Product Name:    Ketotifen fumarate

Synonyms:    Ketotifene fumarate;10H-Benzo4,5cyclohepta1,2-bthiophen-10-one, 4,9-dihydro-4-(1-methyl-4-piperidinylidene)-, (2E)-2-butenedioate (1:1);zaditor;KETOTIFEN FUMARATE EP;Allerkif;Anatifen;4,9-Dihydro-4-(1-methyl-4-piperidylidene)-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one fumarate;zaditen

CAS:    34580-14-8

MF:    C23H23NO5S

MW:    425.5

EINECS:    252-100-0

Product Categories:    Antagonists;Histaminergics;Neurotransmitters;Histamine receptor;Aromatics;Antiallergic agents;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;Pharmaceutical raw material;SERC;Other APIs;API

Ketotifen is a histamine H1 receptor antagonist (Ki = 1.3 nM) and mast cell stabilizer. It is selective for H1 receptors over H2 and H3 receptors (Kis = 987 and 2,500 nM, respectively). Ketotifen (50 and 100 μM) inhibits degranulation of rat peritoneal mast cells induced by compound 48/80 . It inhibits the passive cutaneous anaphylaxis (PCA) reaction in rats by 54.6% when administered orally at a dose of 20 mg/kg. Ketotifen (30 mg/kg) inhibits the quick phase airway response in a rat ovalbumin-induced immediate airway response model. Formulations containing ketotifen have been used in the treatment of itching associated with allergic conjunctivitis.