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药品详细

Phensuximide(苯琥胺)

化学结构式图
中文名
苯琥胺
英文名
Phensuximide
分子式
C11H11NO2
化学名
1-methyl-3-phenylpyrrolidine-2,5-dione
分子量
Average: 189.2105
Monoisotopic: 189.078978601
CAS号
86-34-0
ATC分类
N03A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Phensuximide is an anticonvulsant in the succinimide class. It suppresses the paroxysmal three cycle per second spike and wave EEG pattern associated with lapses of consciousness in petit mal seizures. The frequency of attacks is reduced by depression of nerve transmission in the motor cortex.

生产厂家
  • Parke davis div warner lambert co
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Rankin GO, Cressey-Veneziano K, Wang RT, Brown PI: Urinary tract effects of phensuximide in the Sprague-Dawley and Fischer 344 rat. J Appl Toxicol. 1986 Oct;6(5):349-56. Pubmed
  2. CHEN G, WESTON JK, BRATTON AC Jr: Anticonvulsant activity and toxicity of phensuximide, methsuximide and ethosuximide. Epilepsia. 1963 Mar;4:66-76. Pubmed
  3. Ferrendelli JA, Kinscherf DA: Inhibitory effects of anticonvulsant drugs on cyclic nucleotide accumulation in brain. Ann Neurol. 1979 Jun;5(6):533-8. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Phenethylamines
  • Phenylpropylamines
  • Gamma Lactams
Substructures
  • Amino Ketones
  • Pyrrolidines
  • Benzene and Derivatives
  • Phenethylamines
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamides and Derivatives
  • Phenylpropylamines
  • Carboxylic Acids and Derivatives
  • Gamma Lactams
适应症
药理
Indication For the treatment of epilepsy.
Pharmacodynamics Phensuximide suppresses the paroxysmal three cycle per second spike and wave EEG pattern associated with lapses of consciousness in absence (petit mal) seizures. The frequency of attacks is reduced by depression of nerve transmission in the motor cortex.
Mechanism of action Phensuximide's mechanism of action not understood, but may act in inhibitory neuronal systems that are important in the generation of the three per second rhythm. It's effects may be related to its ability to inhibit depolarization-induced accumulation of cyclic AMP and cyclic GMP in brain tissue.
Absorption Rapid and complete.
Volume of distribution Not Available
Protein binding 21%
Metabolism
Hepatic.
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 72 °C PhysProp
water solubility 7020 mg/L Not Available
logP 0.7 Not Available
Predicted Properties
Property Value Source
water solubility 2.21e+00 g/l ALOGPS
logP 0.61 ALOGPS
logP 0.91 ChemAxon
logS -1.9 ALOGPS
pKa (strongest acidic) 19.4 ChemAxon
pKa (strongest basic) -7.4 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 37.38 ChemAxon
rotatable bond count 1 ChemAxon
refractivity 51.85 ChemAxon
polarizability 19.66 ChemAxon
药物相互作用
食物相互作用
Not Available

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