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Identification
NameKetotifen
Accession NumberDB00920  (APRD01061)
TypeSmall Molecule
GroupsApproved
Description

A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis. [PubChem]

Structure
Thumb
Synonyms
Ketotifene
Ketotifeno
Ketotifenum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ketotifen Ophthalmic Solutionsolution0.25 mgophthalmicSterimax Inc2013-03-07Not applicableCanada
Novo-ketotifen - Syr 1mg/5mlsyrup1 mgoralNovopharm Limited1995-12-312015-10-26Canada
Novo-ketotifen Tab 1mgtablet1 mgoralNovopharm Limited1997-07-292013-02-11Canada
Nu-ketotifen Syrup - 1mg/5mlsyrup1 mgoralNu Pharm Inc1996-12-092012-09-04Canada
PMS-ketotifensyrup1 mgoralPharmascience Inc1998-08-312013-02-07Canada
PMS-ketotifentablet1 mgoralPharmascience Inc1998-08-312013-02-07Canada
Zaditentablet1 mgoralTeva Canada Limited1990-12-31Not applicableCanada
Zaditensyrup1 mgoralTeva Canada Limited1990-12-31Not applicableCanada
Zaditen - Dps 1mg/mldrops1 mgoralNovartis Pharmaceuticals Canada IncNot applicableNot applicableCanada
Zaditorsolution0.25 mgophthalmicLaboratoires Thea2000-08-01Not applicableCanada
Zaditorsolution0.25 mgophthalmicNovartis Pharmaceuticals Canada Inc2006-08-032012-01-17Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-ketotifen - Syr 1mg/5mlsyrup1 mgoralApotex Inc1996-11-07Not applicableCanada
Approved Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AlawaykitBausch & Lomb Incorporated2006-12-01Not applicableUs
Alawaysolution/ drops.25 mg/mLophthalmicBausch & Lomb Incorporated2006-12-01Not applicableUs
Allergy Eyesolution/ drops.25 mg/mLophthalmicH E B2010-09-15Not applicableUs
Allergy Eyesolution/ drops.25 mg/mLophthalmicCVS Pharmacy2011-01-07Not applicableUs
Allergy Eye Dropssolution/ drops.35 mg/mLophthalmicH E B2014-02-25Not applicableUs
Allergy Eye Dropssolution/ drops.35 mg/mLophthalmicCardinal Health2014-01-13Not applicableUs
Allergy Eye Dropssolution/ drops.35 mg/mLophthalmicAdvanced Vision Research (Subsidiary of Akorn, Inc.)2013-11-14Not applicableUs
Allergy Eye Original Prescription Strengthsolution/ drops.25 mg/mLophthalmicMeijer Distribution Inc1995-12-12Not applicableUs
Allergy Relief Eyesolution/ drops.25 mg/mLophthalmicWestern Family Foods Inc2011-05-25Not applicableUs
Allergy Relief Eye Dropssolution/ drops.35 mg/mLophthalmicKinray Inc.2014-03-18Not applicableUs
Antihistamine Eyesolution.25 mg/mLophthalmicCVS Pharmacy2010-10-19Not applicableUs
Care One Allergy Eyesolution/ drops.25 mg/mLophthalmicAmerican Sales Company2010-08-30Not applicableUs
Care One Eye Itch Reliefsolution.25 mg/mLophthalmicAmerican Sales Company2010-08-30Not applicableUs
Equaline Eye Itch Reliefsolution.25 mg/mLophthalmicSupervalu Inc2010-10-15Not applicableUs
Equate Eye Itch Reliefsolution.25 mg/mLophthalmicWal Mart Stores Inc2010-07-08Not applicableUs
Equate Itchy Eyesolution.25 mg/mLophthalmicWal Mart Stores Inc2010-09-09Not applicableUs
Eye Itchsolution/ drops.35 mg/mLophthalmicKroger Company2014-01-22Not applicableUs
Eye Itchsolution/ drops.35 mg/mLophthalmicMeijer Distribution Inc2014-01-23Not applicableUs
Eye Itchsolution.25 mg/mLophthalmicKroger Company2010-10-16Not applicableUs
Eye Itch Reliefsolution/ drops.35 mg/mLophthalmicRite Aid Corporation2013-12-06Not applicableUs
Eye Itch Reliefsolution/ drops.35 mg/mLophthalmicCVS Pharmacy2014-02-07Not applicableUs
