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药品详细

Tofisopam(托非索泮)

化学结构式图
中文名
托非索泮
英文名
Tofisopam
分子式
C22H26N2O4
化学名
1-(3,4-dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5H-2,3-benzodiazepine
分子量
Average: 382.4528
Monoisotopic: 382.18925733
CAS号
22345-47-7
ATC分类
N05B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Tofisopam (marketed under brand names Emandaxin and Grandaxin) is a 2,3-benzodiazepine drug which is a benzodiazepine derivative. In contrast to classical 1,4-benzodiazepines, the compound does not bind to the benzodiazepine binding site of the gamma-aminobutyric acid receptor and its psychopharmacological profile differs from such compounds. Although Tofisopam is not approved for sale in North America, it is approved for use in various countries worldwide, including parts of Europe. The D-enantiomer (dextofisopam) is currently in phase II trials in the U.S. for the treatment of irritable bowel syndrome.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Rundfeldt C, Socala K, Wlaz P: The atypical anxiolytic drug, tofisopam, selectively blocks phosphodiesterase isoenzymes and is active in the mouse model of negative symptoms of psychosis. J Neural Transm. 2010 Nov;117(11):1319-25. Epub 2010 Oct 22. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes Not Available
    Substructures Not Available
    适应症
    药理
    Indication For the treatment of anxiety and alcohol withdrawal.
    Pharmacodynamics Like other benzodiazepines, tofisopam possesses anxiolytic properties but unlike other benzodiazepines it does not have anticonvulsant, sedative, skeletal muscle relaxant, motor skill-impairing or amnestic properties. While it may not be an anticonvulsant in and of itself, it has been shown to enhance the anticonvulsant action of classical 1,4-benzodiazepines such as diazepam (but not sodium valproate, carbamazepine, phenobarbital, or phenytoin).
    Mechanism of action Tofisopam does not bind to the benzodiazepine binding site of the gamma-aminobutyric acid receptor. One study (Rundfeldt C. et al.) has shown that tofisopam acts as an isoenzyme-selective inhibitor of phosphodiesterases (PDEs) with highest affinity to PDE-4A1 (0.42 μM) followed by PDE-10A1 (0.92 μM), PDE-3 (1.98 μM) and PDE-2A3 (2.11 μM).
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Hepatic.
    Route of elimination Not Available
    Half life 6-8 hours
    Clearance Not Available
    Toxicity The onset of impairment of consciousness is relatively rapid in benzodiazepine poisoning. Onset is more rapid following larger doses and with agents of shorter duration of action. The most common and initial symptom is somnolence. This may progress to coma (Grade I or Grade II) following very large ingestions. Oral, rat LD50 is 825 mg/kg.
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 156.5 °C PhysProp
    Predicted Properties
    Property Value Source
    water solubility 2.39e-03 g/l ALOGPS
    logP 4.29 ALOGPS
    logP 3.83 ChemAxon
    logS -5.2 ALOGPS
    pKa (strongest basic) -2.2 ChemAxon
    physiological charge 0 ChemAxon
    hydrogen acceptor count 6 ChemAxon
    hydrogen donor count 0 ChemAxon
    polar surface area 61.64 ChemAxon
    rotatable bond count 6 ChemAxon
    refractivity 109.03 ChemAxon
    polarizability 42.14 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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