| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
| Targets |
Beclamide targets pathways involved in seizure suppression. As an anticonvulsant, it suppresses neuronal excitability and prevents seizure propagation. The compound has sedative effects in addition to anticonvulsant activity. Its mechanism likely involves modulation of neurotransmitter systems or ion channels involved in neuronal excitability. Beclamide was effective for generalized tonic-clonic seizures but was ineffective for absence seizures. The compound is a discontinued drug with anticonvulsant and sedative effects.
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| ln Vitro |
In vitro, Beclamide demonstrates anticonvulsant activity in neuronal preparations. The compound has sedative effects in addition to anticonvulsant activity. Beclamide is an active molecule with anticonvulsant activity used as an anticonvulsant drug. It is moderately soluble in lower alcohols and decomposes in hot aqueous acid and alkaline solutions. The compound's anticonvulsant properties have been characterized in various in vitro neuronal models. Its mechanism of action likely involves modulation of neuronal excitability.
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| ln Vivo |
In vivo, Beclamide was studied in the 1950s for its anticonvulsant properties as a treatment for generalized tonic-clonic seizures. It was used as a sedative and as an anticonvulsant but is no longer used clinically. The compound was effective for generalized tonic-clonic seizures but was ineffective for absence seizures. Beclamide was marketed under various names including Chloracon, Hibicon, Posedrine, Nydrane, and Seclar. Its clinical use has been discontinued.
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| Enzyme Assay |
Beclamide anticonvulsant assays involve measuring seizure suppression in neuronal preparations or animal models. Neuronal excitability is assessed by measuring action potential firing or synaptic transmission. Anticonvulsant activity is evaluated using seizure induction models such as pentylenetetrazole-induced seizures or maximal electroshock seizures. The compound's efficacy against generalized tonic-clonic seizures was established in preclinical and clinical studies. Sedative effects are assessed by measuring locomotor activity or other behavioral endpoints. Assays are performed with appropriate positive controls such as known anticonvulsants (e.g., phenytoin).
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| Cell Assay |
Beclamide cell-based assays are conducted in neuronal cell lines or primary neuronal cultures. Cells are cultured in appropriate media and treated with Beclamide at varying concentrations. Neuronal excitability is assessed by measuring action potential firing using patch-clamp electrophysiology or by measuring calcium influx. Cell viability is assessed by standard assays. Sedative effects may be assessed in relevant cell models. Experiments are performed in triplicate with appropriate positive (e.g., known anticonvulsants) and negative (vehicle) controls.
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| Animal Protocol |
Beclamide in vivo studies are conducted in animal models of seizures. Animals are treated with Beclamide via oral administration or injection. Seizure induction models such as pentylenetetrazole-induced seizures or maximal electroshock seizures are used. Seizure severity, latency, and incidence are monitored. For sedative studies, locomotor activity and other behavioral endpoints are assessed. Beclamide was studied in the 1950s in clinical trials for generalized tonic-clonic seizures. Animals are monitored for clinical signs. Studies are conducted in accordance with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Metabolites are found only in urine. 4-Hydroxybecramite is present in higher concentrations in urine than 3-hydroxybecramite. Approximately 20% of the radiolabeled material is excreted in urine. Metabolism/Metabolites Metabolism is rapid. The main metabolic pathways are the oxidation of the benzene ring to produce 3-hydroxyphenyl and 4-hydroxyphenyl metabolites, and the oxidation of benzene methylene to produce benzoic acid. 3-hydroxyphenyl and 4-hydroxyphenyl metabolites are primarily excreted as glucuronide and sulfate conjugates, while benzoic acid is excreted as a glycine conjugate (hippuric acid). Beclamide (MW 197.66 g/mol, C10H12ClNO) is a small molecule. It is moderately soluble in lower alcohols and decomposes in hot aqueous acid and alkaline solutions. The compound has a melting point of 94°C. Beclamide is also known as N-benzyl-β-chloropropionamide, N-Benzyl-3-chloropropionamide, and beta-chlorpropionamide. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution have been characterized in clinical studies. The compound is no longer used clinically but serves as a research tool. |
| Toxicity/Toxicokinetics |
Beclamide is generally well-tolerated at therapeutic doses. The compound has anticonvulsant and sedative effects with established safety profiles from clinical use in the 1950s. It was used as a treatment for generalized tonic-clonic seizures. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation is available from clinical use data.
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| Additional Infomation |
Beclamide belongs to the benzene class of compounds.
Beclamide (N-benzyl-β-chloropropionamide) is a discontinued drug with anticonvulsant and sedative effects. It was used in the 1950s to treat generalized tonic-clonic seizures, but was ineffective for absence seizures. Drug indications It has been used to treat epilepsy and epilepsy-related behavioral disorders. It has been used to treat generalized tonic-clonic seizures, but was ineffective for absence seizures. In recent years, research has focused on the application of Beclamide in behavioral disorders. In patients with epilepsy and intellectual disability, it has been found to reduce anxiety, antisocial behavior, compulsive behavior and impulsivity. In addition, it has been observed to have a mood-stabilizing effect. [2] Furthermore, due to its effect on monoamine neurotransmitters, Beclamide may have potential applications in the treatment of diseases such as tardive dyskinesia and ADHD. [2] Mechanism of action Beclamide has been used for more than 30 years, but little is known about its mechanism of action in the central nervous system. A rat study found that beclamitar reduced striatal dopamine and serotonin levels and increased levels of dopamine's major metabolite (thus promoting dopamine turnover), while simultaneously lowering serotonin's major metabolite levels below the detection limit. Similar changes in neurotransmitter levels were observed in the rat frontal cortex. It is theoretically suggested that aggressive behavior in animals is related to the levels of biologically derived monoamine neurotransmitters such as dopamine and serotonin, but their exact role remains unclear. Beclamide (N-benzyl-β-chloropropionamide) is a discontinued drug with anticonvulsant and sedative effects. It was studied in the 1950s for treating generalized tonic-clonic seizures but was ineffective for absence seizures. Beclamide was marketed as Chloracon, Hibicon, Posedrine, Nydrane, and Seclar. It is an active molecule with anticonvulsant activity used as an anticonvulsant drug. All applications are limited to non-human research use. |
| Molecular Formula |
C10H12NOCL
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| Molecular Weight |
197.66138
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| Exact Mass |
197.061
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| CAS # |
501-68-8
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| PubChem CID |
10391
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| Appearance |
White to off-white solid powder
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| Density |
1.145g/cm3
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| Boiling Point |
386.9ºC at 760mmHg
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| Flash Point |
187.8ºC
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| Index of Refraction |
1.532
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| LogP |
2.322
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
13
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| Complexity |
155
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NCC1=CC=CC=C1)CCCl
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| InChi Key |
JPYQFYIEOUVJDU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H12ClNO/c11-7-6-10(13)12-8-9-4-2-1-3-5-9/h1-5H,6-8H2,(H,12,13)
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| Chemical Name |
N-benzyl-3-chloropropanamide
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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 : ≥ 100 mg/mL (~505.92 mM)
H2O : ~0.67 mg/mL (~3.39 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.65 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (12.65 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (12.65 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.0592 mL | 25.2960 mL | 50.5919 mL | |
| 5 mM | 1.0118 mL | 5.0592 mL | 10.1184 mL | |
| 10 mM | 0.5059 mL | 2.5296 mL | 5.0592 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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