Formulation: A solid
Formal Name: 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl-d8]ethoxy]-acetic acid, dihydrochloride
Purity: ≥99% deuterated forms (d1-d8)
Formula Markup: C21H17ClD8N2O3 • 2HCl
Formula Weight: 469,9
Shelf life (days): 1460
CAS Number: 2070015-04-0
Notes: Cetirizine-d8 (hydrochloride) is intended for use as an internal standard for the quantification of cetirizine (Item No. 19686), (R)-cetirizine (Item No. 23992), and (S)-cetirizine by GC- or LC-MS. 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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