Eye Itch Reliefsolution/ drops.35 mg/mLophthalmicMc Kesson Corporation Valu Rite2014-02-07Not applicableUs
Eye Itch Reliefsolution.25 mg/mLophthalmicSafeway2014-08-20Not applicableUs
Eye Itch Reliefsolution.25 g/mLophthalmicCVS Pharmacy2010-09-14Not applicableUs
Eye Itch Reliefsolution.25 mg/mLophthalmicWalgreen Company2010-08-13Not applicableUs
Eye Itch Reliefsolution/ drops.35 mg/mLophthalmicH E B2014-02-25Not applicableUs
Eye Itch Reliefsolution/ drops.35 mg/mLophthalmicRite Aid Corporation2013-12-06Not applicableUs
Eye Itch Reliefsolution/ drops.35 mg/mLophthalmicChain Drug Consortium2014-01-10Not applicableUs
Eye Itch Reliefsolution.25 mg/mLophthalmicMeijer Distribution Inc2010-08-23Not applicableUs
Eye Itch Reliefsolution.25 mg/mLophthalmicRite Aid Corporation2010-10-06Not applicableUs
Eye Itch Reliefsolution/ drops.35 mg/mLophthalmicMc Kesson Corp.2014-02-07Not applicableUs
Eye Itch Reliefsolution/ drops.25 mg/mLophthalmicWalgreens2012-05-01Not applicableUs
Eye Itch Reliefsolution/ drops.35 mg/mLophthalmicAmerisource Bergen2013-12-06Not applicableUs
Eye Itch Reliefsolution/ drops.35 mg/mLophthalmicGood Sense2014-06-20Not applicableUs
Eye Itch Reliefsolution/ drops.35 mg/mLophthalmicCVS Pharmacy2014-02-07Not applicableUs
Eye Itch Reliefsolution.25 mg/mLophthalmicH E B2010-09-10Not applicableUs
Eye Itch Reliefsolution/ drops.35 mg/mLophthalmicCardinal Health2014-01-13Not applicableUs
Eye Itch Reliefsolution/ drops.35 mg/mLophthalmicKinray Inc.2014-03-18Not applicableUs
Eye Itch Reliefsolution/ drops.35 mg/mLophthalmicRugby Laboratories2016-01-20Not applicableUs
Good Neighbor Pharmacy Eye Itch Reliefsolution.25 mg/mLophthalmicDispensing Solutions, Inc.2010-11-13Not applicableUs
Good Neighbor Pharmacy Eye Itch Reliefsolution.25 mg/mLophthalmicAmerisource Bergen2010-11-13Not applicableUs
Good Neighbor Pharmacy Itchy Eyesolution.25 mg/mLophthalmicAmerisource Bergen2010-10-07Not applicableUs
Good Sense Allergy Eyesolution/ drops.25 mg/mLophthalmicL Perrigo Company1997-11-18Not applicableUs
Good Sense Eye Itch Reliefsolution.25 mg/mLophthalmicL Perrigo Company2010-09-15Not applicableUs
Good Sense Itchy Eye Original Prescription Strengthsolution.25 mg/mLophthalmicL Perrigo Company1997-10-28Not applicableUs
Health Mart Eye Itch Reliefsolution.25 mg/mLophthalmicMc Kesson2012-02-03Not applicableUs
Itchy Eyesolution/ drops.35 mg/mLophthalmicKroger Company2014-01-22Not applicableUs
Itchy Eyesolution.25 mg/mLophthalmicH E B2010-09-15Not applicableUs
Itchy Eyesolution/ drops.35 mg/mLophthalmicMeijer Distribution Inc2014-01-23Not applicableUs
Itchy Eyesolution.25 mg/mLophthalmicKroger Company2011-05-27Not applicableUs
Itchy Eyesolution.25 mg/mLophthalmicMajor Pharmaceuticals2010-11-16Not applicableUs
Itchy Eyesolution/ drops.35 mg/mLophthalmicMeijer Distribution Inc2016-01-26Not applicableUs
Itchy Eye Dropssolution/ drops.35 mg/mLophthalmicGood Sense2014-06-20Not applicableUs
Itchy Eye Dropssolution/ drops.35 mg/mLophthalmicAmerisource Bergen2013-12-06Not applicableUs
Itchy Eye Original Prescription Strengthsolution.25 mg/mLophthalmicMeijer Distribution Inc2010-08-23Not applicableUs
Itchy Eye Reliefsolution.25 mg/mLophthalmicWestern Family Foods Inc2011-05-25Not applicableUs
Ketotifen Fumaratesolution/ drops.35 mg/mLophthalmicCVS Pharmacy2013-11-08Not applicableUs
Ketotifen Fumaratesolution/ drops.35 mg/mLophthalmicCVS Pharmacy2013-02-21Not applicableUs
Ketotifen Fumaratesolution/ drops.35 mg/mLophthalmicAkorn, Inc.2007-10-01Not applicableUs
