| Identification | Back Directory | [Name]
Cetirizine-d8 (hydrochloride) | [CAS]
2070015-04-0 | [Synonyms]
Cetirizine-d8 DiHCl
Cetirizine-d8 (hydrochloride)
[2H8]-Cetirizine Dihydrochloride | [Molecular Formula]
C21H18Cl2D8N2O3 | [MOL File]
2070015-04-0.mol | [Molecular Weight]
433.398 |
| Hazard Information | Back Directory | [Description]
Cetirizine-d8 (hydrochloride) is intended for use as an internal standard for the quantification of cetirizine , (R)-cetirizine , and (S)-cetirizine by GC- or LC-MS. Cetirizine is a bioactive carboxylated metabolite of hydroxyzine 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 and (S)-cetirizine, with pharmacological activity residing primarily in the (R) isomer. Cetirizine inhibits eosinophil chemotaxis and leukotriene B4 (LTB4; ) 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. | [Uses]
A nonsedating type histamine H1-receptor antagonist. A major metabolite of Hydroxyzine. Pharmacological activity resides primarily in the (R)-isomer. Antihystaminic. | [IC 50]
H1 Receptor | [References]
[1] ROBIN L. THURMOND Paul J D Erwin W Gelfand. The role of histamine H1 and H4 receptors in allergic inflammation: the search for new antihistamines[J]. Nature Reviews. Drug Discovery, 2008, 7 1: 41-53. DOI: 10.1038/nrd2465
[2] LUO ZHANG Jianguo H Lei Cheng. The clinical use of cetirizine in the treatment of allergic rhinitis.[J]. Pharmacology, 2013: 14-25. DOI: 10.1159/000351843
[3] TILLEMENT J P. The advantages for an H1 antihistamine of a low volume of distribution[J]. Allergy, 2002, 55 supp60: 17-21. DOI: 10.1034/j.1398-9995.2000.00003.x
[4] M K?LLER. Cetirizine exerts anti-inflammatory effects on human neutrophils.[J]. International Archives of Allergy and Immunology, 1996, 110 1: 52-56. DOI: 10.1159/000237310
[5] JOSEP LLUPIà Jesús L Jordi Gras. Comparative antiallergic effects of second-generation H1-antihistamines ebastine, cetirizine and loratadine in preclinical models.[J]. Arzneimittel-Forschung-Drug Research, 2003, 53 2: 93-97. DOI: 10.1055/s-0031-1297078 |
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