Identification
- Summary
Ketotifen is a histamine H1 receptor blocker and mast cell stabilizer used to treat mild atopic asthma and allergic conjunctivitis.
- Brand Names
- Alaway, Zaditen, Zaditor
- Generic Name
- Ketotifen
- DrugBank Accession Number
- DB00920
- Background
Ketotifen is a benzocycloheptathiophene derivative3 with potent antihistaminic and mast cell stabilizing properties. It has a similar structure to some other first-generation antihistamines such as cyproheptadine and azatadine.3
Ketotifen was first developed in Switzerland in 1970 by Sandoz Pharmaceuticals and was initially marketed for the treatment of anaphylaxis.3 In the US, it is now used in an over-the-counter ophthalmic formulation for the treatment of itchy eyes associated with allergies,6 and in Canada a prescription-only oral formulation is available and indicated as an add-on therapy for children with atopic asthma.7 In addition, oral ketotifen is used in Mexico and across Europe for the treatment of various allergic symptoms and disorders,3 including urticaria, mastocytosis, and food allergy.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Ketotifen (DB00920)
- Weight
- Average: 309.425
Monoisotopic: 309.118734925 - Chemical Formula
- C19H19NOS
- Synonyms
- Ketotifen
- Ketotifene
- Ketotifeno
- Ketotifenum
Pharmacology
- Indication
Administered orally, ketotifen is indicated as an add-on medication in the chronic treatment of mild atopic asthma in children.7 It is also available as an over-the-counter ophthalmic solution which is indicated for the temporary prevention of itching of the eye due to allergic conjunctivitis.6
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 Symptomatic treatment of Allergic rhinitis (ar) •••••••••••• ••••••• ••••••• Adjunct therapy in management of Atopic asthma •••••••••••• ••••••••• •••••• Symptomatic treatment of Eye pruritus ••• ••• •••••••• • ••••• Prevention of Seasonal allergic conjunctivitis •••••••••••• Treatment of Seasonal allergic conjunctivitis •••••••••••• - 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
Ketotifen is a non-competitive histamine antagonist and mast cell stabilizer.6 Administered orally, it functions as a non-bronchodilator antiasthmatic drug by inhibiting the effects of endogenous substances known to be inflammatory mediators.7 While effects can take 6 to 12 weeks to become apparent,5 the use of ketotifen has been demonstrated to reduce the frequency, severity, and duration of asthma symptoms, and may allow for a reduction in the use of other asthma therapies.7
- Mechanism of action
The precise mechanism(s) through which ketotifen exerts its therapeutic effects are unclear. Ketotifen is a potent and non-competitive antagonist of H1 histamine receptors, which is likely to be a significant contributor to its anti-allergic activity.7 In addition, ketotifen stabilizes mast cells and has demonstrated in vitro the ability to inhibit the release of allergic and inflammatory mediators such as histamine, leukotrienes C4 and D4 (i.e. SRS-A), and platelet-activating factor (PAF).7
Other in vivo observations thought to contribute to ketotifen's efficacy in asthma include the inhibition of various PAF-mediated processes (e.g. airway hyperreactivity, eosinophil and platelet accumulation in the airways), prevention of leukotriene-induced bronchoconstriction, and suppression of eosinophil priming.7
Target Actions Organism AHistamine H1 receptor antagonistHumans U6-phosphogluconate dehydrogenase, decarboxylating inhibitorHumans - Absorption
Following oral administration, absorption is relatively quick (with a Tmax of ~3 hours) and nearly complete as judged by plasma concentrations and urinary excretion levels - despite this, oral bioavailability is only ~50% due to a significant first-pass effect in the liver.7
- Volume of distribution
Not Available
- Protein binding
Ketotifen is 75% protein-bound in plasma, though the specific proteins to which it binds are unclear.7
- Metabolism
Ketotifen is extensively metabolized in humans5 and three distinct metabolites have been detected in human urine. The main metabolite is the N-glucuronide, comprising roughly 50% of urinary drug product,5 with the N-demethylated nor-ketotifen and the 10-hydroxyl derivative comprising 2% and <1%, respectively.7 Nor-ketotifen appears to be equally as active as its parent drug,7 though the clinical relevance of this is unclear given the relatively small proportion in which nor-ketotifen is found in the plasma.