Ketotifen Fumaratesolution/ drops.25 mg/mLophthalmicWalgreens2013-01-25Not applicableUs
Ketotifen Fumaratesolution.35 mg/mLophthalmicAdvanced Vision Research (Subsidiary of Akorn, Inc.)2012-03-15Not applicableUs
Leader Allergy Eyesolution.25 mg/mLophthalmicCardinal Health2010-09-22Not applicableUs
Leader Eye Itch Relief Dropssolution/ drops.345 mg/mLophthalmicHANLIM PHARM. CO., LTD.2010-04-21Not applicableUs
Smart Sense Allergysolution/ drops.25 mg/mLophthalmicKmart Corporation2010-08-27Not applicableUs
Sunmark Eye Itch Reliefsolution.25 mg/mLophthalmicMc Kesson2012-02-21Not applicableUs
Topcare Eye Itch Reliefsolution.25 mg/mLophthalmicTopco Associates LLC2013-02-08Not applicableUs
Up and Up Eye Itch Reliefsolution.25 mg/mLophthalmicTarget Corporation2010-09-03Not applicableUs
Wal Zyrsolution.25 mg/mLophthalmicWalgreen Company2010-03-12Not applicableUs
Zaditorsolution.35 mg/mLophthalmicAlcon Laboratories, Inc.2012-12-21Not applicableUs
Unapproved/Other Products Not Available
International Brands
NameCompany
TotifenPatron
ZastenNovartis
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Ketotifen fumarate
34580-14-8
Thumb
  • InChI Key: YNQQEYBLVYAWNX-WLHGVMLRSA-N
  • Monoisotopic Mass: 425.129694019
  • Average Mass: 425.5
DBSALT001856
Categories
UNIIX49220T18G
CAS number34580-13-7
WeightAverage: 309.425
Monoisotopic: 309.118734925
Chemical FormulaC19H19NOS
InChI KeyInChIKey=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[8.4.0.0³,⁷]tetradeca-1(14),3(7),4,10,12-pentaen-8-one
SMILES
CN1CCC(CC1)=C1C2=C(SC=C2)C(=O)CC2=CC=CC=C12
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassCycloheptathiophenes
Sub ClassNot Available
Direct ParentCycloheptathiophenes
Alternative Parents
Substituents
  • Cycloheptathiophene
  • Aryl alkyl ketone
  • Aryl ketone
  • Benzenoid
  • Piperidine
  • Heteroaromatic compound
  • Thiophene
  • Tertiary aliphatic amine
  • Tertiary amine
  • Ketone
  • Azacycle
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationIndicated as an add-on or prophylactic oral medication in the chronic treatment of mild atopic asthmatic children. Also used as self-medication for the temporary relief of itching of the eye due to allergic conjunctivitis (ophthalmic).
PharmacodynamicsKetotifen is a fast acting non-competitive histamine antagonist. It inhibits the release of mediators from mast cells. It is a non-bronchodilator antiasthmatic drug (when taken orally).
Mechanism of actionKetotifen is a relatively selective, non-competitive histamine antagonist (H1-receptor) and mast cell stabilizer. Ketotifen inhibits the release of mediators from mast cells involved in hypersensitivity reactions. Decreased chemotaxis and activation of eosinophils have also been demonstrated. Ketotifen also inhibits cAMP phosphodiesterase. Properties of ketotifen which may contribute to its antiallergic activity and its ability to affect the underlying pathology of asthma include inhibition of the development of airway hyper-reactivity associated with activation of platelets by PAF (Platelet Activating Factor), inhibition of PAF-induced accumulation of eosinophils and platelets in the airways, suppression of the priming of eosinophils by human recombinant cytokines and antagonism of bronchoconstriction due to leukotrienes. Ketotifen inhibits of the release of allergic mediators such as histamine, leukotrienes C4 and D4(SRS-A) and PAF.
