Methsuximide (Synonyms: (±)-Mesuximide,PM 396) |
Katalog-Nr.GC17442
One-Click Copy Product Info
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Methsuximid ist ein Antikonvulsivum.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 77-41-8
Sample solution is provided at 25 µL, 10mM.
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Methsuximide (or methsuximide, methosuximide, Celontin) is a succinimide anticonvulsant medication that is pharmacologically converted to its active metabolite N-desmethylmethosuximide, a channel blocker that targets low threshold calcium currents.
Methsuximide effectively suppressed the initial clonic seizures induced by Metrazol in rats and mice. Methsuximide was capable of protecting mice from tonic extensor seizures to supramaximal electroshock [2]. In children with intractable epilepsies, administration of MSM greatly reduced the seizure frequency with no serious or irreversible adverse effects [3].
Methsuximide can function as a substrate of cytochrome P450 (CYP) isoform 2C19 which in turn, inhibits CYP2C19-mediated metabolism of biguanides [4]. Cytochrome P450 2C19 (abbreviated CYP2C19) is an enzyme involved in the metabolism of xenobiotics. Polymorphism of CYP2C19is has been associated with variable ability to metabolize mephenytoin [5].
References:
[1] Nicholls, P. J., and Orton, T.C. The physiological disposition of 14C-methsuximide in the rat. Br.J.Pharmacol. 45(1), 48-59 (1972).
[2] Chen G, Weston J K, Bratton A C. Anticonvulsant activity and toxicity of phensuximide, methsuximide and ethosuximide[J]. Epilepsia, 1963, 4(1‐4): 66-76.
[3] Sigler M, Strassburg H M, Boenigk H E. Effective and safe but forgotten: methsuximide in intractable epilepsies in childhood[J]. Seizure, 2001, 10(2): 120-124.
[4] Wright J D, Helsby N A, Ward S A. The role of S‐mephenytoin hydroxylase (CYP2C19) in the metabolism of the antimalarial biguanides[J]. British journal of clinical pharmacology, 1995, 39(4): 441-444.
[5] Guengerich F P. Human cytochrome P450 enzymes[M]//Cytochrome P450. Springer US, 1995: 473-535.
| Cas No. | 77-41-8 | SDF | |
| Überlieferungen | (±)-Mesuximide,PM 396 | ||
| Chemical Name | 1,3-dimethyl-3-phenyl-2,5-pyrrolidinedione | ||
| Canonical SMILES | CN(C(CC1(C)C2=CC=CC=C2)=O)C1=O | ||
| Formula | C12H13NO2 | M.Wt | 203.2 |
| Löslichkeit | ≥ 8.35mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.9213 mL | 24.6063 mL | 49.2126 mL |
| 5 mM | 984.3 μL | 4.9213 mL | 9.8425 mL |
| 10 mM | 492.1 μL | 2.4606 mL | 4.9213 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)