Datasheet Inhibitors / Agonists / Screening Libraries a DRUG SCREENING EXPERT

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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. FOR RESEARCH PURPOSES ONLY. NOT FOR DIAGNOSTIC OR THERAPEUTIC USE. Information for product storage and handling is indicated on the product datasheet. Targetmol products are stable for long term under the recommended storage conditions. Our products may be shipped under different conditions as many of them are stable in the short-term at higher or even room temperatures. We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, please follow the storage recommendations on the product data sheet. [email protected] | Tel: +1-781-999-4286 | www.targetmol.com.

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Guaiana, G., Barbui, C., Caldwell, DM, Davies, SJC, Furukawa, TA
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