| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Mephenesin targets the NMDA receptor, acting as an antagonist. It is a centrally acting muscle relaxant, meaning it acts on the central nervous system to reduce muscle tone. Its mechanism involves modulation of neuronal signaling through NMDA receptor inhibition.
|
|---|---|
| ln Vitro |
In vitro, mephenesin has been characterized as an NMDA receptor antagonist. Its muscle relaxant and anticonvulsant effects have been demonstrated in various experimental models. It is a centrally acting agent that modulates neuronal excitability.
|
| ln Vivo |
In vivo, mephenesin is used as a centrally acting muscle relaxant with antianxiety, muscle-paralyzing, and anticonvulsant effects. It is used for the treatment of spasticity or painful muscle spasm. Its effects are mediated through its action on the central nervous system.
|
| Enzyme Assay |
The activity of mephenesin at the NMDA receptor can be assessed using radioligand binding assays. Membranes prepared from brain tissue are incubated with a radiolabeled NMDA receptor ligand and varying concentrations of mephenesin. The displacement of the radioligand is measured to determine the affinity of mephenesin for the receptor.
|
| Cell Assay |
The cellular effects of mephenesin can be evaluated using neuronal cell cultures. Cells are treated with mephenesin, and the effects on neuronal activity and neurotransmitter release are measured. The compound's ability to inhibit NMDA receptor-mediated calcium influx can be assessed using calcium imaging.
|
| Animal Protocol |
In vivo studies with mephenesin involve administration to animals via oral or parenteral routes. In models of muscle spasticity or seizures, the compound's efficacy in reducing muscle tone or preventing convulsions is assessed. The compound's pharmacokinetic profile and tolerability are also evaluated.
|
| ADME/Pharmacokinetics |
Mephenesin has a molecular formula of C10H14O3 and a molecular weight of 182.22. It is a centrally acting muscle relaxant. It is soluble in organic solvents and has moderate lipophilicity.
|
| Toxicity/Toxicokinetics |
Specific toxicology data for mephenesin are not detailed in the available literature. As a centrally acting muscle relaxant, it can cause central nervous system depression at high doses. Its use is associated with potential for abuse and dependence. Standard safety precautions should be taken when handling this compound.
|
| References | |
| Additional Infomation |
1-(2-Methylphenyl)glycerol is a glycerol ether in which a single 2-methylphenyl group is linked to the 1-position of glycerol via an ether bond. It is an aromatic ether and glycerol ether, functioning similarly to o-cresol. Mefenoxam is a synthetic cresol glycerol ether that produces transient muscle relaxation and paralysis by inhibiting the central nervous system. It was first used in the 1950s. It is a short-acting, centrally acting muscle relaxant. Drug Indications Mefenoxam has been used to treat muscle spasms caused by diseases such as Parkinson's disease or multiple sclerosis. Mechanism of Action The exact mechanism of action of mefenoxam is not yet clear. It has been observed to block inward sodium and calcium currents in neurons. It has physiological effects opposite to strychnine. Pharmacodynamics Mefenoxam reduces neuronal excitability, leading to a decrease in muscle fiber action potentials, ultimately resulting in spasm relief.
Mephenesin is an NMDA receptor antagonist and a centrally acting muscle relaxant used for the treatment of spasticity and painful muscle spasms. It has antianxiety and anticonvulsant effects. It is not a first-line drug in modern clinical practice but is used in research as a reference compound for muscle relaxants and NMDA receptor antagonists. |
| Molecular Formula |
C10H14O3
|
|---|---|
| Molecular Weight |
182.2164
|
| Exact Mass |
182.094
|
| CAS # |
59-47-2
|
| PubChem CID |
4059
|
| Appearance |
White to off-white solid powder
|
| Density |
1.152g/cm3
|
| Boiling Point |
153ºC(4 torr)
|
| Melting Point |
69ºC
|
| Flash Point |
161.5ºC
|
| Index of Refraction |
1.545
|
| LogP |
0.727
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
13
|
| Complexity |
138
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
JWDYCNIAQWPBHD-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C10H14O3/c1-8-4-2-3-5-10(8)13-7-9(12)6-11/h2-5,9,11-12H,6-7H2,1H3
|
| Chemical Name |
3-(2-methylphenoxy)propane-1,2-diol
|
| 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 : ≥ 100 mg/mL (~548.79 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (13.72 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 (13.72 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 (13.72 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 | 5.4879 mL | 27.4394 mL | 54.8787 mL | |
| 5 mM | 1.0976 mL | 5.4879 mL | 10.9757 mL | |
| 10 mM | 0.5488 mL | 2.7439 mL | 5.4879 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
