Originator
Grandaxine,Ozothine,France,1975
Uses
Tofisopam is a reagent used in preparation of allosteric ligands for pharmacological dark receptors GPR68 and GPR65. An anticonvulsant.
Definition
ChEBI: Tofisopam is an organic molecular entity.
Manufacturing Process
A mixture of 38.6 g (0.1 mol) of 3,4,3',4'-tetramethoxy-6-(α-acetopropyl)-
benzophenone, 5.5 g (0.11 mol) of 100% hydrazine hydrate or 3.52 g (0.11
mol) of hydrazine, and 500 ml of absolute ethanol is boiled for 5 hours. After adding 100 ml of benzene, 400 ml of solvent mixture is distilled off from the
reaction mixture by slow boiling for 3 hours. After cooling for 8 hours, 19 g of
5H-2,3-benzodiazepine derivative are separated from the residue as small,
white crystals. The melting point is 133°C to 136°C (after recrystallizing from
absolute ethanol, 136°C)
Therapeutic Function
Tranquilizer
Biological Activity
Studies have reported th at 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.
