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药品详细

Chlormezanone(氯美扎酮)

化学结构式图
中文名
氯美扎酮
英文名
Chlormezanone
分子式
C11H12ClNO3S
化学名
2-(4-chlorophenyl)-3-methyl-1$l^{6},3-thiazinane-1,1,4-trione
分子量
Average: 273.736
Monoisotopic: 273.022641652
CAS号
80-77-3
ATC分类
M03B 未知
药物类型
small molecule
阶段
approved, withdrawn
商品名
同义名
基本介绍

A non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm. [PubChem]

生产厂家
  • Sanofi aventis us llc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Wollina U, Hipler UC, Seeling A, Oelschlager H: Investigations of interactions of chlormezanone racemate and its enantiomers on human keratinocytes and human leucoytes in vitro. Skin Pharmacol Physiol. 2005 May-Jun;18(3):132-8. Pubmed
  2. Seeling A, Oelschlager H, Rothley D: [Important pharmaceutical-chemical characteristics of the central muscle relaxant chlormezanone] Pharmazie. 2000 Apr;55(4):293-6. Pubmed
  3. Oelschlager H, Klinger W, Rothley D, Seeling A, Bockhard H, Hofmann B, Machts H, Riederer H, Rackur H: [Cleavage and biotransformation of the central muscle relaxant chlormezanone] Pharmazie. 1998 Sep;53(9):620-4. Pubmed
  4. Gautier V, Vincon G, Demotes-Mainard F, Albin H: [Pharmacokinetics of chlormezanone in healthy volunteers] Therapie. 1990 Jul-Aug;45(4):315-9. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Benzene and Derivatives
  • Halobenzenes
  • Lactams
Substructures
  • Amino Ketones
  • Sulfonyls
  • Benzene and Derivatives
  • Aliphatic and Aryl Amines
  • Aryl Halides
  • Halobenzenes
  • Sulfones
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamides and Derivatives
  • Lactams
  • Sulfoxides
适应症
药理
Indication Used in the management of anxiety and in the treatment of muscle spasm.
Pharmacodynamics Chlormezanone is a non-benzodiazepine muscle relaxant. It was discontinued worldwide in 1996 by its manufacturer due to confirmed serious and rare cutaneous reactions (toxic epidermal necrolysis).
Mechanism of action Chlormezanone binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.
Absorption Not Available
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Not Available
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Symptoms of overdose include drowsiness, weakness, nausea, dizziness, abdominal pain, cerebral oedema and renal tubular necrosis, hyperglycaemia and hypoglycaemia, liver damage, encephalopathy, coma and death.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 116.2 °C PhysProp
water solubility 2500 mg/L (at 25 °C) MERCK INDEX (1996)
logP 1.3 Not Available
Predicted Properties
Property Value Source
water solubility 1.61e+00 g/l ALOGPS
logP 0.84 ALOGPS
logP 0.92 ChemAxon
logS -2.2 ALOGPS
pKa (strongest acidic) 19.07 ChemAxon
pKa (strongest basic) -2.5 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 3 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 54.45 ChemAxon
rotatable bond count 1 ChemAxon
refractivity 64.88 ChemAxon
polarizability 25.89 ChemAxon
药物相互作用
食物相互作用
Not Available

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