Formation of the N-glucuronide metabolite is carried out by several UGT enzymes, including UGT1A3, UGT1A4, and UGT2B10.2
Hover over products below to view reaction partners
- Route of elimination
More than 60% of an administered dose is excreted in the urine, primarily as metabolites7 - of this material, <1% is found as unchanged drug, while the glucuronide and pharmacologically active nor-ketotifen metabolites account for 50% and 10%, respectively.5
- Half-life
Ketotifen clearance is biphasic - the half-life of the distribution phase is approximately 3-5 hours and the half-life of the elimination phase is 22 hours.5
- Clearance
Not Available
- Adverse Effects
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Oral ingestion of up to 60x the recommended dose has been reported, although no fatal overdoses of ketotifen have been described.4 Symptoms of ketotifen overdosage may include significant sedation, confusion, disorientation, tachycardia, hypotension, convulsions, hyperexcitability (particularly in children), and/or reversible coma.7 If ingestion is recent, consider the use of gastric lavage or activated charcoal.7 Other treatments should be supportive and administered as necessary based on symptoms.
Physostigmine may be useful to mitigate anticholinergic effects, and short-acting barbiturates or benzodiazepines may be used if the patient presents with excitation or convulsions.7
- Pathways
Pathway Category Ketotifen H1-Antihistamine Action Drug action - Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAcarbose The risk or severity of thrombocytopenia can be increased when Acarbose is combined with Ketotifen. Acetohexamide The risk or severity of thrombocytopenia can be increased when Acetohexamide is combined with Ketotifen. Alogliptin The risk or severity of thrombocytopenia can be increased when Alogliptin is combined with Ketotifen. Amphetamine Amphetamine may decrease the sedative activities of Ketotifen. Benzphetamine Benzphetamine may decrease the sedative activities of Ketotifen. - Food Interactions
- Take with or without food. The co-administration of food does not significantly affect ketotifen disposition.
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 Ketotifen fumarate HBD503WORO 34580-14-8 YNQQEYBLVYAWNX-WLHGVMLRSA-N - International/Other Brands
- Totifen (Patron) / Zasten (Novartis)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ketotifen Ophthalmic Solution Solution 0.25 mg / mL Ophthalmic Sterimax Inc 2013-03-07 Not applicable Canada 
Zaditen Syrup 1 mg / 5 mL Oral TEVA Canada Limited 1990-12-31 2021-07-30 Canada Zaditen Tablet 1 mg Oral TEVA Canada Limited 1990-12-31 Not applicable Canada Zaditen - Dps 1mg/ml Solution / drops 1 mg / mL Oral Novartis Not applicable Not applicable Canada Zaditor Solution 0.25 mg / mL Ophthalmic Novartis 2006-08-03 2012-01-17 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-ketotifen - Syr 1mg/5ml Syrup 1 mg / 5 mL Oral Apotex Corporation 1996-11-07 2019-01-16 Canada Jamp Ketotifen Ophthalmic Solution 0.25 mg / mL Ophthalmic Jamp Pharma Corporation Not applicable Not applicable Canada Jamp-ketotifen Solution 0.25 mg / mL Ophthalmic Jamp Pharma Corporation Not applicable Not applicable Canada Novo-ketotifen - Syr 1mg/5ml Syrup 1 mg / 5 mL Oral Novopharm Limited 1995-12-31 2015-10-26 Canada Novo-ketotifen Tab 1mg Tablet 1 mg Oral Novopharm Limited 1997-07-29 2013-02-11 Canada - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Alaway Solution / drops 0.25 mg/1mL Ophthalmic Bausch & Lomb Incorporated 2006-12-01 Not applicable US 
