| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
| Targets |
Pheneturide exerts its anticonvulsant effects through modulation of the gamma-aminobutyric acid (GABA) neurotransmitter system. It acts as a positive allosteric modulator of GABAA receptors. By enhancing GABAergic inhibitory neurotransmission, it increases the inhibitory tone in the central nervous system, which helps to suppress the neuronal hyperexcitability that leads to seizures.
|
|---|---|
| ln Vitro |
In vitro, Pheneturide has been shown to enhance the effects of GABA at GABAA receptors. It acts as a positive allosteric modulator, increasing the chloride ion influx in response to GABA. This leads to a more hyperpolarized membrane potential and reduced neuronal excitability. Its effects are similar to those of barbiturates.
|
| ln Vivo |
In vivo, Pheneturide is an effective anticonvulsant, used to treat psychomotor epilepsy. It is a decarboxylated product of Phenobarbital and shares a similar mechanism of action. It is an orally active compound that has been used in the past for the management of seizure disorders. Its use has largely been superseded by newer antiepileptic drugs.
|
| Enzyme Assay |
In vitro receptor binding assays for Pheneturide are not standard, as its mechanism of action is allosteric modulation. Instead, its activity is assessed in a functional assay measuring chloride ion flux. GABAA receptors are expressed in cells, and the compound's ability to enhance GABA-induced chloride influx is measured using a chloride-sensitive fluorescent dye or by patch-clamp electrophysiology.
|
| Cell Assay |
In vitro cell-based assays for Pheneturide are often performed using primary neuronal cultures or cell lines expressing GABAA receptors. Cells are treated with the compound, and the GABA-evoked currents are measured using patch-clamp or calcium imaging to assess its modulatory effect.
|
| Animal Protocol |
In vivo animal studies for Pheneturide would typically involve using rodent models of epilepsy, such as the pentylenetetrazol (PTZ) or maximal electroshock seizure (MES) tests. The compound is administered orally or intraperitoneally, and the latency to seizure onset or the percentage of animals protected from seizures is measured.
|
| ADME/Pharmacokinetics |
Specific pharmacokinetic properties of Pheneturide, such as half-life and bioavailability, are not detailed in the available literature. As an older antiepileptic drug, its pharmacokinetics are expected to be similar to other barbiturate-like compounds. It is likely to be absorbed from the gastrointestinal tract and metabolized in the liver.
|
| Toxicity/Toxicokinetics |
Pheneturide, as an anticonvulsant, can cause side effects similar to other barbiturates, including sedation, dizziness, and ataxia. Chronic use can lead to tolerance and dependence. It is contraindicated in patients with a history of drug allergy, severe liver disease, or porphyria. It is intended for research purposes.
|
| Additional Infomation |
Pheneturide is an amine compound.
Pheneturide is a synthetic ureide with anticonvulsant activity. It acts by modulating GABAA receptors, enhancing inhibitory neurotransmission. It is a decarboxylated product of Phenobarbital. This product is for research use only. |
| Molecular Formula |
C11H14N2O2
|
|---|---|
| Molecular Weight |
206.245
|
| Exact Mass |
206.106
|
| CAS # |
90-49-3
|
| PubChem CID |
72060
|
| Appearance |
White to off-white solid powder
|
| Density |
1.15g/cm3
|
| Melting Point |
149.5 °C
|
| Index of Refraction |
1.547
|
| LogP |
2.466
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
15
|
| Complexity |
235
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(NC(C(CC)C1C=CC=CC=1)=O)N
|
| InChi Key |
AJOQSQHYDOFIOX-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C11H14N2O2/c1-2-9(10(14)13-11(12)15)8-6-4-3-5-7-8/h3-7,9H,2H2,1H3,(H3,12,13,14,15)
|
| Chemical Name |
N-carbamoyl-2-phenylbutanamide
|
| Synonyms |
Pheneturide S 46 S-46 M 551 M-551 S46
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~1212.18 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.09 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 20.8 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: ≥ 2.08 mg/mL (10.09 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 20.8 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: ≥ 2.08 mg/mL (10.09 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 | 4.8485 mL | 24.2424 mL | 48.4848 mL | |
| 5 mM | 0.9697 mL | 4.8485 mL | 9.6970 mL | |
| 10 mM | 0.4848 mL | 2.4242 mL | 4.8485 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
