Datasheet Inhibitors / Agonists / Screening Libraries A DRUG SCREENING EXPERT

Product Name : Gidazepam Catalog Number : T15380 CAS Number : 129186-29-4 Molecular Formula : C17H15BrN4O2 Molecular Weight : 387.23

Description: Gidazepam is an GABA receptor channels agonist.

Storage: 2 years -80°C in solvent; 3 years -20°C powder;

Receptor (IC50) GABA receptor

In vitro Activity 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]. In vivo Activity 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].

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.

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