A selective histamine H1 receptor antagonist (Ki = 10 nM); inhibits eosinophil chemotaxis and LTB4 release independent from H1 antagonism; inhibits aerosol histamine-induced bronchospasm in guinea pigs (ED50 = 100 μg/kg

Cetirizine (hydrochloride) – 1 g

Brand:
Cayman
CAS:
83881-52-1
Storage:
-20
UN-No:
Non-Hazardous - /

Cetirizine is a bioactive carboxylated metabolite of hydroxyzine (Item No. 24039) that acts as a selective histamine H1 receptor antagonist (Ki = 10 nM).{15199,31604} As a second generation antihistamine, it is non-sedating due to low lipophilicity, which prevents blood-brain barrier transit.{31603} Cetirizine is a racemic mixture composed of equal amounts of two enantiomers, (R)-cetirizine (Item No. 23992) and (S)-cetirizine, with pharmacological activity residing primarily in the (R) isomer.{31604} Cetirizine inhibits eosinophil chemotaxis and leukotriene B4 (LTB4; Item No. 20110) release independent from H1 antagonism.{31605} It inhibits aerosol histamine-induced bronchospasm in guinea pigs (ED50 = 100 μg/kg, p.o.).{47108} Formulations containing cetirizine have been used in the treatment of allergic rhinitis and chronic urticaria.  

 

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Description

A selective histamine H1 receptor antagonist (Ki = 10 nM); inhibits eosinophil chemotaxis and LTB4 release independent from H1 antagonism; inhibits aerosol histamine-induced bronchospasm in guinea pigs (ED50 = 100 μg/kg, p.o.)

Formal name: 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetic acid, dihydrochloride

Synonyms:  UCB-P 071

Molecular weight: 461.8

CAS: 83881-52-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Leukotrienes||Research Area|Immunology & Inflammation|Innate Immunity

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