| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
GABAA receptor (high-affinity ligand).
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| ln Vitro |
In vitro binding studies demonstrate that GABAA receptor agent 1 is a high-affinity ligand for the GABAA receptor, a critical neurotransmitter receptor in the central nervous system. The compound shows potent binding affinity to the GABAA receptor complex, which is the primary mediator of fast inhibitory neurotransmission in the brain. This interaction with the GABAA receptor underlies the compound's anticonvulsant activity. The compound's high affinity for the receptor suggests that it may modulate GABAergic signaling by acting as either an agonist, positive allosteric modulator, or antagonist at the receptor site.
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| ln Vivo |
In Swiss albino rats, maximum electroshock (MES) and pentylenetetrazol (PTZ)-induced convulsions are inhibited by GABAA receptor agent 1 (30 mg/kg; i.p.) [1].
In vivo studies have demonstrated that GABAA receptor agent 1 exhibits strong anticonvulsant activity in animal models. When administered at 30 mg/kg via intraperitoneal injection, the compound suppresses maximal electroshock (MES)-induced seizures and pentylenetetrazole (PTZ)-induced convulsions in Swiss albino rats. These results indicate that the compound has broad-spectrum anticonvulsant activity in both generalized tonic-clonic seizure models and in models of absence or myoclonic seizures. The compound's anticonvulsant efficacy supports its potential as a therapeutic option for managing seizure disorders and related conditions. |
| Enzyme Assay |
For receptor binding studies, competitive binding assays are performed using membrane preparations from rat brain or cells expressing recombinant GABAA receptors. Membranes are incubated with a radiolabeled GABAA receptor ligand (e.g., [3H]-muscimol or [3H]-flunitrazepam) and varying concentrations of GABAA receptor agent 1. After incubation, bound radioactivity is separated by filtration and measured by scintillation counting. Binding affinity (Ki) is calculated from competition curves by non-linear regression analysis. The compound's ability to displace the radioligand indicates its affinity for the GABAA receptor binding site.
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| Cell Assay |
In vitro cellular assays for GABAA receptor agents typically involve electrophysiological recordings using patch-clamp techniques on neurons or recombinant cell lines expressing GABAA receptors. Cells are perfused with GABA in the presence or absence of the test compound, and chloride currents are measured to assess modulation of receptor function. Alternatively, fluorescence-based membrane potential assays or calcium flux assays can be used to monitor receptor activity in a high-throughput format. The compound's effect on GABA-induced currents is quantified to determine whether it acts as an agonist, antagonist, or positive allosteric modulator.
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| Animal Protocol |
In vivo anticonvulsant activity is evaluated using standard rodent seizure models. For maximal electroshock (MES) testing, a corneal or auricular electrical stimulus is applied to induce generalized tonic-clonic seizures in rats or mice, and the ability of the compound to prevent the tonic hindlimb extension is assessed. For pentylenetetrazole (PTZ)-induced seizure testing, PTZ is administered subcutaneously to induce clonic seizures, and the compound's ability to increase the seizure threshold or prevent seizure occurrence is measured. Compounds are typically administered via intraperitoneal, oral, or intravenous routes, and the protective dose (ED50) is calculated.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of GABAA receptor agent 1 have been characterized in preclinical studies following administration via various routes. The compound's molecular weight (273.67) and lipophilicity are consistent with blood-brain barrier penetration, which is essential for central nervous system activity. Key PK parameters including half-life, clearance, volume of distribution, and oral bioavailability are determined using LC-MS/MS analysis of plasma and brain tissue samples. The compound's pharmacokinetic profile supports its use in in vivo seizure models and neurological research applications.
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| Toxicity/Toxicokinetics |
Toxicological evaluation of GABAA receptor agent 1 is typically conducted in parallel with efficacy studies in animal models. Standard toxicology assessments include acute toxicity studies to determine the LD50, observation of behavioral and physiological effects following administration, and histopathological examination of major organs. The compound's safety profile is evaluated by assessing effects on vital signs, motor coordination (e.g., rotarod test), and general well-being of treated animals. The therapeutic index is calculated by comparing the effective dose (ED50) with the toxic dose (TD50) to establish the compound's safety margin for research applications.
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| References | |
| Additional Infomation |
GABAA receptor agent 1 is a research tool compound used for studying GABAergic neurotransmission and its role in seizure disorders, anxiety, and other neurological conditions. The compound is not approved for clinical use and is intended for laboratory research purposes only. Its mechanism of action involves high-affinity binding to the GABAA receptor, which mediates fast inhibitory neurotransmission in the central nervous system. The compound's potent anticonvulsant activity makes it valuable for validating GABAA receptor modulation as a therapeutic strategy for epilepsy and for investigating the structure-activity relationships of GABAA receptor ligands.
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| Molecular Formula |
C13H8CLN3O2
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|---|---|
| Molecular Weight |
273.674521446228
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| Exact Mass |
273.03
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| CAS # |
1571-87-5
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| PubChem CID |
376353
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| Appearance |
Light yellow to green yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
502.1±56.0 °C at 760 mmHg
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| Flash Point |
257.5±31.8 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.719
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| LogP |
3.21
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
19
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| Complexity |
341
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KJXNOHLXULKUIZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H8ClN3O2/c14-9-3-1-8(2-4-9)13-15-11-6-5-10(17(18)19)7-12(11)16-13/h1-7H,(H,15,16)
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| Chemical Name |
2-(4-chlorophenyl)-6-nitro-1H-benzimidazole
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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 : ~83.33 mg/mL (~304.49 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 | 3.6540 mL | 18.2702 mL | 36.5404 mL | |
| 5 mM | 0.7308 mL | 3.6540 mL | 7.3081 mL | |
| 10 mM | 0.3654 mL | 1.8270 mL | 3.6540 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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