A histamine H1 receptor antagonist (Ki = 1.3 nM) and mast cell stabilizer; selective for H1 receptors over H2 and H3 receptors (Kis = 987 and 2

Ketotifen (fumarate) – 250 mg

Brand:
Cayman
CAS:
34580-14-8
Storage:
-20
UN-No:
Non-Hazardous - /

Ketotifen is a histamine H1 receptor antagonist (Ki = 1.3 nM) and mast cell stabilizer.{21941,48520} It is selective for H1 receptors over H2 and H3 receptors (Kis = 987 and 2,500 nM, respectively).{21941} Ketotifen (50 and 100 μM) inhibits degranulation of rat peritoneal mast cells induced by compound 48/80 (Item No. 22173).{48520} It inhibits the passive cutaneous anaphylaxis (PCA) reaction in rats by 54.6% when administered orally at a dose of 20 mg/kg.{32040} Ketotifen (30 mg/kg) inhibits the quick phase airway response in a rat ovalbumin-induced immediate airway response model.{26817} Formulations containing ketotifen have been used in the treatment of itching associated with allergic conjunctivitis.  

 

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Description

A histamine H1 receptor antagonist (Ki = 1.3 nM) and mast cell stabilizer; selective for H1 receptors over H2 and H3 receptors (Kis = 987 and 2,500 nM, respectively); inhibits compound 48/80-induced degranulation of rat peritoneal mast cells at 50 and 100 μM; inhibits the PCA reaction in rats by 54.6% at 20 mg/kg; inhibits the quick phase airway response in a rat ovalbumin-induced immediate airway response model at 30 mg/kg

Formal name: 4,9-dihydro-4-(1-methyl-4-piperidinylidene)-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one-(2E)-2-butenedioate

Synonyms:  HC 20511

Molecular weight: 425.5

CAS: 34580-14-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Immunology & Inflammation|Pulmonary Diseases|Asthma

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