuticals Inc.
- Par Pharmaceuticals
- Patheon Inc.
- Perrigo Co.
- Pharmaceutical Utilization Management Program VA Inc.
- Pharmacia Inc.
- Physicians Total Care Inc.
- Prepak Systems Inc.
- Remedy Repack
- Southwood Pharmaceuticals
- Vangard Labs Inc.
- Watson Pharmaceuticals
- Dosage Forms
Form Route Strength Oil Topical 5 g/100mL Spray, suspension Topical 5 g/100g Aerosol, foam Topical 5 mg/100mL Spray Topical 5 mg/100mL Spray Topical Solution Topical Spray Topical 5 % Solution Topical 5.000 g Aerosol, foam Topical Aerosol, foam Topical 20 mg/g Aerosol, foam Topical 50 mg/g Solution Topical 20 mg/g Solution Topical 50 mg/g Aerosol Topical 5.000 g Solution Topical 5 %w/v Solution / drops Topical 2 g/100mL Solution / drops Topical 5 g/100mL Liquid Topical Solution Topical 0.05 mg/1mL Spray Topical 2 % Liquid Topical 5 g/100mL Spray Cutaneous Cream Cutaneous Liquid Topical 2 mg/100mL Aerosol Topical 5.00 g Solution Topical 5.0000 g Gel Topical 5 g/100g Gel Topical 5 mg/100mL Aerosol Topical 5 g Aerosol Topical 500000 g Liquid Topical 5 g/100g Liquid Topical 2 g/100g Solution Cutaneous 5.000 g Solution Cutaneous 5.00 g Solution Cutaneous 2 g Liquid Topical 5 mg/100mL Liquid Topical 2 % Spray Topical 5 g/100g Lotion Topical 2 % w/v Lotion Topical 5 % w/v Spray Topical Aerosol, foam Topical 2 g/100mL Solution Topical 20 mg / mL Oil Topical 0.05 g/1mL Solution Topical 3 g/60mL Solution Topical 5 % w/v Liquid Topical 20 mg/1mL Spray Topical 2 g/100mL Liquid Topical 0.05 g/1mL Liquid Cutaneous Tablet Oral 2.5 mg Tablet Oral Lotion Topical 2 g Liquid Topical 5 % w/v Aerosol, foam Topical 5 % Liquid Topical 50 mg/1mL Solution Topical 50 mg/1mL Kit; solution Topical 50 mg/1mL Aerosol, foam Topical 50 mg/1g Lotion Topical Aerosol, foam Topical 2 % Aerosol, foam Topical 50 mg/1mL Powder Not applicable 1 g/1g Solution Topical 2 g/100mL Tablet Oral 10 mg/1 Tablet Oral 2.5 mg/1 Solution Topical 2 g Solution Topical 5000 mg Solution Topical Solution Topical 5 g Aerosol, foam Topical Lotion Topical 3 % w/v Solution Topical 20 g/1mL Liquid Cutaneous 5 g/100mL Solution Topical 50 mg/ml Solution Topical 2 % Kit; solution Topical 5 g/100mL Kit Topical 2 g/100mL Solution Topical 5 g/100mL Solution Topical 0.05 g/1mL Liquid Topical 2 g/100mL Cream Topical 2 g Gel Topical 5 g Gel Topical 2 g Shampoo Topical 1.5 g/100mL Aerosol Cutaneous 5.000 g Spray Topical 50 mg/ml Aerosol, foam Topical 50 mg/50mg Liquid Topical 50 mg/50mg Aerosol, foam Gel Topical Aerosol, foam Cutaneous Solution Topical 5 % Solution Topical 20 mg/ml Liquid Topical 5 mg/1mL Lotion Topical 5 % Lotion Topical 3 % Lotion Topical 5 g Lotion Topical 20 mg/ml Lotion Topical 50 mg/ml Gel Extracorporeal 5 g/100mL Spray Topical 5 g/10mL Solution Topical 5 mg/100mL Solution Topical 2 mg/100mL Aerosol, foam Topical 5 g/100g Solution Cutaneous 5.000 g Solution Topical 0.02 g/1mL Cream Topical 5 g/100g Spray Topical 5 g/100mL Solution Topical 20 mg/1mL Solution Topical 2 g/100g Solution Topical 5 g/100g Solution Topical 2 % w/v Aerosol, foam Topical 5 % w/w Kit; liquid Topical 20 mg/1mL Liquid Topical 6 g/100mL Tablet Oral 10 mg Tablet Oral 5 mg - Prices
Unit description Cost Unit Rogaine ex-str starter kit 28.32USD kit Minoxidil powder 2.07USD g Loniten 10 mg Tablet 1.52USD tablet Minoxidil 10 mg tablet 1.32USD tablet Minoxidil 2.5 mg tablet 0.7USD tablet Loniten 2.5 mg Tablet 0.39USD tablet Rogaine 5 % foam 0.27USD g DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US6946120 No 2005-09-20 2019-04-20 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 248 °C PhysProp water solubility 2200 mg/L MERCK INDEX (1996) logP 1.24 HANSCH,C ET AL. (1995) pKa 4.61 MERCK INDEX (2001) - Predicted Properties
