|1-((4-氯苯基)(苯基)甲基)-4-(3-甲基苄基)哌嗪二盐酸盐|CsnPharm

CAS No.: 1104-22-9

盐酸美克洛嗪 Catalog No. CSN11366

Synonyms: NSC 28728;Meclizine (hydrochloride);Meclozine

Meclizine 2HCl is a histamine H1 receptor antagonist with Ki of 250 nM and is used to treat nausea and motion sickness.

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生物活性

实验方案

技术信息

生物活性

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... more >>ing Collapse <<	Not Applicable	Completed	-	United States, Tennessee ... more >> Vanderbilt University Medical Center Nashville, Tennessee, United States, 37212 Collapse <<
NCT02130622	-	-	Terminated(Lack of recruitment... more >>) Collapse <<	-	-
NCT02130622	Diabetic Gastroparesis	Phase 2	Terminated(Lack of recruitment... more >>) Collapse <<	-	United States, New Hampshire ... more >> Dartmouth-Hitchcock Medical Center Lebanon, New Hampshire, United States, 03756 Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1558 mL
- 10.7789 mL
- 21.5578 mL
- 5 mM
- 0.4312 mL
- 2.1558 mL
- 4.3116 mL
- 10 mM
- 0.2156 mL
- 1.0779 mL
- 2.1558 mL

技术信息

CAS号

1104-22-9

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H29Cl3N2

运输

蓝冰

分子量

463.87

别名

NSC 28728;Meclizine (hydrochloride);Meclozine;Meclizine hydrochloride;Meclizine Hcl;C25H27ClN2.2HCl.H2O;Roberts Brand of Meclizine Dihydrochloride;Ru-Vert-M;Torrens Brand of Meclizine Dihydrochloride;盐酸美克洛嗪;Meclozine dihydrochloride

溶解度

DMSO	4.0 mg/mL (8.6 mM) warming
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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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... more >>ing Collapse <<	Not Applicable	Completed	-	United States, Tennessee ... more >> Vanderbilt University Medical Center Nashville, Tennessee, United States, 37212 Collapse <<
NCT02130622	-	-	Terminated(Lack of recruitment... more >>) Collapse <<	-	-
NCT02130622	Diabetic Gastroparesis	Phase 2	Terminated(Lack of recruitment... more >>) Collapse <<	-	United States, New Hampshire ... more >> Dartmouth-Hitchcock Medical Center Lebanon, New Hampshire, United States, 03756 Collapse <<
NCT03586817	Nausea and Vomiting, Postopera... more >>tive Collapse <<	Phase 4	Not yet recruiting	August 1, 2019	Brazil ... more >> Hospital Federal de Bonsucesso Rio de Janeiro, Brazil, 21041-030 Collapse <<
NCT00641797	Benign Paroxysmal Positional V... more >>ertigo Collapse <<	Not Applicable	Completed	-	United States, Pennsylvania ... more >> Lehigh Valley Hospital Allentown, Pennsylvania, United States, 18103 Collapse <<
NCT03270839	Drug Reaction	Phase 4	Recruiting	May 1, 2018	Israel ... more >> Israeli Navy Medical Institute Recruiting Haifa, Israel Contact: Dror Tal, PhD +972549096080 tldror1@gmail.com Sub-Investigator: Daniel Lagami, BSc Collapse <<
NCT01537471	Healthy	Phase 1	Completed	-	United States, North Carolina ... more >> Duke University Medical Center Durham, North Carolina, United States, 27705 Collapse <<
NCT02112578	Vertigo, Peripheral	Phase 3	Unknown	December 2017	Brazil ... more >> Clinilive Not yet recruiting Maringá, Paraná, Brazil Contact: Antonio Carlos da Silva 55 44 30293004 Principal Investigator: Antonio Carolos da Silva Irmandade da Santa Casa de Misericórdia de São Paulo Recruiting São Paulo, SP, Brazil Contact: Monica Alcantra 55 11 21767235 Principal Investigator: José Eduardo Lutaif Dolci Alergoalpha Not yet recruiting Barueri, São Paulo, Brazil, 06454010 Contact: Thainara Bisognini 55 11 46882251 Principal Investigator: Karina Tavares Pesquisare Saude S/S Ltda Not yet recruiting Santo André, São Paulo, Brazil, 09080110 Contact: Amanda Faulhaber 55 11 44273339 Principal Investigator: Amanda Faulhaber Clinica de Alergia MarttiAntila Not yet recruiting Sorocaba, São Paulo, Brazil, 18040425 Contact: Simone Fernandes 55 15 35194909 Principal Investigator: Martti Anton Antila ISPEM Not yet recruiting São José dos Campos, São Paulo, Brazil, 12243280 Contact: Renata Bolsolani 55 12 39131789 Principal Investigator: Marcio Antonio Pereira CCBR SP Not yet recruiting São Paulo, Brazil, 04063001 Contact: Norton Sayeg, PhD 5511 43064691 Principal Investigator: Norton Sayeg, PhD Collapse <<
NCT00641797	-	-	Completed	-	-
NCT01443858	Smoking Cessation	Phase 2	Completed	-	United States, North Carolina ... more >> Duke Center for Nicotine and Smoking Cessation Research Charlotte, North Carolina, United States, 28210 Duke Center for Nicotine and Smoking Cessation Research Durham, North Carolina, United States, 27705 Duke Center for Nicotine and Smoking Cessation Research Raleigh, North Carolina, United States, 27609 Duke Center for Nicotine and Smoking Cessation Research Winston-Salem, North Carolina, United States, 27103 Collapse <<
NCT03253289	Carcinoma, Hepatocellular	Phase 1	Recruiting	May 1, 2019	United States, Texas ... more >> Baylor Clinic Recruiting Houston, Texas, United States, 77030 Contact: Brandon Smaglo, MD 713-798-3750 smaglo@bcm.edu Baylor St. Luke's Medical Center Recruiting Houston, Texas, United States, 77030 Contact: Brando Smaglo, MD 713-798-3750 smaglo@bcm.edu Dan L. Duncan Cancer Center at Baylor College of Medicine Recruiting Houston, Texas, United States, 77030 Contact: Clinical Trials Office - Dan L. Duncan Cancer Center at Baylor 713-798-1297 Collapse <<
NCT01443858	-	-	Completed	-	-

盐酸美克洛嗪 Catalog No. CSN11366

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