产品描述
Gidazepam is an GABA receptor channels agonist.
体外活性
Gidazepam shows considerably lower affinities to GABA RCs than phenazepam, 3-hydrozyphenazepam, and Br-nordiazepam. For Gidazepam, the Ki value is 2,200±50 nM. This is showed in different values of the Ki of binding of a specific ligand of benzodiazepine receptors, diazepam [1].
体内活性
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. Mice are distributed into 10 groups of five animals each, treated with Gidazepam (GDZ, 1 mg/kg; p.o.); ester 1 (175 mg/kg); ester 2 (20 mg/kg); esters 3 and 4 (200 mg/kg); mixtures of Gidazepam and esters 1-4. After oral administration in 3 h, all esters of GABA with monoterpenes show antiseizure effects as evidenced by increasing of inducing clonic-tonic convulsions (DCTC) and tonic extension (DTE) values [1].
Cas No.
129186-29-4
分子式
C17H15BrN4O2
分子量
387.23
别名
Gidasepam;Hydazepam;Hidazepam
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years