Trimethobenzamide HCl | 盐酸曲美苄胺 | Ro 2-9578 | Influenza Virus Inhibitor

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Trimethobenzamide HCl/盐酸三甲氧苯酰胺 {[allProObj[0].p_purity_real_show]}

货号：A148362 同义名： 盐酸曲美苄胺 / Ro 2-9578; Trimethobenzamide (hydrochloride)

Trimethobenzamide HCl is a dopamine D2 receptor antagonist and antiemetic drug.

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Trimethobenzamide HCl/盐酸三甲氧苯酰胺化学结构
CAS号：554-92-7

Trimethobenzamide HCl/盐酸三甲氧苯酰胺 3D分子结构
CAS号：554-92-7

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Trimethobenzamide HCl/盐酸三甲氧苯酰胺纯度/质量文件产品仅供科研

货号：A148362 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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多巴胺受体亚型比较

产品名称	D1 receptor ↓ ↑	D2 receptor ↓ ↑	D3 receptor ↓ ↑	D4 receptor ↓ ↑	D5 receptor ↓ ↑	DAT ↓ ↑	Dopamine receptor ↓ ↑	其他靶点	纯度
Penfluridol	+ Dopamine receptor, Ki: 1.6 μM								98%
Ansofaxine HCl	++ Dopamine receptor, IC50: 491 nM								99%
Tetrahydroberberine		+ D2 receptor, pKi: 6.08							98+%
Prochlorperazine Maleate		✔							98% (HPLC)
Olanzapine		✔							99+%
Trifluoperazine		++++ Dopamine D2 receptor, IC50: 1.1 nM							98%
Ropinirole HCl		++ D2 receptor, Ki: 29 nM							99%
Lurasidone		++++ D2 receptor, Ki: 1 nM							98%
Levosulpiride		✔							99+%
Pridopidine		✔							95%
Metoclopramide		✔					✔		99+%
Molindone HCl		✔							99%
Sulpiride		✔							99+%
Perospirone		++++ D2 receptor, Ki: 1.4 nM							99%
Perospirone HCl		++++ D2 receptor, Ki: 1.4 nM							99%
Phenothiazine		✔							98%
Pimozide	+ Dopamine D1 receptor, Ki: 6600 nM	+++ Dopamine D2 receptor, Ki: 3.0 nM	++++ Dopamine D3 receptor, Ki: 0.83 nM						98%
Rotundine	++ D1 receptor, IC50: 166 nM	+ D2 receptor, IC50: 1.47 μM	+ D3 receptor, IC50: 3.25 μM						98%
Domperidone		✔							99+%
ONC206		✔							99%
Pimethixene maleate	++ Dopamine D1 Receptor, pKi: 6.37	+++ Dopamine D2 Receptor, pKi: 8.19		++ Dopamine D4.4 Receptor, pKi: 7.54					97%
Loxapine succinate	++ D2 receptor (Human), Ki: 62 nM D1 receptor (human), Ki: 26 nM	++ D2 receptor (bovine), Ki: 26 nM D2 receptor (human), Ki: 24 nM		+++ D4 receptor (human), Ki: 7.5 nM					98%
Chlorprothixene	+++ D1 receptor, Ki: 18 nM	+++ D2 receptor, Ki: 2.96 nM	+++ D3 receptor, Ki: 4.56 nM		+++ D5 receptor, Ki: 9 nM				99%
SCH-23390 HCl	++++ D1 dopamine receptor, Ki: 0.2 nM				++++ D5 dopamine receptor, Ki: 0.3 nM				98%
MPP+ iodide						✔			97%
σ1 Receptor antagonist-1						+ DAT, pKi: 5.8			97%
Benztropine mesylate						++ DAT, IC50: 118 nM			98%
Azaperone							✔		98%
Ziprasidone HCl							✔		98+%
Paliperidone							✔		98%
Alizapride HCl							✔		99+%
Amisulpride							✔		98%
Quetiapine hemifumarate							✔	Adrenergic Receptor	98%
Clozapine N-oxide							✔		99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Trimethobenzamide HCl/盐酸三甲氧苯酰胺生物活性

