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Merck
CN

T8200

Sigma-Aldrich

Tofisopam

≥98% (HPLC), solid

别名:

7,8-Dimethoxy-1-(3,4-dimethoxyphenyl)-5-ethyl-4-methyl-5H-2,3-benzodiazepine, EGYT 341, Seriel

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关于此项目

经验公式(希尔记法):
C22H26N2O4
化学文摘社编号:
分子量:
382.45
EC 号:
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
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质量水平

方案

≥98% (HPLC)

表单

solid

药品控制

regulated under CDSA - not available from Sigma-Aldrich Canada

颜色

white

溶解性

DMSO: ~14 mg/mL
H2O: insoluble

SMILES字符串

CCC1C(C)=NN=C(c2ccc(OC)c(OC)c2)c3cc(OC)c(OC)cc13

InChI

1S/C22H26N2O4/c1-7-15-13(2)23-24-22(14-8-9-18(25-3)19(10-14)26-4)17-12-21(28-6)20(27-5)11-16(15)17/h8-12,15H,7H2,1-6H3

InChI key

RUJBDQSFYCKFAA-UHFFFAOYSA-N

应用

Tofisopam has been used for studying its biochemical mechanisms of actions using drug repositioning strategies.

生化/生理作用

Ligand for the GABAA receptor benzodiazepine modulatory site.
Studies have reported that tofisopam functions by blocking PDE4 (phosphodiesterase 4). Furthermore, the S-enantiomer of tofisopam is considered ten times more active than R-enantiomer.

制备说明

Tofisopam is soluble in DMSO at approximately 14 mg/ml. However, it is insoluble in water.

象形图

Exclamation markEnvironment

警示用语:

Warning

危险声明

预防措施声明

危险分类

Acute Tox. 4 Oral - Aquatic Acute 1

储存分类代码

11 - Combustible Solids

WGK

WGK 2

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

dust mask type N95 (US), Eyeshields, Gloves

法规信息

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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[Grandaxin in neurological practice].
G M Diukova et al.
Zhurnal nevrologii i psikhiatrii imeni S.S. Korsakova, 109(9), 44-48 (2009-11-17)
P Bernard et al.
Current medicinal chemistry, 15(30), 3196-3203 (2008-12-17)
Drug repositioning strategy is an interesting approach for pharmaceutical companies; especially to increase their productivity. SELNERGY(tm) is a reverse docking based-program able to virtually screen thousands of compounds on more than 2000 3D biological targets. This program was successfully applied
Soo Kyoung Baek et al.
Biomedical chromatography : BMC, 16(4), 277-281 (2002-04-05)
A rapid and sensitive column-switching semi-micro HPLC method is described for the direct analysis of tofisopam in human serum. The sample (100 microL) was directly injected onto the precolumn (Capcell Pak MF Ph-1), where unretained proteins were eluted to waste.
Drug repositioning: identifying and developing new uses for existing drugs.
Ted T Ashburn et al.
Nature reviews. Drug discovery, 3(8), 673-683 (2004-08-03)
N P Vanchakova et al.
Bulletin of experimental biology and medicine, 148(2), 343-345 (2009-12-23)
The study demonstrated high anxiolytic activity of tenoten, which was not inferior to the anxiolytic effect of grandaxin. The positive changes persisted after termination of treatment in the tenoten group (but not in grandaxin group). Tenoten can be recommended for

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