Benztropine mesylate | 苯托品甲磺酸盐 | Benztropine methanesulfonate | Anticholinergic Agent

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甲磺酸苯扎托品 /Benztropine mesylate {[allProObj[0].p_purity_real_show]}

货号：A308385 同义名： 苯托品甲磺酸盐 / Benztropine methanesulfonate;Benzotropine mesylate

Benztropine mesylate is a central muscarinic antagonist and a DAT inhibitor with IC50 of 118 nM, indicated for symptomatic relief of parkinsonism and drug-induced extrapyramidal reactions.

Benztropine mesylate 化学结构
CAS号：132-17-2

Benztropine mesylate 3D分子结构
CAS号：132-17-2

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Benztropine mesylate 纯度/质量文件产品仅供科研

货号：A308385 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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AChR 亚型比较

产品名称	AChE ↓ ↑	AChR ↓ ↑	mAChR ↓ ↑	nAChR ↓ ↑	其他靶点	纯度
Donepezil	+++ bAChE, IC50: 8.12 nM hAChE, IC50: 11.6 nM					98%
Loganin	++ AChE, IC50: 3.95 μM					99%+
topride HCl	++ AChE, IC50: 2.04 μM					98%
Dehydroevodiamine HCl	✔					99%+
Jatrorrhizine	++ AChE, IC50: 872 nM					99%+
Palmatine	++ AChE, IC50: 0.51 μM					98%
(-)-Huperzine A	++++ AChE (G4 form), Ki: 7 nM					98%
Galanthamine HBr	++ AChE, IC50: 0.35 μM					98%
Trospium chloride		✔				99%
Tiotropium Bromide Monohydrate		✔				98+%
Gallamine Triethiodide		+ AChR, IC50: 68.0 μM				98%
Hexamethonium Bromide		✔				99%
Pancuronium dibromide		✔				98%
Neostigmine bromide		✔				98%
Orphenadrine citrate		✔				98%
Oxybutynin		✔				98%
Irsogladine		✔			PDE	98%
Pyridostigmine bromide		✔				99+%
Rivastigmine		+ AChR, IC50: 5.5 μM				98%
Paroxetine hydrochloride		✔				97%
Rocuronium Bromide		✔				98%
Tropicamide			+++ M4 mAChR, IC50: 8 nM			98%
Diphenmanil methylsulfate			✔			98%
Umeclidinium bromide			✔			95%
Otilonium bromide			✔			98%
Flavoxate HCl			+ mAChR, IC50: 12.2 μM			98%
Ipratropium bromide			✔			98%
Diphenidol HCl			✔			98%
Darifenacin hydrobromide			++++ M3 mAChR, pKi: 8.9			98%
Aclidinium Bromide			++++ M2 mAChR, Ki: 0.1 nM M4 mAChR, Ki: 0.21 nM			98%
Oxybutynin chloride			✔			99%
Pentoxyverine citrate			✔			98%
Solifenacin			✔			98%
Catharanthine				✔		98%
Benzethonium chloride				+++ α4β2 nAChRs, IC50: 49 nM α7 nAChRs, IC50: 122 nM		99+%
Vinblastine sulfate				+ nAChR, IC50: 8.9 μM		99%
PNU-120596				++ α7 nAChR, EC50: 216 nM		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。

Benztropine mesylate 生物活性

靶点

DAT

DAT, IC50:118 nM

描述

Benztropine mesylate is a centrally acting anticholinergic agent for the treatment of Parkinson's disease. In a multiple sclerosis mouse model, benztropine mesylate induced the differentiation of oligodendrocytes through M1 and M3 muscarinic receptors and enhanced re-myelination. Benztropine mesylate also acts as an anti-histamine and a dopamine re-uptake inhibitor, and as an allosteric antagonist of the human D2 dopamine receptor. For 4T1-luc2 spheres, the IC₅₀ value of benztropine mesylate was around 5 μM^[3]. Benztropine (BZT) and its analogues inhibit dopamine uptake and bind with moderate to high affinity to the dopamine transporter (DAT). The BZT analogues showed a wide range of histamine H(1) receptor (K_i=16-37,600 nM) and DAT (K_i=8.5-6370 nM) binding affinities^[4].

Benztropine mesylate 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
NCT01833897	Bipolar Disorder	Phase 4	Completed	-	United States, New York ... 展开 >> New York State Psychiatric Institute New York, New York, United States, 10032 收起 <<
NCT00009672	Radiculopathy ... 展开 >> Sciatica 收起 <<	Phase 2	Completed	-	United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 收起 <<
NCT00167856	Neuropathic Pain ... 展开 >> Pain Spinal Cord Injuries 收起 <<	Not Applicable	Completed	-	United States, Florida ... 展开 >> VA Medical Center, Miami Miami, Florida, United States, 33125 收起 <<

Benztropine mesylate 参考文献

[1]Simoni D, Rossi M, et al. Synthesis and pharmacology of 6-substituted benztropines: discovery of novel dopamine uptake inhibitors possessing low binding affinity to the dopamine transporter. J Med Chem. 2005 May 5;48(9):3337-43.

[2]Reith ME, Berfield JL, et al. The uptake inhibitors cocaine and benztropine differentially alter the conformation of the human dopamine transporter. J Biol Chem. 2001 Aug 3;276(31):29012-8.

