Gidazepam

Gidazepam is an agonist of GABA receptor channels (GABA RCs). IC50 & Target: GABA receptor^[1] In Vitro: Gidazepam demonstrates considerably lower affinities to GABA RCs than phenazepam, 3-hydrozyphenazepam, and Br-nordiazepam. This is manifested in different values of the inhibition constant (K_i) of binding of a specific ligand of benzodiazepine receptors, diazepam. For Gidazepam, the K_i value is 2,200±50 nM^[1]. In Vivo: Mice are distributed into 10 groups of five animals each, treated orally with Gidazepam (GDZ, 1 mg/kg); ester 1 (175 mg/kg); ester 2 (20 mg/kg); esters 3 and 4 (200 mg/kg); mixtures of Gidazepam and esters 1-4. All esters of GABA with monoterpenes display antiseizure effects in 3 h after oral administration as evidenced by increasing of inducing clonic-tonic convulsions (DCTC) and tonic extension (DTE) values. Gidazepam (1 mg/kg) is found to protect against seizures with DCTC and DTE values of 250% and 215%, accordingly; whereas co-administration of Gidazepam and esters 5-7 is shown to increase anticonvulsant activity compared with each compound alone^[1].