Inhibitors Product Data Sheet
Gidazepam • Agonists
Cat. No.: HY-U00315 CAS No.: 129186-29-4
Molecular Formula: C₁₇H₁₅BrN₄O₂ •
Molecular Weight: 387.23 Screening Libraries Target: GABA Receptor Pathway: Membrane Transporter/Ion Channel; Neuronal Signaling Storage: Please store the product under the recommended conditions in the Certificate of Analysis.
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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
Page 1 of 2 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
Page 2 of 2 www.MedChemExpress.com