推薦產品
化驗
≥98% (HPLC)
形狀
solid
藥物控制
regulated under CDSA - not available from Sigma-Aldrich Canada
顏色
white
溶解度
DMSO: ~14 mg/mL
H2O: insoluble
SMILES 字串
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 密鑰
RUJBDQSFYCKFAA-UHFFFAOYSA-N
應用
Tofisopam has been used for studying its biochemical mechanisms of actions using drug repositioning strategies.
生化／生理作用
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.
Ligand for the GABAA receptor benzodiazepine modulatory site.
準備報告
Tofisopam is soluble in DMSO at approximately 14 mg/ml. However, it is insoluble in water.
訊號詞
Warning
危險聲明
危險分類
Acute Tox. 4 Oral - Aquatic Acute 1
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 2
閃點（°F）
Not applicable
閃點（°C）
Not applicable
個人防護裝備
dust mask type N95 (US), Eyeshields, Gloves
分析證明 (COA)
輸入產品批次/批號來搜索 分析證明 (COA)。在產品’s標籤上找到批次和批號，寫有 ‘Lot’或‘Batch’.。
Maria Tóth et al.
Journal of pharmaceutical and biomedical analysis, 41(4), 1354-1359 (2006-05-10)
Tofisopam (1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7,8-dimethoxy-5H-2,3-benzodiazepine) has been shown to be an effective anxiolytic agent in the wide-ranging clinical practice. A high sensitive gas chromatography nitrogen phosphorous detection (GC-NPD) bioanalytical method was developed and validated for the purpose of pharmacokinetic study of tofisopam. A
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)
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
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.
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