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Merck
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Key Documents

K2628

Sigma-Aldrich

Ketotifen fumarate salt

≥99% (TLC), powder, H₁ histamine receptor antagonist

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About This Item

Fórmula empírica (notación de Hill):
C19H19NOS · C4H4O4
Número de CAS:
34580-14-8
Peso molecular:
425.50
EC Number:
252-100-0
MDL number:
MFCD00079394
UNSPSC Code:
12352200
PubChem Substance ID:
24278506
NACRES:
NA.77

product name

Ketotifen fumarate salt,

form

powder

originator

Novartis

SMILES string

OC(=O)\C=C\C(O)=O.CN1CCC(\CC1)=C2/c3ccccc3CC(=O)c4sccc24

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+

InChI key

YNQQEYBLVYAWNX-WLHGVMLRSA-N

Gene Information

human ... HRH1(3269) , PDE7B(27115)

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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.

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302,H319

Hazard Classifications

Acute Tox. 4 Oral - Eye Irrit. 2

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

ppe

dust mask type N95 (US), Eyeshields, Faceshields, Gloves

Certificados de análisis (COA)

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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
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
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
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
Inhibitory effect of various Tunisian olive oils on chemical mediator release and cytokine production by basophilic cells
Yamada P, et al.
Journal of Ethnopharmacology, 116(2), 279-287 (2008)
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