Related Articles
AbsorptionFollowing oral administration absorption is at least 60%
Volume of distributionNot Available
Protein binding75%
Metabolism

Primarily hepatic. The main metabolite found in both plasma and urine is the inactive ketotifen-N-glucuronide. Nor-ketotifen, the N-demethylated metabolite, and the 10-alpha-hydroxyl derivative are the only other metabolites detectable in human urine.

SubstrateEnzymesProduct
Ketotifen
Not Available
Ketotifen-N-glucuronideDetails
Ketotifen
Not Available
10-alpha-hydroxyl KetotifenDetails
Ketotifen
Not Available
Nor-ketotifenDetails
Route of eliminationNot Available
Half life21 hours (for elimination)
ClearanceNot Available
ToxicityAdverse reactions include headaches, conjunctival injection and rhinitis.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9923
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.87
P-glycoprotein inhibitor IInhibitor0.8564
P-glycoprotein inhibitor IINon-inhibitor0.7474
Renal organic cation transporterInhibitor0.8198
CYP450 2C9 substrateNon-substrate0.7542
CYP450 2D6 substrateNon-substrate0.5638
CYP450 3A4 substrateSubstrate0.6984
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8607
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6414
Ames testNon AMES toxic0.7576
CarcinogenicityNon-carcinogens0.9649
BiodegradationNot ready biodegradable0.9547
Rat acute toxicity2.7979 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6336
hERG inhibition (predictor II)Non-inhibitor0.5145
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Bausch and lomb inc
  • Akorn inc
  • Alcon inc
  • Apotex inc etobicoke site
  • Novartis pharmaceuticals corp
Packagers
Dosage forms
FormRouteStrength
Kit
Solutionophthalmic.25 g/mL
Solution/ dropsophthalmic.35 mg/mL
Solution/ dropsophthalmic.25 mg/mL
Solutionophthalmic.25 mg/mL
Solution/ dropsophthalmic.345 mg/mL
Syruporal1 mg
Tabletoral1 mg
Dropsoral1 mg
Solutionophthalmic.35 mg/mL
Solutionophthalmic0.25 mg
Prices
Unit descriptionCostUnit
Ketotifen fumarate powder926.63USD g
Zaditor 0.025% Solution 5ml Bottle74.96USD bottle
Ketotifen fum 0.025% eye drops2.44USD ml
Refresh 0.025% eye drops2.2USD ml
Zaditor 0.025% eye drops2.15USD ml
Alaway 0.025% eye drops0.96USD ml
Zaditen 1 mg Tablet0.83USD tablet
Novo-Ketotifen 1 mg Tablet0.66USD tablet
Novo-Ketotifen 0.2 mg/ml Syrup0.14USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point152-153U.S. Patents 3,682,930; 3,770,728; and 3,960,894
logP2.2Not Available
pKa8.43Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00787 mg/mLALOGPS
logP3.49ALOGPS
logP3.35ChemAxon
logS-4.6ALOGPS
pKa (Strongest Acidic)12.3ChemAxon
pKa (Strongest Basic)7.15ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area20.31 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity101.73 m3·mol-1ChemAxon
Polarizability34.61 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
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 ReferencesNot Available
External Links
ATC CodesR06AX17S01GX08
AHFS Codes
  • 04:00.00
  • 04:92.00
  • 52:02.00
PDB EntriesNot Available
FDA labelDownload (9.05 KB)
MSDSNot Available
Interactions
Drug InteractionsNot Available
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
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 catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
Molecular Weight:
55783.61 Da
References
  1. 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. [PubMed:7893266 ]
  2. 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. [PubMed:1434122 ]
  3. 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. [PubMed:16404130 ]
  4. 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. [PubMed:8836617 ]
  5. 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. [PubMed:8101246 ]
  6. 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. [PubMed:18490184 ]
  7. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Metal ion binding
Specific Function:
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes.
