Hydroxyzine dihydrochloride是一种苯二氮卓抗组胺剂,是可口服的组胺 H1 受体和血清素拮抗剂,可有效治疗慢性荨麻疹、皮炎和组胺介导的瘙痒。它还可以作为止吐剂和镇静剂,有缓解焦虑和紧张的作用。
产品描述
Hydroxyzine hydrochloride is a histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.
体外活性
在甩尾试验中,腹腔注射12.5 mg/kg Hydroxyzine降低吗啡在大鼠体内的镇痛作用而腹腔注射50 mg/kg Hydroxyzine加强吗啡的作用.500 μM Hydroxyzine使稳态的依托泊苷浓度明显降低2倍,在Sprague-Dawley大鼠体内的稳态浓度达到0.055 μM/mL.
体内活性
0.1 mM Hydroxyzine抑制实验性变应性脑脊髓炎Lewis大鼠体内50%的EAE恶化,且抑制70%肥大细胞脱颗粒作用。10 μM Hydroxyzine在预处理的膀胱切片中经过60分钟,抑制34%的10 μM的卡巴胆碱诱导的5-羟色胺释放,1 μM抑制25%,0.1 μM抑制17%。500 μM Hydroxyzine明显增加空肠外翻囊中依托泊苷到浆膜部位的运输。Hydroxyzine明显降低空肠和回肠中大约2.4 μg/mL的依托泊苷流出。
Cas No.
2192-20-3
分子式
C21H29Cl3N2O2
分子量
447.83
别名
盐酸羟嗪;Hydroxyzine 2HCl
储存和溶解度
DMSO:201 mM
H2O:201 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years