Property Value Source Water Solubility 19.9 mg/mL ALOGPS logP 1.24 ALOGPS logP 0.00079 Chemaxon logS -1 ALOGPS pKa (Strongest Acidic) 17.62 Chemaxon pKa (Strongest Basic) 1.69 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 95.11 Å2 Chemaxon Rotatable Bond Count 1 Chemaxon Refractivity 60.42 m3·mol-1 Chemaxon Polarizability 21.97 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9945 Blood Brain Barrier + 0.9496 Caco-2 permeable + 0.7214 P-glycoprotein substrate Substrate 0.596 P-glycoprotein inhibitor I Non-inhibitor 0.8959 P-glycoprotein inhibitor II Non-inhibitor 0.8453 Renal organic cation transporter Non-inhibitor 0.5721 CYP450 2C9 substrate Non-substrate 0.8761 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Non-substrate 0.6099 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.907 CYP450 2D6 inhibitor Non-inhibitor 0.923 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6999 Ames test AMES toxic 0.5253 Carcinogenicity Non-carcinogens 0.9006 Biodegradation Not ready biodegradable 0.9616 Rat acute toxicity 2.2308 LD50, mol/kg Not applicable hERG inhibition (predictor I) Strong inhibitor 0.678 hERG inhibition (predictor II) Inhibitor 0.7016
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 153.650814 predictedDarkChem Lite v0.1.0 [M-H]- 153.514614 predictedDarkChem Lite v0.1.0 [M-H]- 146.2263 predictedDeepCCS 1.0 (2019) [M+H]+ 153.313614 predictedDarkChem Lite v0.1.0 [M+H]+ 153.241514 predictedDarkChem Lite v0.1.0 [M+H]+ 148.6219 predictedDeepCCS 1.0 (2019) [M+Na]+ 153.791214 predictedDarkChem Lite v0.1.0 [M+Na]+ 154.53441 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inducer
- General Function
- In the kidney, probably plays a major role in potassium homeostasis. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward rectification is mainly due to the blockage of outward current by internal magnesium. This channel is activated by internal ATP and can be blocked by external barium
- Specific Function
- ATP binding
- Gene Name
- KCNJ1
- Uniprot ID
- P48048
- Uniprot Name
- ATP-sensitive inward rectifier potassium channel 1
- Molecular Weight
- 44794.6 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Kirsten R, Nelson K, Kirsten D, Heintz B: Clinical pharmacokinetics of vasodilators. Part I. Clin Pharmacokinet. 1998 Jun;34(6):457-82. [Article]
- Evans JM, Allan AK, Davies SA, Dow JA: Sulphonylurea sensitivity and enriched expression implicate inward rectifier K+ channels in Drosophila melanogaster renal function. J Exp Biol. 2005 Oct;208(Pt 19):3771-83. [Article]
- Loffler-Walz C, Quast U: Binding of K(ATP) channel modulators in rat cardiac membranes. Br J Pharmacol. 1998 Apr;123(7):1395-402. [Article]
- Bray KM, Quast U: A specific binding site for K+ channel openers in rat aorta. J Biol Chem. 1992 Jun 15;267(17):11689-92. [Article]
- Black KL, Yin D, Konda BM, Wang X, Hu J, Ko MK, Bayan JA, Sacapano MR, Espinoza AJ, Ong JM, Irvin D, Shu Y: Different effects of KCa and KATP agonists on brain tumor permeability between syngeneic and allogeneic rat models. Brain Res. 2008 Aug 28;1227:198-206. doi: 10.1016/j.brainres.2008.06.046. Epub 2008 Jun 21. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Renin is a highly specific endopeptidase, whose only known function is to generate angiotensin I from angiotensinogen in the plasma, initiating a cascade of reactions that produce an elevation of blood pressure and increased sodium retention by the kidney
- Specific Function
- aspartic-type endopeptidase activity
- Gene Name
- REN
- Uniprot ID
- P00797
- Uniprot Name
- Renin
- Molecular Weight
- 45057.125 Da
References
- Werning C: The effect of minoxidil on blood pressure and plasma renin activity in patients with essential and renal hypertension. Klin Wochenschr. 1976 Aug 1;54(15):727-34. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Dual cyclooxygenase and peroxidase that plays an important role in the biosynthesis pathway of prostanoids, a class of C20 oxylipins mainly derived from arachidonate ((5Z,8Z,11Z,14Z)-eicosatetraenoate, AA, C20:4(n-6)), with a particular role in the inflammatory response. The cyclooxygenase activity oxygenates AA to the hydroperoxy endoperoxide prostaglandin G2 (PGG2), and the peroxidase activity reduces PGG2 to the hydroxy endoperoxide prostaglandin H2 (PGH2), the precursor of all 2-series prostaglandins and thromboxanes. This complex transformation is initiated by abstraction of hydrogen at carbon 13 (with S-stereochemistry), followed by insertion of molecular O2 to form the endoperoxide bridge between carbon 9 and 11 that defines prostaglandins. The insertion of a second molecule of O2 (bis-oxygenase activity) yields a hydroperoxy group in PGG2 that is then reduced to PGH2 by two electrons (PubMed:7947975). Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the generation of thromboxane A2 (TXA2), which promotes platelet activation and aggregation, vasoconstriction and proliferation of vascular smooth muscle cells (Probable). Can also use linoleate (LA, (9Z,12Z)-octadecadienoate, C18:2(n-6)) as substrate and produce hydroxyoctadecadienoates (HODEs) in a regio- and stereospecific manner, being (9R)-HODE ((9R)-hydroxy-(10E,12Z)-octadecadienoate) and (13S)-HODE ((13S)-hydroxy-(9Z,11E)-octadecadienoate) its major products (By similarity)
- Specific Function
- heme binding
- Gene Name
- PTGS1
- Uniprot ID
- P23219
- Uniprot Name
- Prostaglandin G/H synthase 1
- Molecular Weight
- 68685.82 Da
References
- Kurbel S, Kurbel B, Zanic-Matanic D: Minoxidil and male-pattern alopecia: a potential role for a local regulator of sebum secretion with vasoconstrictive effects? Med Hypotheses. 1999 Nov;53(5):402-6. [Article]
- Gaffar A, Scherl D, Afflitto J, Coleman EJ: The effect of triclosan on mediators of gingival inflammation. J Clin Periodontol. 1995 Jun;22(6):480-4. [Article]
- Michelet JF, Commo S, Billoni N, Mahe YF, Bernard BA: Activation of cytoprotective prostaglandin synthase-1 by minoxidil as a possible explanation for its hair growth-stimulating effect. J Invest Dermatol. 1997 Feb;108(2):205-9. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- UDP-glucuronosyltransferase (UGT) that catalyzes phase II biotransformation reactions in which lipophilic substrates are conjugated with glucuronic acid to increase the metabolite's water solubility, thereby facilitating excretion into either the urine or bile (PubMed:12181437, PubMed:15472229, PubMed:18004206, PubMed:18004212, PubMed:18719240, PubMed:19830808, PubMed:23288867). Essential for the elimination and detoxification of drugs, xenobiotics and endogenous compounds (PubMed:12181437, PubMed:18004206, PubMed:18004212). Catalyzes the glucuronidation of endogenous estrogen hormones such as estradiol, estrone and estriol (PubMed:15472229, PubMed:18719240, PubMed:23288867). Involved in the glucuronidation of bilirubin, a degradation product occurring in the normal catabolic pathway that breaks down heme in vertebrates (PubMed:17187418, PubMed:18004206, PubMed:19830808, PubMed:24525562). Also catalyzes the glucuronidation the isoflavones genistein, daidzein, glycitein, formononetin, biochanin A and prunetin, which are phytoestrogens with anticancer and cardiovascular properties (PubMed:18052087, PubMed:19545173). Involved in the glucuronidation of the AGTR1 angiotensin receptor antagonist losartan, a drug which can inhibit the effect of angiotensin II (PubMed:18674515). Involved in the biotransformation of 7-ethyl-10-hydroxycamptothecin (SN-38), the pharmacologically active metabolite of the anticancer drug irinotecan (PubMed:12181437, PubMed:18004212, PubMed:20610558)
- Specific Function
- enzyme binding
- Gene Name
- UGT1A1
- Uniprot ID
- P22309
- Uniprot Name
- UDP-glucuronosyltransferase 1A1
- Molecular Weight
- 59590.91 Da
References
- Uchaipichat V, Mackenzie PI, Guo XH, Gardner-Stephen D, Galetin A, Houston JB, Miners JO: Human udp-glucuronosyltransferases: isoform selectivity and kinetics of 4-methylumbelliferone and 1-naphthol glucuronidation, effects of organic solvents, and inhibition by diclofenac and probenecid. Drug Metab Dispos. 2004 Apr;32(4):413-23. doi: 10.1124/dmd.32.4.413. [Article]
- Canadian DPD Label - LONITEN (minoxidil) [File]
Drug created at June 13, 2005 13:24 / Updated at October 07, 2024 17:27