Product Data Sheet Inhibitors

Gidazepam • Agonists

Cat. No.: HY-U00315

CAS No.: 129186-29-4

Molecular Formula: C₁₇H₁₅BrN₄O₂ • Screening Libraries Molecular Weight: 387.23

Target: GABA Receptor

Pathway: Membrane Transporter/Ion Channel; Neuronal Signaling

Storage: Please store the product under the recommended conditions in the COA.

BIOLOGICAL ACTIVITY

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

IC₅₀ & Target GABA receptor[1]

In Vitro 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 [1] benzodiazepine receptors, diazepam. For Gidazepam, the Ki value is 2,200±50 nM .

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].

PROTOCOL

Animal Mice[1] Administration [1] The outbreed male white mice (18-22 g) are used. Mice are distributed into 10 groups of five animals each, treated orally with Gidazepam 1 mg/kg (GDZ); GABA ester of menthol 175 mg/kg (1); GABA ester of thymol 20 mg/kg (2); GABA ester of carvacrol 200 mg/kg (3); GABA ester of guaiacol 200 mg/kg (4); mixture of Gidazepam and 1; mixture of Gidazepam and 2; mixture of Gidazepam and 3; mixture of Gidazepam and 4. Doses of esters 1-4 are calculated in equimolar amounts with respect to monoterpenes based on our preliminary investigation and from literature citations. The anticonvulsant activity of compounds 1-4 and Gidazepam as well as mixtures of Gidazepam with 1-4 is evaluated in model of acute generalized seizures; pharmacological effect of compounds is estimated in 3 h[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

REFERENCES

1 www.MedChemExpress.com [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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Caution: Product has not been fully validated for medical applications. For research use only. Tel: 609-228-6898 Fax: 609-228-5909 E-mail: [email protected] Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA

2 www.MedChemExpress.com