产品说明书

Meclizine dihydrochloride

Print
Chemical Structure| 1104-22-9 同义名 : 美克洛嗪二盐酸盐 ;Meclozine dihydrochloride;Meclizine (hydrochloride);NSC 28728;Meclozine;Meclizine 2HCl
CAS号 : 1104-22-9
货号 : A142777
分子式 : C25H29Cl3N2
纯度 : 98%
分子量 : 463.87
MDL号 : MFCD00058199
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 :

DMSO: 35 mg/mL(75.45 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • H1 receptor
描述 Meclizine dihydrochloride, is a piperazine-derived histamine H1 antagonist, and has been frequently used for prevention and treatment of vomiting and nausea. In primary bone marrow-derived macrophages (BMMs), meclizine reduced osteoclast formation and bone resorption in a dose-dependent manner[3]. Meclizine is also an agonist of human pregnane X receptor (PXR). The inhibition of human liver microsomal testosterone 6β-hydroxylation by meclizine occurred by a mixed mode and with an apparent Ki of 31 ± 6μM[4]. Meclizine is a first generation antihistamine that is used largely to treat vertigo and motion sickness. It has not been linked to instances of clinically apparent acute liver injury[5]. Meclizine protected against 6-hydroxydopamine-induced apoptosis and cell death in both SH-SY5Y cells and rat primary cortical cultures. It increases the level of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3), which activates phosphofructokinase, a rate-determining enzyme of glycolysis[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02625181 Postoperative Nausea and Vomit... 展开 >>ing 收起 << Not Applicable Completed - United States, Tennessee ... 展开 >> Vanderbilt University Medical Center Nashville, Tennessee, United States, 37212 收起 <<
NCT02130622 - Terminated(Lack of recruitment... 展开 >>) 收起 << - -
NCT02130622 Diabetic Gastroparesis Phase 2 Terminated(Lack of recruitment... 展开 >>) 收起 << - United States, New Hampshire ... 展开 >> Dartmouth-Hitchcock Medical Center Lebanon, New Hampshire, United States, 03756 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.78mL

2.16mL

1.08mL

21.56mL

4.31mL

2.16mL
参考文献

[1]Huang W, Zhang J, et al. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR. Mol Endocrinol. 2004 Oct;18(10):2402-8.

[2]King CT, Weaver SA, Narrod SA. Antihistamine and Teratogenicity in the Rat. J Pharmacol Exp Ther. 1965 Mar;147:391-8.

[3]Guo J, Li W, Wu Y, Jing X, Huang J, Zhang J, Xiang W, Ren R, Lv Z, Xiao J, Guo F. Meclizine Prevents Ovariectomy-Induced Bone Loss and Inhibits Osteoclastogenesis Partially by Upregulating PXR. Front Pharmacol. 2017 Oct 4;8:693

[4]Foo WY, Tay HY, Chan EC, Lau AJ. Meclizine, a pregnane X receptor agonist, is a direct inhibitor and mechanism-based inactivator of human cytochrome P450 3A. Biochem Pharmacol. 2015 Oct 1;97(3):320-30

[5]LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Meclizine. 2017 Jan 16

[6]Hong CT, Chau KY, Schapira AH. Meclizine-induced enhanced glycolysis is neuroprotective in Parkinson disease cell models. Sci Rep. 2016 May 5;6:25344