描述

Trimethobenzamide HCl is a blocker of the D2 receptor. Trimethobenzamide is an antiemetic used to prevent nausea and vomiting. Trimethobenzamide is a (non-phenothiazine) benzamide antiemetic that acts centrally to block D2 receptors, thereby inhibiting the medullary chemoreceptor trigger zone by blocking emetic impulses to the vomiting center^[1]. Trimethobenzamide was shown to be significantly better than placebo in relieving periodic and total nausea over the 48-hour study. Vomiting incidence was also reduced in the group receiving trimethobenzamide^[2]. Trimethobenzamide HCl was found to have more toxic and teratogenic potential on embryonic growth and development in cultured rat embryos^[3]. Open-label studies suggest that the combination of trimethobenzamide and diphenhydramine (TMB/DPH) may provide effective relief in a high proportion of migraineurs^[4]. In utero TMB (Trimethobenzamide) exposure may cause growth retardation, neurological damage in the developing brain and intestine, and hepatic damage^[5].

Trimethobenzamide HCl/盐酸三甲氧苯酰胺临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00626327	Meningococcal Infections	Phase 3	Completed	-	-
NCT00626327	-		Completed	-	-
NCT00806195	-		Completed	-	-

Trimethobenzamide HCl/盐酸三甲氧苯酰胺参考文献

[1]Smith HS, Cox LR, Smith BR. Dopamine receptor antagonists. Ann Palliat Med. 2012;1(2):137‐142

[2]Hurley JD, Eshelman FN. Trimethobenzamide HCl in the treatment of nausea and vomiting associated with antineoplastic chemotherapy. J Clin Pharmacol. 1980;20(5-6 Pt 1):352‐356

[3]Fazliogullari Z, Karabulut AK, Uysal II, Unver Dogan N, Acar H. Investigation of developmental toxicity and teratogenicity of antiemetics on rat Fazliogullari Z, Karabulut AK, Uysal II, Unver Dogan N, Acar H. Investigation of developmental toxicity and teratogenicity of antiemetics on rat embryos cultured in vitro. Anat Histol Embryol. 2013;42(4):239‐246embryos cultured in vitro. Anat Histol Embryol. 2013;42(4):239‐246

[4]Friedman BW, Hochberg M, Esses D, et al. A clinical trial of trimethobenzamide/diphenhydramine versus sumatriptan for acute migraines. Headache. 2006;46(6):934‐941

[5]Goksu Erol AY, Gokcimen A, Ozdemir O. Growth failure, tardive dyskinesia, megacolon development, and hepatic damage in neonatal rats following exposure to trimethobenzamide in utero. J Matern Fetal Neonatal Med. 2011;24(9):1176‐1180

Trimethobenzamide HCl/盐酸三甲氧苯酰胺实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.24mL

11.77mL

2.35mL

1.18mL

23.53mL

4.71mL

2.35mL

Trimethobenzamide HCl/盐酸三甲氧苯酰胺技术信息

CAS号	554-92-7
分子式	C₂₁H₂₉ClN₂O₅
分子量	424.92
SMILES Code	O=C(NCC1=CC=C(OCCN(C)C)C=C1)C2=CC(OC)=C(OC)C(OC)=C2.[H]Cl
MDL No.	MFCD00057999

别名	盐酸曲美苄胺 ;Ro 2-9578; Trimethobenzamide (hydrochloride); Trimethobenzamide hydrochloride
运输	蓝冰
InChI Key	WIIZEEPFHXAUND-UHFFFAOYSA-N
Pubchem ID	68385

