中文同义词:
左西替利嗪;2-[2-[4-[(4-氯苯基)-苯基甲基]哌嗪-1-基]乙氧基]乙酸;左旋西替利嗪二盐酸盐;左西替利嗪盐酸盐;西替利嗪R异构体;左西替利;左西替立嗪;(R)-西替利嗪-D4
英文同义词:
LEVOCETIRIZINE;alerlisin;2-[2-[4-[(R)-(4-chlorophenyl)-phenylmethyl]-1-piperazinyl]ethoxy]acetic acid;Cetirizine Impurity 20;(R)-2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)acetic acid;LEVOCETRIZINE;(R)-2-[2-[4-(4-chlorophenyl)-phenylmethyl]-phenylmethyl-1-]-piperazinyl-]ethoxyl﹞acetic acid dihydrochloride;LevocetirizineHydrochloride
相关类别:
小分子抑制剂;医药原料;XYZAL;Aromatics;Chiral Reagents;Heterocycles;Intermediates Fine Chemicals;Pharmaceuticals
沸点
542.1±45.0 °C(Predicted)
密度
1.237±0.06 g/cm3(Predicted)
酸度系数(pKa)
3.46±0.10(Predicted)
CAS 数据库
130018-77-8(CAS DataBase Reference)
概述
左西替利嗪属于第二代的H1组胺受体拮抗体，其被认为相对于第一代化合物能够表现出显著的优势。研究表明，左西替利嗪能够安全有效地减轻周期性过敏的症状。
用途
盐酸左西替利嗪主要用于治疗组胺引起的季节性、常年性变应性鼻炎、眼睛和皮肤瘙痒、慢性特发性荨麻疹。
生物活性
Levocetirizine ((R)-Cetirizine) 是第三代 peripheral H1-receptor 拮抗剂。Levocetirizine 是一种抗组胺剂，是 Cetirizine 的 R 对映体。Levocetirizine 对组胺 H1-受体的亲和力高于 (S)-Cetirizine，并且可用于研究变应性鼻炎和慢性特发性荨麻疹。
体内研究
Levocetirizine (0.4 mg/kg; oral administration; male Sprague-Dawley rats) treatment shows that the C max , AUC 0-t , AUC 0-∞ and t 1/2 are 0.34 μg/mL, 3.26 μg h/mL, 3.67 μg h/mL and 2.34 hours, respectively in Sprague-Dawley rats.
Animal Model: 30 male Sprague-Dawley rats (8 weeks old; 200-250 g)
Dosage: 0.4 mg/kg
Administration: Oral administration (Pharmacokinetic Analysis)
Result: The C max , AUC 0-t , AUC 0-∞ and t 1/2 were 0.34 μg/mL, 3.26 μg h/mL, 3.67 μg h/mL and 2.34 hours, respectively.
Animal Model:
30 male Sprague-Dawley rats (8 weeks old; 200-250 g)
Administration:
Oral administration (Pharmacokinetic Analysis)
Result:
The C max , AUC 0-t , AUC 0-∞ and t 1/2 were 0.34 μg/mL, 3.26 μg h/mL, 3.67 μg h/mL and 2.34 hours, respectively.