Alaway Preservative Free Solution / drops 0.35 mg/1mL Ophthalmic Bausch & Lomb Incorporated 2020-09-24 Not applicable US Allergy Eye Solution / drops 0.25 mg/1mL Ophthalmic CVS Health 2011-01-07 2014-07-01 US Allergy Eye Solution / drops 0.25 mg/1mL Ophthalmic H.E.B. 2010-09-15 2015-05-01 US Allergy Eye Drops Solution / drops 0.35 mg/1mL Ophthalmic H E B 2014-02-25 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Alaway Ketotifen fumarate (0.25 mg/1mL) + Ketotifen fumarate (0.25 mg/1mL) Solution Ophthalmic Bausch & Lomb Incorporated 2006-12-01 2015-09-30 US Alaway Ketotifen fumarate (0.25 mg/1mL) + Ketotifen fumarate (0.25 mg/1mL) Solution Ophthalmic Bausch & Lomb Incorporated 2006-12-01 2015-09-30 US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Zaditor Ketotifen fumarate (0.345 mg/1mL) Solution Ophthalmic Physicians Total Care, Inc. 2002-11-04 2010-12-29 US
Categories
- ATC Codes
- S01GX08 — Ketotifen
- S01GX — Other antiallergics
- S01G — DECONGESTANTS AND ANTIALLERGICS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- Drug Categories
- Anti-Allergic Agents
- Anti-Asthmatic Agents
- Antihistamine Drugs
- Antihistamines for Systemic Use
- Antipruritics
- Decongestants and Antiallergics
- Histamine Agents
- Histamine Antagonists
- Histamine H1 Antagonists
- Histamine H1 Inhibitors
- Ophthalmologicals
- Other Antihistamines
- Piperidines
- Sensory Organs
- Sulfur Compounds
- Thiophenes
- UGT1A3 substrates
- UGT1A4 substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as cycloheptathiophenes. These are polycyclic compounds containing a thiophene ring fused to a 7 member carbocyclic moiety. Thiophene is 5-membered ring consisting of four carbon atoms and one sulfur atom.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Cycloheptathiophenes
- Sub Class
- Not Available
- Direct Parent
- Cycloheptathiophenes
- Alternative Parents
- Aryl alkyl ketones / Piperidines / Benzenoids / Thiophenes / Heteroaromatic compounds / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Organic oxides / Hydrocarbon derivatives
- Substituents
- Amine / Aromatic heteropolycyclic compound / Aryl alkyl ketone / Aryl ketone / Azacycle / Benzenoid / Cycloheptathiophene / Heteroaromatic compound / Hydrocarbon derivative / Ketone
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- X49220T18G
- CAS number
- 34580-13-7
- InChI Key
- ZCVMWBYGMWKGHF-UHFFFAOYSA-N
- InChI
- InChI=1S/C19H19NOS/c1-20-9-6-13(7-10-20)18-15-5-3-2-4-14(15)12-17(21)19-16(18)8-11-22-19/h2-5,8,11H,6-7,9-10,12H2,1H3
- IUPAC Name
- 2-(1-methylpiperidin-4-ylidene)-6-thiatricyclo[8.4.0.0^{3,7}]tetradeca-1(14),3(7),4,10,12-pentaen-8-one
- SMILES
- CN1CCC(CC1)=C1C2=C(SC=C2)C(=O)CC2=CC=CC=C12
References
- Synthesis Reference
Roy W. Bryant, Ravi Parihar, Thomas Rowe, Susan Caballa, "Methods of Making and Using Stable Pharmaceutical Compositions Comprising Ketotifen and Naphazoline." U.S. Patent US20110312998, issued December 22, 2011.
