129186-29-4
129186-29-4 structure
- Name: Gidazepam
- Chemical Name: 2-(7-bromo-2-oxo-5-phenyl-3H-1,4-benzodiazepin-1-yl)acetohydrazide
- CAS Number: 129186-29-4
- Molecular Formula: C17H15BrN4O2
- Molecular Weight: 387.23100
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel GABA Receptor
- Create Date: 2016-12-27 07:26:28
- Modify Date: 2024-01-11 19:20:17
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Gidazepam is an agonist of GABA receptor channels (GABA RCs).
| Name | 2-(7-bromo-2-oxo-5-phenyl-3H-1,4-benzodiazepin-1-yl)acetohydrazide |
|---|---|
| Synonyms |
(1-Hydrazinocarbonyl)-7-bromo-5-phenyl-1,2-dihydro-3H-1,4-benzodiazepine-2-one
UNII-XMJ87I93Y9 1H-1,4-Benzodiazepine-1-aceticacid,7-bromo-2,3-dihydro-2-oxo-5-phenyl-,hydrazide gidazepam |
| Description | Gidazepam is an agonist of GABA receptor channels (GABA RCs). |
|---|---|
| Related Catalog | |
| 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 benzodiazepine receptors, diazepam. For Gidazepam, the Ki value is 2,200±50 nM[1]. |
| 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]. |
| Animal Admin | Mice[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]. |
| References |
| Density | 1.58g/cm3 |
|---|---|
| Boiling Point | 675.6ºC at 760mmHg |
| Molecular Formula | C17H15BrN4O2 |
| Molecular Weight | 387.23100 |
| Flash Point | 362.4ºC |
| Exact Mass | 386.03800 |
| PSA | 91.28000 |
| LogP | 2.66420 |
| Vapour Pressure | 4.14E-18mmHg at 25°C |
| Index of Refraction | 1.698 |
| Storage condition | 2-8℃ |