K2628
Ketotifen fumarate salt
≥99% (TLC), powder, H₁ histamine receptor antagonist
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A propos de cet article
Formule empirique (notation de Hill) :
C19H19NOS · C4H4O4
Numéro CAS:
Poids moléculaire :
425.50
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
EC Number:
252-100-0
MDL number:
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Ketotifen fumarate salt,
InChI key
YNQQEYBLVYAWNX-WLHGVMLRSA-N
InChI
1S/C19H19NOS.C4H4O4/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;5-3(6)1-2-4(7)8/h2-5,8,11H,6-7,9-10,12H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+
SMILES string
OC(=O)\C=C\C(O)=O.CN1CCC(\CC1)=C2/c3ccccc3CC(=O)c4sccc24
form
powder
originator
Novartis
Quality Level
Gene Information
human ... HRH1(3269), PDE7B(27115)
Catégories apparentées
General description
Ketotifen fumarate salt is an antihistamine drug.
Application
Ketotifen fumarate salt has been used: for mast cell product antagonism, as a positive control in β-hexosaminidase release assay, as mast cell stabilizer to treat pregnant dams added to ad libitum drinking water
Biochem/physiol Actions
H1 histamine receptor antagonist.
Ketotifen fumarate plays a key role in preventing histamine release by blocking the histamine H1 receptors. It interferes with the release of histamine, serotonin and other inflammatory mediators from mast cells. It exhibits with anti-allergic activity, anti-inflammatory effects including mast cell stabilization. It has been widely used for ophthalmic allergic conjunctivitis.
Features and Benefits
This compound was developed by Novartis. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Eye Irrit. 2
Classe de stockage
11 - Combustible Solids
wgk
WGK 3
ppe
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
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Jing Wang et al.
Diabetes/metabolism research and reviews, 27(8), 919-924 (2011-11-10)
Mast cells are essential in allergic responses and beyond. White adipose tissue from obese humans contains large numbers of mast cells. Serum mast cell tryptase levels are also significantly higher in obese subjects than in lean subjects, suggesting a role
Katsuya Unno et al.
European journal of pharmacology, 683(1-3), 179-185 (2012-03-28)
First generation H₁ histamine receptor antagonists, such as d-chlorpheniramine (d-CPA) and diphenhydramine, produce drowsiness in humans. They are currently used as over-the-counter sleep aids. However, the mechanisms underlying drowsiness induced by these H₁ histamine receptor antagonists remain obscure because they
Anthony Soluri et al.
Optometry and vision science : official publication of the American Academy of Optometry, 89(8), 1140-1149 (2012-07-10)
To investigate the uptake and delivery of the anti-allergy drug ketotifen fumarate (KF) by commercially available contact lenses. A total of 14 different commercially available contact lenses were investigated, including five frequent-replacement silicone hydrogels, three conventional hydrogels, and six daily
A Tieppo et al.
Journal of controlled release : official journal of the Controlled Release Society, 157(3), 391-397 (2011-10-11)
In this paper, we demonstrate the successful in vivo extended release of a small molecular weight therapeutic, ketotifen fumarate (MW=425), from molecularly imprinted, therapeutic contact lenses. This is the first time that a steady, effective concentration of drug is maintained
Investigation into the mechanism of action of Moringa oleifera for its anti-asthmatic activity
Mehta A and Agrawal B
Oriental Pharmacy and Experimental Medicine, 8(1), 24-31 (2008)
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