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Hydroxyzine 2HCl

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Chemical Structure| 2192-20-3 同义名 : 羟嗪 二盐酸盐 ;Hydroxyzine dihydrochloride
CAS号 : 2192-20-3
货号 : A738838
分子式 : C21H29Cl3N2O2
纯度 : 99+%
分子量 : 447.826
MDL号 : MFCD00058200
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 150 mg/mL(334.95 mM)
动物实验配方：
生物活性
靶点

  • H1 receptor

    Histamine H1 receptor, IC50:10 nM-19 nM
描述 Hydroxyzine Dihydrochloride is the first generation H1 receptor antagonist drug. Hydroxyzine is an antihistaminic with sedative properties used in the control of anxiety and emesis[3]. Hydroxyzine provided sustained pain relief to six hours, whereas meperidine produced analgesia up to two hours. The combination produced additive analgesia only during the first 2 hr[4]. The mean systemic availability of oral hydroxyzine was 72%. Hydroxyzine was rapidly converted to cetirizine regardless of the route of administration. The mean area-under-the-curve was eight and ten times higher for cetirizine than hydroxyzine after intravenous and oral dosing, respectively. After oral administration of hydroxyzine, the mean peak concentration of cetirizine was approximately 2.2 mg/mL and that of hydroxyzine 0.16 mg/mL. The terminal half-life for cetirizine varied between 10 and 11 h after intravenous and oral administration of hydroxyzine. Pharmacodynamic modelling predicted that maximal antihistamine effect would occur with twice daily oral administration of hydroxyzine at 2 mg/kg[5]. Hydroxyzine reduced carbachol-induced serotonin release from rat bladder in vitro through a mechanism which was unrelated to its H1 receptor antagonistic properties. The ability of hydroxyzine to inhibit bladder mast cell activation by neurogenic stimuli along with its anticholinergic, anxiolytic and analgesic properties[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.17mL

2.23mL

1.12mL

22.33mL

4.47mL

2.23mL
参考文献

[1]Anthes JC, Gilchrest H, et al. Biochemical characterization of desloratadine, a potent antagonist of the human histamine H(1) receptor. Eur J Pharmacol. 2002 Aug 9;449(3):229-37.

[2]Minogiannis P, El-Mansoury M, et al. Hydroxyzine inhibits neurogenic bladder mast cell activation. Int J Immunopharmacol. 1998 Oct;20(10):553-63.

[3]Elzainy AA, Gu X, Simons FE, Simons KJ. Hydroxyzine from topical phospholipid liposomal formulations: evaluation of peripheral antihistaminic activity and systemic absorption in a rabbit model. AAPS PharmSci. 2003 Nov 5;5(4):E28

[4]Stambaugh JE Jr, Lane C. Analgesic efficacy and pharmacokinetic evaluation of meperidine and hydroxyzine, alone and in combination. Cancer Invest. 1983;1(2):111-7

[5]Bizikova P, Papich MG, Olivry T. Hydroxyzine and cetirizine pharmacokinetics and pharmacodynamics after oral and intravenous administration of hydroxyzine to healthy dogs. Vet Dermatol. 2008 Dec;19(6):348-57

[6]Minogiannis P, El-Mansoury M, Betances JA, Sant GR, Theoharides TC. Hydroxyzine inhibits neurogenic bladder mast cell activation. Int J Immunopharmacol. 1998 Oct;20(10):553-63