US20110312998- General References
- Hawes EM: N+-glucuronidation, a common pathway in human metabolism of drugs with a tertiary amine group. Drug Metab Dispos. 1998 Sep;26(9):830-7. [Article]
- Kato Y, Izukawa T, Oda S, Fukami T, Finel M, Yokoi T, Nakajima M: Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4. Drug Metab Dispos. 2013 Jul;41(7):1389-97. doi: 10.1124/dmd.113.051565. Epub 2013 Apr 23. [Article]
- Sokol KC, Amar NK, Starkey J, Grant JA: Ketotifen in the management of chronic urticaria: resurrection of an old drug. Ann Allergy Asthma Immunol. 2013 Dec;111(6):433-6. doi: 10.1016/j.anai.2013.10.003. Epub 2013 Oct 25. [Article]
- Jeffreys DB, Volans GN: Ketotifen overdose: surveillance of the toxicity of a new drug. Br Med J (Clin Res Ed). 1981 May 30;282(6278):1755-6. doi: 10.1136/bmj.282.6278.1755. [Article]
- Grant SM, Goa KL, Fitton A, Sorkin EM: Ketotifen. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in asthma and allergic disorders. Drugs. 1990 Sep;40(3):412-48. doi: 10.2165/00003495-199040030-00006. [Article]
- FDA Approved Drug Products: Zaditor (ketotifen fumarate) ophthalmic solution [Link]
- Health Canada Product Monograph: Zaditen (ketotifen fumarate) for oral administration [Link]
- External Links
- Human Metabolome Database
- HMDB0015056
- KEGG Drug
- D01332
- PubChem Compound
- 3827
- PubChem Substance
- 46508921
- ChemSpider
- 3695
- BindingDB
- 94597
- 6146
- ChEBI
- 92511
- ChEMBL
- CHEMBL534
- ZINC
- ZINC000000004351
- Therapeutic Targets Database
- DAP000329
- PharmGKB
- PA450152
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Ketotifen
- FDA label
- Download (9.05 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Treatment Asthma 1 4 Completed Treatment Seasonal Allergic Conjunctivitis 1 4 Not Yet Recruiting Treatment Hepatic Disease 1 4 Not Yet Recruiting Treatment ST Segment Elevation Myocardial Infarction (STEMI) 1 4 Unknown Status Treatment Dengue Fever / Pleural Effusions 1
Pharmacoeconomics
- Manufacturers
- Bausch and lomb inc
- Akorn inc
- Alcon inc
- Apotex inc etobicoke site
- Novartis pharmaceuticals corp
- Packagers
- Akorn Inc.
- Allergan Inc.
- Apotex Inc.
- Bausch & Lomb Inc.
- Ciba Vision Canada Inc.
- Novartis AG
- Physicians Total Care Inc.
- Spectrum Pharmaceuticals
- Dosage Forms
Form Route Strength Solution Ophthalmic Solution Ophthalmic 0.25 mg/mL Solution / drops Ophthalmic 0.35 mg/1mL Tablet, extended release Oral Syrup Oral 27.503 mg Syrup Oral 100 ml Syrup Oral Solution / drops Ophthalmic Solution Ophthalmic 0.25 g/1mL Solution Ophthalmic 0.25 mg/1mL Solution Oral 1.000 mg Solution Ophthalmic 0.250 mg Solution Ophthalmic 0.688 mg Solution Ophthalmic 0.25 mg Solution Conjunctival; Ophthalmic 0.5 mg Solution / drops Ophthalmic 0.25 MG/ML Solution Oral 27.6 mg Capsule Oral 1 mg Gel Ophthalmic Solution Ophthalmic 0.35 mg/1mL Solution / drops Ophthalmic 250 Mikrogramm/ml Solution Oral 20 mg Syrup Oral 0.02 g Syrup Oral 20 mg Syrup Oral 0.0275 g Solution Ophthalmic 0.5 mg Solution / drops Ophthalmic 0.345 mg/1mL Syrup Oral 1 mg / 5 mL Solution / drops Ophthalmic 0.1 mg/mL Tablet Oral 1 MG Tablet Oral Solution / drops Oral 2 MG/ML Tablet, soluble Oral 1 MG Solution / drops Oral Tablet, soluble Oral Solution Ophthalmic .25 mg/1mL Capsule Oral Solution Conjunctival; Ophthalmic 0.25 mg Syrup Oral 0.2 MG/ML Tablet, extended release Oral 2 MG Solution / drops Oral 1 mg / mL Solution / drops Ophthalmic 0025 % Solution Ophthalmic Solution / drops Ophthalmic 0.025 % Solution / drops Oral 1 mg/ml Tablet Oral 2 mg Solution Ophthalmic .35 mg/1mL Solution Ophthalmic 0.25 mg / mL Solution Ophthalmic 0.345 mg/1mL Solution / drops Ophthalmic 0.25 mg/1mL Syrup Oral 1 mg/5mL - Prices
