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药品详细

Progabide(Progabide)

化学结构式图
中文名
Progabide
英文名
Progabide
分子式
C17H16ClFN2O2
化学名
4-{[(4-chlorophenyl)[(1E)-3-fluoro-6-oxocyclohexa-2,4-dien-1-ylidene]methyl]amino}butanamide
分子量
Average: 334.773
Monoisotopic: 334.088433678
CAS号
62666-20-0
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

Progabide is an analog and prodrug of gamma-aminobutyric acid. It is commonly used in the treatment of epilepsy. It has agonistic activity for both the GABAA and GABAB receptors. Progabide has been investigated for many diseases besides epilepsy, including Parkinson’s disease, schizophrenia, clinical depression and anxiety disorder with varying success.

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    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Bartholini G, Scatton B, Zivkovic B, Lloyd KG: GABA receptor agonists and extrapyramidal motor function: therapeutic implications for Parkinson’s disease. Adv Neurol. 1987;45:79-83. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Phenylpropenes
    • Cinnamaldehydes
    Substructures
    • Alkanes and Alkenes
    • Amino Ketones
    • Phenylpropenes
    • Benzene and Derivatives
    • Aryl Halides
    • Halobenzenes
    • Carbamates and Derivatives
    • Enamines
    • Isoprenes
    • Aromatic compounds
    • Cinnamaldehydes
    • Carboxamides and Derivatives
    • Carboxylic Acids and Derivatives
    • Styrene Derivatives
    • Ketones
    适应症
    药理
    Indication Indicated for the treatment of epilepsy.
    Pharmacodynamics Progabide, a fatty acid derivative, is a GABA receptor agonist used to treat the symptoms of epilepsy.
    Mechanism of action Progabide binds to both GABAA and GABAB receptors located on the terminals of primary afferent fibers. Binding to GABAA results in an increased affinity of the GABA receptor for the amino acid, an augmented flux of chloride ions across the terminal membrane, and an increase in the amount of presynaptic inhibition. Activation of the GABAB receptors retards the influx of calcium ions into the terminals, thereby reducing the evoked release of excitatory amino acids and possibly other transmitters.
    Absorption Well absorbed with a bioavailability of 60%
    Volume of distribution Not Available
    Protein binding 95%
    Metabolism
    Hepatic
    Route of elimination Not Available
    Half life 4 hours
    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 133-135 °C PhysProp
    water solubility 70.9 mg/L Not Available
    logP 3.06 FARRAJ,NF ET AL. (1988)
    Predicted Properties
    Property Value Source
    water solubility 4.42e-03 g/l ALOGPS
    logP 2.68 ALOGPS
    logP 1.8 ChemAxon
    logS -4.9 ALOGPS
    pKa (strongest acidic) 15.32 ChemAxon
    pKa (strongest basic) 4.01 ChemAxon
    physiological charge 0 ChemAxon
    hydrogen acceptor count 3 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 72.19 ChemAxon
    rotatable bond count 6 ChemAxon
    refractivity 91.22 ChemAxon
    polarizability 33.21 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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