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| Targets |
The primary target of Gidazepam is the GABA receptor channel (GABA RC), specifically the benzodiazepine binding site on the GABAA receptor complex. As a benzodiazepine agonist, Gidazepam binds to this allosteric site and enhances the inhibitory effects of GABA, leading to increased chloride influx and neuronal hyperpolarization. Gidazepam demonstrates considerably lower affinities to GABA RCs than phenazepam, 3-hydrozyphenazepam, and Br-nordiazepam. It is also reported to be a ligand for mitochondrial benzodiazepine receptors (MBRs).
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| ln Vitro |
The affinity of gidazepam for GABA RC is notably lower than that of br-norzepam, phenazepam, and 3-hydroxyfenazepam. The benzodiazepine receptor-specific ligand diazepam exhibits varying values of the binding inhibition constant (Ki). The Ki value for gidazepam is 2,200±50 nM[1].
In vitro, Gidazepam demonstrates agonist activity at GABA receptor channels. However, its affinity for GABA receptors is notably lower than that of phenazepam, 3-hydrozyphenazepam, and Br-nordiazepam. The compound's activity is assessed in receptor binding assays measuring its displacement of radiolabeled benzodiazepine ligands from GABAA receptors. Its functional activity is assessed in electrophysiological assays measuring the enhancement of GABA-induced chloride currents. |
| ln Vivo |
Ten groups of five mice each were used to administer oral treatments of gidazepam (GDZ, 1 mg/kg), ester 1 (175 mg/kg), ester 2 (20 mg/kg), ester 3 and 4 (200 mg/kg), or a combination of gidazepam and esters 1-4. Within three hours of oral treatment, all GABA esters containing monoterpenes demonstrated anticonvulsant effects, as indicated by an increase in the values of tonic extension (DTE) and produced clonic tonic convulsions (DCTC). With comparable DCTC and DTE values of 250% and 215%, respectively, gidazepam (1 mg/kg) was shown to prevent epileptic seizures; when administered in combination with its esters 5-7, gidazepam and their combined administration may boost anticonvulsant activity as compared with each drug alone [1].
In vivo, Gidazepam has been shown to protect against seizures. At a dose of 1 mg/kg, it demonstrates anticonvulsant activity with DCTC and DTE values of 250% and 215%, respectively. When administered in combination with its esters, the anticonvulsant activity is increased compared to each compound alone. These findings support the compound's potential as an anticonvulsant agent. |
| Enzyme Assay |
In vitro receptor binding assays for Gidazepam typically involve measuring its affinity for the benzodiazepine binding site on the GABAA receptor. Membrane preparations from brain tissue or cells expressing GABAA receptors are incubated with a radiolabeled benzodiazepine ligand (e.g., [³H]-flunitrazepam) in the presence of varying concentrations of Gidazepam. The Ki for displacement is calculated from the competition curve.
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| Cell Assay |
Cellular assays for Gidazepam are performed in neurons or cells expressing GABAA receptors. The compound's functional activity is assessed using electrophysiological techniques, such as patch-clamp recordings, to measure its ability to enhance GABA-induced chloride currents. The compound's effects on neuronal excitability are also assessed.
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| Animal Protocol |
In vivo animal studies with Gidazepam have been performed in models of seizures. In these studies, Gidazepam is administered (e.g., 1 mg/kg), and its anticonvulsant activity is assessed by measuring protection against chemically or electrically induced seizures. The compound's effects on locomotor activity and other behavioral parameters may also be assessed.
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| ADME/Pharmacokinetics |
Gidazepam is metabolized in the liver, with metabolites that may also exhibit pharmacological activity. However, detailed pharmacokinetic parameters such as half-life, bioavailability, volume of distribution, and clearance are not extensively reported in the available literature. As a benzodiazepine, it is expected to have good oral bioavailability and central nervous system penetration.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for Gidazepam are not extensively reported. As a benzodiazepine, it may have side effects typical of this class, including sedation, dependence, and withdrawal symptoms. The compound is classified as a research-use-only chemical and is not intended for human consumption. Specific toxicological data, including acute toxicity, genotoxicity, and target organ effects, are not reported in the available literature.
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| References |
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| Additional Infomation |
Gidazepam is a research-grade compound that was developed as an anxiolytic and anticonvulsant agent. It is not approved for clinical use in most countries. Its primary application is as a pharmacological tool for studying GABA receptor pharmacology. The compound's lower affinity for GABA receptors compared to other benzodiazepines makes it a useful tool for studying structure-activity relationships at the benzodiazepine binding site.
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| Molecular Formula |
C17H15N4O2BR
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|---|---|
| Molecular Weight |
387.2306
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| Exact Mass |
386.038
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| CAS # |
129186-29-4
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| Related CAS # |
Gidazepam-d5
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| PubChem CID |
121919
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| Appearance |
White to off-white solid powder
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| Density |
1.58g/cm3
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| Boiling Point |
675.6ºC at 760mmHg
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| Flash Point |
362.4ºC
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| Vapour Pressure |
4.14E-18mmHg at 25°C
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| Index of Refraction |
1.698
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| LogP |
2.664
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
24
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| Complexity |
519
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XLGCMZLSEXRBSG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H15BrN4O2/c18-12-6-7-14-13(8-12)17(11-4-2-1-3-5-11)20-9-16(24)22(14)10-15(23)21-19/h1-8H,9-10,19H2,(H,21,23)
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| Chemical Name |
2-(7-bromo-2-oxo-5-phenyl-3H-1,4-benzodiazepin-1-yl)acetohydrazide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~645.61 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5824 mL | 12.9122 mL | 25.8244 mL | |
| 5 mM | 0.5165 mL | 2.5824 mL | 5.1649 mL | |
| 10 mM | 0.2582 mL | 1.2912 mL | 2.5824 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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