About: Tofisopam

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An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

Attributes	Values
rdf:type	http://linked.opendata.cz/ontology/drugbank/Drug
http://linked.open...gbank/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. (en)
http://linked.open...generalReferences	# 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":http://www.ncbi.nlm.nih.gov/pubmed/20967473 (en)
http://linked.open...gy/drugbank/group	approved (en)
http://linked.open...drugbank/halfLife	6-8 hours (en)
http://linked.open...ugbank/indication	For the treatment of anxiety and alcohol withdrawal. (en)
sameAs	Tofisopam Tofisopam
Title	Tofisopam (en)
adms:identifier	http://linked.opendata.cz/resource/drugbank/drug/DB08811/identifier/drugbank/DB08811 http://linked.opendata.cz/resource/drugbank/drug/DB08811/identifier/kegg-drug/D01254 http://linked.opendata.cz/resource/drugbank/drug/DB08811/identifier/pharmgkb/PA165958428 http://linked.opendata.cz/resource/drugbank/drug/DB08811/identifier/wikipedia/Tofisopam
http://linked.open...mechanismOfAction	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). (en)
http://linked.open.../drugbank/synonym	Emandaxin (en) Tofizopam (en)
http://linked.open...drugbank/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. (en)
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http://linked.open...l/drug/hasATCCode	Tofisopam
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http://linked.open.../affectedOrganism	Humans and other mammals (en)
http://linked.open...casRegistryNumber	22345-47-7 (en)
http://linked.open...drugbank/category	(en)
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