Gene Name:
PDE4A
Uniprot ID:
P27815
Molecular Weight:
98142.155 Da
References
  1. Castillo JG, Gamboa PM, Garcia BE, Oehling A: Effect of ketotifen on phosphodiesterase activity from asthmatic individuals. Allergol Immunopathol (Madr). 1990 Jul-Aug;18(4):197-201. [PubMed:1702263 ]
  2. Huang Z, Liu S, Zhang L, Salem M, Greig GM, Chan CC, Natsumeda Y, Noguchi K: Preferential inhibition of human phosphodiesterase 4 by ibudilast. Life Sci. 2006 May 1;78(23):2663-8. Epub 2005 Nov 28. [PubMed:16313925 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Metal ion binding
Specific Function:
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes. May be involved in mediating central nervous system effects of therapeutic agents ranging from antidepressants to antiasthmatic and anti-inflammatory agents.
Gene Name:
PDE4B
Uniprot ID:
Q07343
Molecular Weight:
83342.695 Da
References
  1. Castillo JG, Gamboa PM, Garcia BE, Oehling A: Effect of ketotifen on phosphodiesterase activity from asthmatic individuals. Allergol Immunopathol (Madr). 1990 Jul-Aug;18(4):197-201. [PubMed:1702263 ]
  2. Huang Z, Liu S, Zhang L, Salem M, Greig GM, Chan CC, Natsumeda Y, Noguchi K: Preferential inhibition of human phosphodiesterase 4 by ibudilast. Life Sci. 2006 May 1;78(23):2663-8. Epub 2005 Nov 28. [PubMed:16313925 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Ubiquitin protein ligase binding
Specific Function:
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes.
Gene Name:
PDE4D
Uniprot ID:
Q08499
Molecular Weight:
91114.1 Da
References
  1. Castillo JG, Gamboa PM, Garcia BE, Oehling A: Effect of ketotifen on phosphodiesterase activity from asthmatic individuals. Allergol Immunopathol (Madr). 1990 Jul-Aug;18(4):197-201. [PubMed:1702263 ]
  2. Huang Z, Liu S, Zhang L, Salem M, Greig GM, Chan CC, Natsumeda Y, Noguchi K: Preferential inhibition of human phosphodiesterase 4 by ibudilast. Life Sci. 2006 May 1;78(23):2663-8. Epub 2005 Nov 28. [PubMed:16313925 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Metal ion binding
Specific Function:
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes.
Gene Name:
PDE4C
Uniprot ID:
Q08493
Molecular Weight:
79900.795 Da
References
  1. Castillo JG, Gamboa PM, Garcia BE, Oehling A: Effect of ketotifen on phosphodiesterase activity from asthmatic individuals. Allergol Immunopathol (Madr). 1990 Jul-Aug;18(4):197-201. [PubMed:1702263 ]
  2. Huang Z, Liu S, Zhang L, Salem M, Greig GM, Chan CC, Natsumeda Y, Noguchi K: Preferential inhibition of human phosphodiesterase 4 by ibudilast. Life Sci. 2006 May 1;78(23):2663-8. Epub 2005 Nov 28. [PubMed:16313925 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Metal ion binding
Specific Function:
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes. May have a role in muscle signal transduction.
Gene Name:
PDE7A
Uniprot ID:
Q13946
Molecular Weight:
55504.475 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Metal ion binding
Specific Function:
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes. May be involved in the control of cAMP-mediated neural activity and cAMP metabolism in the brain.
Gene Name:
PDE7B
Uniprot ID:
Q9NP56
Molecular Weight:
51834.855 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Metal ion binding
Specific Function:
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes. May be involved in maintaining basal levels of the cyclic nucleotide and/or in the cAMP regulation of germ cell development.
Gene Name:
PDE8A
Uniprot ID:
O60658
Molecular Weight:
93303.05 Da
References
  1. Castillo JG, Gamboa PM, Garcia BE, Oehling A: Effect of ketotifen on phosphodiesterase activity from asthmatic individuals. Allergol Immunopathol (Madr). 1990 Jul-Aug;18(4):197-201. [PubMed:1702263 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Metal ion binding
Specific Function:
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes. May be involved in specific signaling in the thyroid gland.
Gene Name:
PDE8B
Uniprot ID:
O95263
Molecular Weight:
98977.9 Da
References
  1. Castillo JG, Gamboa PM, Garcia BE, Oehling A: Effect of ketotifen on phosphodiesterase activity from asthmatic individuals. Allergol Immunopathol (Madr). 1990 Jul-Aug;18(4):197-201. [PubMed:1702263 ]
Kind
Protein
Organism
Human
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
Molecular Weight:
53139.56 Da
References
  1. 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. [PubMed:20235752 ]
  2. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on May 05, 2016 15:33