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Gidazepam(Gidasepam)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Gidazepam(Gidasepam)图片
CAS NO:129186-29-4
规格:98%
分子量:387.23
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
20mg电议

产品介绍
Gidazepam是一种GABA受体通道(GABARCs)激动剂。
CAS:129186-29-4
分子式:C17H15BrN4O2
分子量:387.23
纯度:98%
存储:Store at -20°C

Background:

Gidazepam is an agonist of GABA receptor channels (GABA RCs).


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].


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].


[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.