[3]Cui J, Hollmén M, Li L, Chen Y, Proulx ST, Reker D, Schneider G, Detmar M. New use of an old drug: inhibition of breast cancer stem cells by benztropine mesylate. Oncotarget. 2017 Jan 3;8(1):1007-1022. doi: 10.18632/oncotarget.13537. PMID: 27894093; PMCID: PMC5352030.

[4]Kulkarni SS, Kopajtic TA, Katz JL, Newman AH. Comparative structure-activity relationships of benztropine analogues at the dopamine transporter and histamine H(1) receptors. Bioorg Med Chem. 2006 Jun 1;14(11):3625-34. doi: 10.1016/j.bmc.2006.01.017. Epub 2006 Feb 3. PMID: 16460947; PMCID: PMC1555624.

Benztropine mesylate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.48mL

0.50mL

0.25mL

12.39mL

2.48mL

1.24mL

24.78mL

4.96mL

2.48mL

Benztropine mesylate 技术信息

CAS号	132-17-2
分子式	C₂₂H₂₉NO₄S
分子量	403.535

别名	苯托品甲磺酸盐 ;Benztropine methanesulfonate;Benzotropine mesylate;ST50997629;NSC42199;MLS000737056;Cogentin;NSC 169913;Benztropine (mesylate);Cogentin mesylate;Benzatropine mesylate
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

DMSO: 105 mg/mL(260.2 mM)，配合低频超声助溶，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

H₂O: 100 mg/mL(247.81 mM)，配合低频超声助溶

动物实验配方

PO 0.5% CMC-Na 60 mg/mL clear

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

NCT01833897	Bipolar Disorder	Phase 4	Completed	-	United States, New York ... 展开 >> New York State Psychiatric Institute New York, New York, United States, 10032 收起 <<
NCT00009672	Radiculopathy ... 展开 >> Sciatica 收起 <<	Phase 2	Completed	-	United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 收起 <<
NCT00167856	Neuropathic Pain ... 展开 >> Pain Spinal Cord Injuries 收起 <<	Not Applicable	Completed	-	United States, Florida ... 展开 >> VA Medical Center, Miami Miami, Florida, United States, 33125 收起 <<
NCT00802100	Schizophrenia	Phase 4	Completed	-	United States, California ... 展开 >> SHANTI Clinical Trials Colton, California, United States, 92324 Stanford University Palo Alto, California, United States, 94305 United States, Connecticut Yale University New Haven, Connecticut, United States, 06519 United States, Florida University of Miami School of Medicine Miami, Florida, United States, 33316 United States, Georgia Medical College of Georgia Augusta, Georgia, United States, 30912 United States, Maryland Clinical Insights Glen Burnie, Maryland, United States, 21061 United States, Massachusetts University of Massachusetts Worcester, Massachusetts, United States, 01605 United States, Michigan Wayne State University Detroit, Michigan, United States, 48201 United States, Minnesota University of Minnesota School of Medicine Minneapolis, Minnesota, United States, 55454 United States, New York Research Foundation for Mental Hygiene New York, New York, United States, 10032 United States, North Carolina Duke University Medical Center-John Umstead Hospital Butner, North Carolina, United States, 27509 United States, Texas University of Texas Southwestern Medical Center Dallas, Texas, United States, 75235 Baylor College of Medicine Houston, Texas, United States, 77030 收起 <<
NCT00802100	-		Completed	-	-
NCT00964886	Back Pain	Phase 2	Completed	-	United States, California ... 展开 >> VA San Diego Healthcare System, San Diego, CA San Diego, California, United States, 92161 收起 <<
NCT00066937	Temporomandibular Joint Disord... 展开 >>ers 收起 <<	Phase 2	Completed	-	United States, Maryland ... 展开 >> University of Maryland, Dental School Baltimore, Maryland, United States, 21201 收起 <<
NCT00066937	-		Completed	-	-
NCT00457366	Agitation	Phase 4	Completed	-	United States, California ... 展开 >> Los Angeles County Hospital Los Angeles, California, United States, 90033 收起 <<
NCT00715377	Schizophrenia ... 展开 >> Schizoaffective Disorder Schizophreniform Disorder Delusional Disorder Psychotic Disorders 收起 <<	Not Applicable	Terminated(Insufficient subjec... 展开 >>t accrual) 收起 <<	-	Canada, Ontario ... 展开 >> Centre for Addiction and Mental Health Toronto, Ontario, Canada, M5T 1R8 收起 <<
NCT00018200	Back Pain Sci... 展开 >>atica 收起 <<	Phase 2	Completed	-	United States, California ... 展开 >> VA San Diego Healthcare System, San Diego San Diego, California, United States, 92161 收起 <<
NCT00964886	-		Completed	-	-
NCT00000793	HIV Infections ... 展开 >> Peripheral Nervous System Disease 收起 <<	Phase 2	Completed	-	-
NCT00000333	Cocaine-Related Disorders	Phase 2	Completed	-	United States, District of Col... 展开 >>umbia Washington DC VA Washington, District of Columbia, United States, 20422 收起 <<
NCT01833897	-		Completed	-	-

甲磺酸苯扎托品 /Benztropine mesylate {[allProObj[0].p_purity_real_show]}

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最近浏览的产品

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