A selective histamine H1 receptor antagonist
Cas No. | 130018-87-0 |
别名 | 盐酸左西替利嗪,(R)-Cetirizine dihydrochloride |
Canonical SMILES | ClC1=CC=C([C@H](N2CCN(CCOCC(O)=O)CC2)C3=CC=CC=C3)C=C1.Cl.Cl |
分子式 | C21H25ClN2O3•2HCl |
分子量 | 461.8 |
溶解度 | DMF: 3 mg/ml,DMSO: 12 mg/ml,PBS (pH 7.2): 10 mg/ml |
储存条件 | 4°C, protect from light |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | (R)-Cetirizine is the (R)-enantiomer of the histamine H1 receptor antagonist and second generation antihistamine cetirizine . (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. 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. Intranasal administration of (R)-cetirizine (0.01-1%) dose-dependently decreases histamine-induced nasal rubbing and sneezing in mice. Formulations containing (R)-cetirizine have been used in the treatment of allergic rhinitis and chronic idiopathic urticaria. |