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

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

NCT00626327	Meningococcal Infections	Phase 3	Completed	-	-
NCT00626327	-		Completed	-	-
NCT00806195	-		Completed	-	-
NCT01345630	HIV-1	Phase 3	Terminated(See termination rea... 展开 >>son in detailed description.) 收起 <<	-	-
NCT02556372	Autoimmune Hepatitis	Phase 2	Active, not recruiting	December 2018	United States, California ... 展开 >> Ruane Clinical Research Group, Inc. Los Angeles, California, United States, 90036 University of California Davis Medical Center - Ticon 1 Sacramento, California, United States, 95817 California Pacific Medical Center San Francisco, California, United States United States, Florida University of Florida Hepatology Research at CTRB Gainesville, Florida, United States, 32610-0272 United States, Illinois Northwestern University Chicago, Illinois, United States, 60611 United States, Indiana Indiana University School of Medicine Indianapolis, Indiana, United States, 46202 United States, Louisiana Tulane University New Orleans, Louisiana, United States United States, Massachusetts Massachusetts General Hospital Boston, Massachusetts, United States United States, New York Mount Sinai Hospital New York, New York, United States, 10029 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Texas Methodist Dallas Medical Center Dallas, Texas, United States, 75203 Advanced Liver Therapies, Baylor College of Medicine Houston, Texas, United States, 77030 The Texas Liver Institute San Antonio, Texas, United States, 78215 Taxes Liver Institute San Antonio, Texas, United States United States, Washington Swedish Medical Center - Organ Transplant and Liver Center Seattle, Washington, United States, 98104 University of Washington Seattle, Washington, United States, 98104 收起 <<
NCT00834704	Solid Tumor	Phase 1	Completed	-	United States, Arizona ... 展开 >> T Gen Clinical Research Services Scottsdale, Arizona, United States, 85258 United States, California Premiere Oncology Santa Monica, California, United States, 90404 United States, Tennessee Sarah Cannon Research Institute Nashville, Tennessee, United States, 37203 收起 <<
NCT00397748	-		Completed	-	United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 收起 <<
NCT00806195	Meningitis Me... 展开 >>ningococcal Infection 收起 <<	Phase 3	Completed	-	-
NCT01345630	-		Terminated(See termination rea... 展开 >>son in detailed description.) 收起 <<	-	-
NCT01882465	Refractive Error	Not Applicable	Terminated	-	Hong Kong ... 展开 >> Hong Kong Polytechnic University Hong Hom, Kowloon, Hong Kong 收起 <<
NCT01882465	-		Terminated	-	-
NCT00029510	Asthma	Phase 2	Completed	-	United States, California ... 展开 >> University of California at Davis School of Medicine, Ticon 1, Suite 100B, 2000 Stockton Blvd Sacramento, California, United States, 95817 收起 <<
NCT02373072	Idiopathic Parkinson Disease	Phase 1	Completed	-	United States, California ... 展开 >> Collaborative Neuroscience Network, LLC. Long Beach, California, United States, 90806 United States, Florida MD Clinical Hallandale, Florida, United States, 33009 United States, Georgia Atlanta Center for Medical Research Atlanta, Georgia, United States, 30331 United States, Maryland SNBL Clinical Pharmacology Center, Inc. Baltimore, Maryland, United States, 21201 Parkinson's Movement Disorder Center of Maryland Elkridge, Maryland, United States, 21075 United States, Texas Neurology Consultants of Dallas, PA Dallas, Texas, United States, 75231 Walnut Hill Medical Center Dallas, Texas, United States, 75231 Belgium Pfizer Clinical Research Unit Brussels, Belgium, B-1070 收起 <<
