Cetirizine (hydrochloride)

Cetirizine is a bioactive carboxylated metabolite of hydroxyzine (Cay-24039) that acts as a selective histamine H1 receptor antagonist (Ki = 10 nM). As a second generation antihistamine, it is non-sedating due to low lipophilicity, which prevents blood-brain barrier transit. Cetirizine is a racemic mixture composed of equal amounts of two enantiomers, (R)-cetirizine (Cay-23992) and (S)-cetirizine, with pharmacological activity residing primarily in the (R) isomer. Cetirizine inhibits eosinophil chemotaxis and leukotriene B4 (LTB4, Cay-20110) release independent from H1 antagonism. It inhibits aerosol histamine-induced bronchospasm in guinea pigs (ED50 = 100 µg/kg, p.o.). Formulations containing cetirizine have been used in the treatment of allergic rhinitis and chronic urticaria.Formal Name: 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetic acid, dihydrochloride. CAS Number: 83881-52-1. Synonyms: UCB-P 071. Molecular Formula: C21H25ClN2O3 . 2HCl. Formula Weight: 461.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3mg/mL, DMSO: 12mg/mL, PBS (pH 7.2): 10mg/mL. lambdamax: 229 nm. SMILES: ClC1=CC=C(C(N2CCN(CCOCC(O)=O)CC2)C3=CC=CC=C3)C=C1.Cl.Cl. InChi Code: InChI=1S/C21H25ClN2O3.2ClH/c22-19-8-6-18(7-9-19)21(17-4-2-1-3-5-17)24-12-10-23(11-13-24)14-15-27-16-20(25)26,,/h1-9,21H,10-16H2,(H,25,26),2*1H. InChi Key: PGLIUCLTXOYQMV-UHFFFAOYSA-N.