A selective histamine H1 receptor antagonist; the (R)-enantiomer of cetirizine; binds to the H1 receptor with higher affinity than cetirizine (Kis = 3 and 6 nM

(R)-Cetirizine (hydrochloride) – 250 mg

Brand:
Cayman
CAS:
130018-87-0
Storage:
-20
UN-No:
De Minimis - 3077 / 9

(R)-Cetirizine is the (R)-enantiomer of the histamine H1 receptor antagonist and second generation antihistamine cetirizine (Item No. 19686).{31604} (R)-Cetirizine binds to the H1 receptor with higher affinity than cetirizine (Kis = 3 and 6 nM, respectively) and is 25,000-100,000-fold selective for H1 receptors over muscarinic M1-M5 receptors.{39482} It decreases production of RANTES and eotaxin following antigen stimulation in mouse eosinophils in vitro in a concentration-dependent manner with a minimum effective concentration (MEC) of 0.05 µM.{39483} Intranasal administration of (R)-cetirizine (0.01-1%) dose-dependently decreases histamine-induced nasal rubbing and sneezing in mice.{39484} Formulations containing (R)-cetirizine have been used in the treatment of allergic rhinitis and chronic idiopathic urticaria.  

 

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SKU: 23992 - 250 mg Category:

Description

A selective histamine H1 receptor antagonist; the (R)-enantiomer of cetirizine; binds to the H1 receptor with higher affinity than cetirizine (Kis = 3 and 6 nM, respectively) and is highly selective for H1 over M1-M5 receptors; decreases production of RANTES and eotaxin following antigen stimulation in mouse eosinophils in vitro (MEC = 0.05 µM); dose-dependently decreases histamine-induced nasal rubbing and sneezing in mice (0.01-1% solution)

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

Synonyms:  Levocetirizine

Molecular weight: 461.8

CAS: 130018-87-0

Purity: ≥98%

Formulation: A crystalline solid

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

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