NCT01770145	Parkinson's Disease ... 展开 >> Motor Symptoms Akinesia Hypomobility Delayed Levodopa Onset 收起 <<	Phase 4	Completed	-	United States, California ... 展开 >> Keck School of Medicine Los Angeles, California, United States, 90033 Neurosearch, Inc. Reseda, California, United States, 91335 United States, District of Columbia Georgetown University Washington, D.C., District of Columbia, United States, 20007 United States, Florida Parkinson's Disease and Movement Disorders Center of Boca Raton Boca Raton, Florida, United States, 33486 United States, Illinois Rush University Medical Center Chicago, Illinois, United States, 60612 United States, Michigan Henry Ford West Bloomfield Hospital Bloomfield Hills, Michigan, United States, 48322 United States, New York Parkinson's Disease and Movement Disorders Center of New York Commack, New York, United States, 11725 United States, Ohio University of Cincinnati Academic Health Center Cincinnati, Ohio, United States, 45267 University Hospitals Case Medical Center Cleveland, Ohio, United States, 44106 United States, Oklahoma The Movement Disorder Clinic of Oklahoma Tulsa, Oklahoma, United States, 74136 United States, Texas University of Texas Health Science Center, Houston, Department of Neurology Houston, Texas, United States, 77030 Center for Neurological Care and Research San Antonio, Texas, United States, 78240 收起 <<
NCT01770145	-		Completed	-	-
NCT00489255	Parkinson's Disease	Phase 4	Completed	-	-
NCT02262767	Healthy	Phase 1	Completed	-	Belgium ... 展开 >> Belgium Pfizer Clinical Research Unit Brussels, Belgium, 1070 Pfizer Clinical Research Unit Brussels, Belgium, B-1070 收起 <<
NCT00489255	-		Completed	-	-
NCT00536185	Heart Disease	Not Applicable	Completed	-	United States, California ... 展开 >> UC Davis, Western Human Nutrition Research Center Davis, California, United States, 95616 Ethnich Health Institute Oakland, California, United States, 94609 UC Davis (TICON-1) Sacramento, California, United States, 95820 收起 <<
NCT03164551	Infertility	Phase 4	Recruiting	March 30, 2020	Canada ... 展开 >> Cambrian Wellness Centre Recruiting Calgary, Canada, T3B 4N2 Denmark Skive Fertility clinic Recruiting Skive, Denmark, 7800 France Hopital Antoine Beclere Not yet recruiting Clamart, France, 92140 Italy Krankenhaus Bruneck Not yet recruiting Bruneck (BZ), Italy, I-39031 Demetra S.R.L Not yet recruiting Firenze, Italy, 50141 Futura Diagnostica medica PMA SRL Not yet recruiting Firenze, Italy, SO129 Unita' di medicina della riproduzione - centro Hera Withdrawn Sant'Agata Li Battiali(CT), Italy, 95030 USL Toscana Nordovest Not yet recruiting Viareggio, Italy, 55043 Norway Oslo University Hospital Recruiting Oslo, Norway Contact +49 6151 72 5200 Sykehuset Telemark HF Fertilitetsavdeliningen Sor Recruiting Skien, Norway, 3710 St. Olavs Hospital Hf, Universitetssykehuset i Trondheim Recruiting Trodheim, Norway, N-7006 Portugal Centro Hospitalar e Universitario de Coimbra Recruiting Coimbra, Portugal, 3000-075 Spain Hospital de Cruces Recruiting Baracaldo, Spain, 48903 Nephrology Service Fundacion Puigvert Recruiting Barcelona, Spain, 8025 Hospital Universitario Virgen de las Nieves Recruiting Granada, Spain Hosp Univ de Canarias Not yet recruiting Santa Cruz de Tenerife, Spain United Kingdom Barts Health Centre for Reproductive medicine Withdrawn London, United Kingdom, EC1A7BE 收起 <<

Trimethobenzamide HCl/盐酸三甲氧苯酰胺 {[allProObj[0].p_purity_real_show]}

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Trimethobenzamide HCl/盐酸三甲氧苯酰胺生物活性

Trimethobenzamide HCl/盐酸三甲氧苯酰胺临床研究

Trimethobenzamide HCl/盐酸三甲氧苯酰胺参考文献

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Trimethobenzamide HCl/盐酸三甲氧苯酰胺纯度/质量文件产品仅供科研

Trimethobenzamide HCl/盐酸三甲氧苯酰胺质控信息

Trimethobenzamide HCl/盐酸三甲氧苯酰胺生物活性

Trimethobenzamide HCl/盐酸三甲氧苯酰胺临床研究

Trimethobenzamide HCl/盐酸三甲氧苯酰胺参考文献

Trimethobenzamide HCl/盐酸三甲氧苯酰胺实验方案

Trimethobenzamide HCl/盐酸三甲氧苯酰胺技术信息