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Methsuximide
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Methsuximide图片
CAS NO:77-41-8
包装与价格：
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
Methsuximide 是一种抗惊厥药。
Cas No.77-41-8
别名甲琥胺,(±)-Mesuximide,PM 396
化学名1,3-dimethyl-3-phenyl-2,5-pyrrolidinedione
Canonical SMILESCN(C(CC1(C)C2=CC=CC=C2)=O)C1=O
分子式C12H13NO2
分子量203.2
溶解度≥ 8.35mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.