T8200
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
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
EC Number:
244-922-3
MDL number:
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
SMILES string
CCC1C(C)=NN=C(c2ccc(OC)c(OC)c2)c3cc(OC)c(OC)cc13
assay
≥98% (HPLC)
form
solid
drug control
regulated under CDSA - not available from Sigma-Aldrich Canada
color
white
solubility
DMSO: ~14 mg/mL, H2O: insoluble
Quality Level
Application
Tofisopam has been used for studying its biochemical mechanisms of actions using drug repositioning strategies.
Biochem/physiol Actions
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.
Preparation Note
Tofisopam is soluble in DMSO at approximately 14 mg/ml. However, it is insoluble in water.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Aquatic Acute 1
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
法规信息
新产品
此项目有
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
[Grandaxin in neurological practice].
G M Diukova et al.
Zhurnal nevrologii i psikhiatrii imeni S.S. Korsakova, 109(9), 44-48 (2009-11-17)
Mougang Hu et al.
Journal of chromatography. A, 1129(1), 47-53 (2006-07-18)
1-(3,4-Dimethoxyphenyl)-4-methyl-5-ethyl-7,8-dimethoxy-5H-2,3-benzodiazepine (tofisopam) contains one chiral center, so two enantiomeric forms exist. The ring system of tofisopam possesses two sterically stable boat structures, leading to two distinct conformers for each enantiomer. A method was developed for the separation of these enantiomers
Tofisopam inhibits the pharmacokinetics of CYP3A4 substrate midazolam.
Mária Tóth et al.
European journal of clinical pharmacology, 64(1), 93-94 (2007-11-09)
Yue Fan et al.
Neuroscience letters, 736, 135262-135262 (2020-07-20)
Spinal cord injury (SCI) is a traumatic condition of the central nervous system (CNS) that can cause paralysis of the limbs. The molecular mechanisms of neural repair following SCI remain unclear and no effective treatment for SCI currently exists, since
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