| Bioactivity | Gidazepam is an agonist of GABA receptor channels (GABA RCs). |
| Target | GABA receptor |
| Invitro | 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 (Ki) of binding of a specific ligand of benzodiazepine receptors, diazepam. For Gidazepam, the Ki 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]. |
| Name | Gidazepam |
| CAS | 129186-29-4 |
| Formula | C17H15BrN4O2 |
| Molar Mass | 387.23 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. N. Ya Golovenko, et al. Pharmacodynamical and Neuroreceptor Analysis of the Permeability of the Blood-Brain Barrier for Derivatives of 1,4-Benzodiazepine. Neurophysiology, Vol. 46, No. 3, June, 2014. [2]. Nesterkina M, et al. Synthesis and Pharmacological Properties of Novel Esters Based on Monocyclic Terpenes and GABA. Pharmaceuticals (Basel). 2016 Jun 13;9(2). pii: E32. |