Unit description Cost Unit Ketotifen fumarate powder 926.63USD g Zaditor 0.025% Solution 5ml Bottle 74.96USD bottle Ketotifen fum 0.025% eye drops 2.44USD ml Refresh 0.025% eye drops 2.2USD ml Zaditor 0.025% eye drops 2.15USD ml Alaway 0.025% eye drops 0.96USD ml Zaditen 1 mg Tablet 0.83USD tablet Novo-Ketotifen 1 mg Tablet 0.66USD tablet Novo-Ketotifen 0.2 mg/ml Syrup 0.14USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US9962376 No 2018-05-08 2030-06-27 US US9474746 No 2016-10-25 2028-03-27 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 190 https://pdf.hres.ca/dpd_pm/00017437.PDF water solubility Readily soluble https://pdf.hres.ca/dpd_pm/00017437.PDF pKa 8.43 ± 0.11 https://pdf.hres.ca/dpd_pm/00017437.PDF - Predicted Properties
Property Value Source Water Solubility 0.00787 mg/mL ALOGPS logP 3.49 ALOGPS logP 3.35 Chemaxon logS -4.6 ALOGPS pKa (Strongest Acidic) 12.67 Chemaxon pKa (Strongest Basic) 7.75 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 20.31 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 101.73 m3·mol-1 Chemaxon Polarizability 34.61 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.9923 Caco-2 permeable + 0.8867 P-glycoprotein substrate Substrate 0.87 P-glycoprotein inhibitor I Inhibitor 0.8564 P-glycoprotein inhibitor II Non-inhibitor 0.7474 Renal organic cation transporter Inhibitor 0.8198 CYP450 2C9 substrate Non-substrate 0.7542 CYP450 2D6 substrate Non-substrate 0.5638 CYP450 3A4 substrate Substrate 0.6984 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.9071 CYP450 2D6 inhibitor Inhibitor 0.8931 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Non-inhibitor 0.8607 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.6414 Ames test Non AMES toxic 0.7576 Carcinogenicity Non-carcinogens 0.9649 Biodegradation Not ready biodegradable 0.9547 Rat acute toxicity 2.7979 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.6336 hERG inhibition (predictor II) Non-inhibitor 0.5145
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-0f7k-1390000000-6db4be150fa1cfb3f6ab Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-03di-0009000000-1dbcde1a4ac16f1bcf45 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0a4i-0009000000-fa65f06e32215cfbf945 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-03di-1039000000-0a58525009b81cd44ae3 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0a4i-0039000000-b359d75878f298787a1c Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-05aj-1090000000-979acb1a747672e7b23f Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0gwo-2290000000-efb8febe2aec8be665c0 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 179.594611 predictedDarkChem Lite v0.1.0 [M-H]- 179.459211 predictedDarkChem Lite v0.1.0 [M-H]- 169.42592 predictedDeepCCS 1.0 (2019) [M+H]+ 180.074611 predictedDarkChem Lite v0.1.0 [M+H]+ 179.921111 predictedDarkChem Lite v0.1.0 [M+H]+ 171.78392 predictedDeepCCS 1.0 (2019) [M+Na]+ 179.677011 predictedDarkChem Lite v0.1.0 [M+Na]+ 177.87706 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Histamine receptor activity
- Specific Function
- In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
- Gene Name
- HRH1
- Uniprot ID
- P35367
- Uniprot Name
- Histamine H1 receptor
- Molecular Weight
