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:
产品名称
Tofisopam, ≥98% (HPLC), solid
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
N Bonnet et al.
Toxicology and applied pharmacology, 221(1), 111-118 (2007-03-27)
The aim of this study was to evaluate the effects of various drugs which present antidepressant properties: selective serotonin-reuptake inhibitors (SSRIs, fluoxetine), serotonin and noradrenaline-reuptake inhibitors (Desipramine) and phosphodiesterase inhibitors (PDE, rolipram and tofisopam) on bone microarchitecture and biomechanical properties.
Michael D Cameron et al.
Drug metabolism and disposition: the biological fate of chemicals, 35(10), 1894-1902 (2007-07-25)
In vitro studies were conducted to elucidate the metabolic profiles of and the enzymes responsible for the metabolism of (R)- and (S)-tofisopam (1-(3,4-dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5H-2,3-benzodiazepine). Large differences were observed between the two enantiomers. The major metabolite in incubations of 500 ng/ml (approximately
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.
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
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)
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