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Tofisopam

产品号 DB08811 公司名称 DrugBank
CAS号 22345-47-7 公司网站 http://www.ualberta.ca/
分子式 C22H26N2O4 电 话 (780) 492-3111
分子量 382.45284 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 6411

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产品别名

标题
Tofisopam
IUPAC标准名
1-(3,4-dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5H-2,3-benzodiazepine
IUPAC传统名
tofisopam
商标名
Grandaxin
Emandaxin
Seriel
别名
Tofizopam

产品登记号

CAS号 22345-47-7

产品性质

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved
Description 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.
Indication For the treatment of anxiety and alcohol withdrawal.
Pharmacology 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).
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
Biotransformation Hepatic.
Half Life 6-8 hours
References
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]
External Links
Wikipedia

参考文献

  • 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