- 55783.61 Da
References
- Mita H, Shida T: Comparison of anti-allergic activities of the histamine H1 receptor antagonists epinastine, ketotifen and oxatomide in human leukocytes. Arzneimittelforschung. 1995 Jan;45(1):36-40. [Article]
- Okabe S, Nakaji S, Tachibana M: Effect of ketotifen on acute gastric lesions and gastric secretion in rats. Jpn J Pharmacol. 1992 Jun;59(2):251-4. [Article]
- Hashimoto T, Ohata H, Honda K: Lysophosphatidic acid (LPA) induces plasma exudation and histamine release in mice via LPA receptors. J Pharmacol Sci. 2006 Jan;100(1):82-7. Epub 2006 Jan 11. [Article]
- Ito K, Sakamoto T, Hayashi Y, Morishita M, Shibata E, Sakai K, Takeuchi Y, Torii S: Role of tachykinin and bradykinin receptors and mast cells in gaseous formaldehyde-induced airway microvascular leakage in rats. Eur J Pharmacol. 1996 Jul 4;307(3):291-8. [Article]
- Yokoyama H, Iinuma K, Yanai K, Watanabe T, Sakurai E, Onodera K: Proconvulsant effect of ketotifen, a histamine H1 antagonist, confirmed by the use of d-chlorpheniramine with monitoring electroencephalography. Methods Find Exp Clin Pharmacol. 1993 Apr;15(3):183-8. [Article]
- Werner-Klein M, Goggel R, Westhof A, Erb KJ: Development and characterisation of a novel and rapid lung eosinophil influx model in the rat. Pulm Pharmacol Ther. 2008 Aug;21(4):648-56. doi: 10.1016/j.pupt.2008.03.002. Epub 2008 Apr 7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Phosphogluconate dehydrogenase (decarboxylating) activity
- Specific Function
- Catalyzes the oxidative decarboxylation of 6-phosphogluconate to ribulose 5-phosphate and CO(2), with concomitant reduction of NADP to NADPH.
- Gene Name
- PGD
- Uniprot ID
- P52209
- Uniprot Name
- 6-phosphogluconate dehydrogenase, decarboxylating
- Molecular Weight
- 53139.56 Da
References
- Akkemik E, Budak H, Ciftci M: Effects of some drugs on human erythrocyte 6-phosphogluconate dehydrogenase: an in vitro study. J Enzyme Inhib Med Chem. 2010 Aug;25(4):476-9. doi: 10.3109/14756360903257900. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Retinoic acid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
- Gene Name
- UGT1A3
- Uniprot ID
- P35503
- Uniprot Name
- UDP-glucuronosyltransferase 1-3
- Molecular Weight
- 60337.835 Da
References
- Kato Y, Izukawa T, Oda S, Fukami T, Finel M, Yokoi T, Nakajima M: Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4. Drug Metab Dispos. 2013 Jul;41(7):1389-97. doi: 10.1124/dmd.113.051565. Epub 2013 Apr 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Protein homodimerization activity
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
- Gene Name
- UGT1A4
- Uniprot ID
- P22310
- Uniprot Name
- UDP-glucuronosyltransferase 1-4
- Molecular Weight
- 60024.535 Da
References
- Kato Y, Izukawa T, Oda S, Fukami T, Finel M, Yokoi T, Nakajima M: Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4. Drug Metab Dispos. 2013 Jul;41(7):1389-97. doi: 10.1124/dmd.113.051565. Epub 2013 Apr 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.
- Specific Function
- Glucuronosyltransferase activity
- Gene Name
- UGT2B10
- Uniprot ID
- P36537
- Uniprot Name
- UDP-glucuronosyltransferase 2B10
- Molecular Weight
- 60773.485 Da
References
- Kato Y, Izukawa T, Oda S, Fukami T, Finel M, Yokoi T, Nakajima M: Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4. Drug Metab Dispos. 2013 Jul;41(7):1389-97. doi: 10.1124/dmd.113.051565. Epub 2013 Apr 23. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:54