Hydroxyzine-d8 (hydrochloride)
(Synonyms: 盐酸羟嗪 d8 （双盐酸盐）) 目录号 : GC47448
An internal standard for the quantification of hydroxyzine
Cas No.:1808202-93-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Hydroxyzine-d8 is intended for use as an internal standard for the quantification of hydroxyzine by GC- or LC-MS. Hydroxyzine is a histamine H1 receptor antagonist (Ki = 1.9 nM).1 It binds competitively with the H1 receptor inverse agonist mepyramine with an IC50 value of 80 µM in polymorphonuclear leukocytes.2 In vivo, it is metabolized to the H1 receptor antagonist cetirizine .3 In situ, hydroxyzine (10 µM) prevents recruitment of rolling leukocytes induced by histamine in rat mesentery post-capillary venules.4 Hydroxyzine also decreases anxiety-like behavior in mice, increasing the time spent in the open arms of the elevated plus maze and in the light side of the light-dark exploration test.5 Formulations containing hydroxyzine have been used in the treatment of anxiety and as antihistamines in the treatment of allergic rhinitis.
1.Gillard, M., Van Der Perren, C., Moguilevsky, N., et al.Binding characteristics of cetirizine and levocetirizine to human H1 histamine receptors: Contribution of Lys191 and Thr194Mol. Pharmacol.61(2)391-399(2002) 2.Wescott, S., and Kaliner, M.Histamine H1 binding site on human polymorphonuclear leukocytesInflammation7(3)291-300(1983) 3.Obach, R.S.Pharmacologically active drug metabolites: Impact on drug discovery and pharmacotherapyPharmacol. Rev.65(2)578-640(2013) 4.Asako, H., Kurose, I., Wolf, R., et al.Role of H1 receptors and P-selectin in histamine-induced leukocyte rolling and adhesion in postcapillary venulesJ. Clin. Invest.93(4)1508-1515(1994) 5.Sawantdesai, N.S., Kale, P.P., and Savai, J.Evaluation of anxiolytic effects of aripiprazole and hydroxyzine as a combination in miceJ. Basic Clin. Pharm.7(4)97-104(2016)
| Cas No. | 1808202-93-8 | SDF | |
| 别名 | 盐酸羟嗪 d8 （双盐酸盐） | ||
| Canonical SMILES | ClC1=CC=C(C(C2=CC=CC=C2)N3C([2H])([2H])C([2H])([2H])N(CCOCCO)C([2H])([2H])C3([2H])[2H])C=C1.Cl.Cl | ||
| 分子式 | C21H19ClD8N2O2.2HCl | 分子量 | 455.9 |
| 溶解度 | Water: slightly soluble | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1935 mL | 10.9673 mL | 21.9346 mL |
| 5 mM | 0.4387 mL | 2.1935 mL | 4.3869 mL |
| 10 mM | 0.2193 mL | 1.0967 mL | 2.1935 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Efficient synthesis of deuterium labeled hydroxyzine and aripiprazole
J Labelled Comp Radiopharm 2015 Jun 15;58(7):304-7.PMID:26011470DOI:10.1002/jlcr.3298
Hydroxyzine and aripiprazole are active pharmaceutical ingredients that have been largely acknowledged for their antipsychotic properties. Deuterium labeled isotopes of hydroxyzine and aripiprazole are internal standards that can aid in the further research of non-isotopic forms via quantification analysis using HPLC-MS/MS. The synthesis of Hydroxyzine-d8 was accomplished by coupling piperazine-d8 with 4-chlorobenzhydryl chloride followed by the reaction of the first intermediate with 2-(2-chloroethoxy) ethanol to afford 11.7% of Hydroxyzine-d8 with 99.5% purity. The synthesis of aripiprazole-d8 was also achieved in two steps. 1,4-Dibromobutane-d8 reacted with 7-hydroxy-3,4-dihydro-2(1H)-quinolinone. The first intermediate was then coupled with 1-(2, 3-dichlorophenyl)piperazine hydrochloride to produce 33.4% of aripiprazole-d8 with 99.93% purity.