Tofisopam

Tofisopam is an atypical 2,3-benzodiazepine anxiolytic. Unlike classical 1,4-benzodiazepines, it does not typically cause sedation, muscle relaxation, or anticonvulsant effects. Its primary mechanism of action involves the selective inhibition of phosphodiesterase (PDE) enzymes, particularly PDE4, PDE10, PDE3, and PDE2, leading to increased intracellular cAMP levels. While it is classified as a benzodiazepine, it does not bind to the classical benzodiazepine binding site of the GABA-A receptor. However, it is reported to modulate GABA-A receptor activity or act as a GABA-A receptor agonist, contributing to its anxiolytic effects. It may also influence dopaminergic and serotonergic systems, as well as the autonomic nervous system. Tofisopam is used for anxiety, depression, alcohol withdrawal, and stress-related disorders. It is marketed in several European and Asian countries but is not approved in the United States or Canada.

Brand names

EmandaxinGrandaxinSérielToficalmNextrilTolrinaTofirydTofirexTofypeaceTofirantTofiuseCalmreyTopysoTOFIZINTofiliveTOFIC

Other names

TofisopamumUZC80HAU42UZC-80HAU42UZC 80HAU42DTXSID3023681DTXSID-3023681DTXSID 3023681DTXCID303681DTXCID-303681DTXCID 303681RefChem:898544N05BA23N-05BA23N 05BA23(5RS)-1-(3,4-Dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5H-2,3-benzodiazepine244-922-3MFCD00823171MFCD-00823171MFCD 008231715H-2,3-Benzodiazepine, 1-(3,4-dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-1-(3,4-Dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5H-benzo[d][1,2]diazepineNCGC00165912-02NCGC-00165912-02NCGC 00165912-02benzodiazepine; EGYT 341; Grandaxin; Nodeprine; SerielTofisopamum [INN-Latin]Tofisopam [INN:DCF:JAN]tofizopam