| 药品名称 | Ketazolam |
|---|---|
| 分子靶点 | Translocator protein;Gamma-aminobutyric acid receptor subunit alpha-1;Gamma-aminobutyric acid receptor subunit beta-1;Gamma-aminobutyric acid receptor subunit gamma-1;Gamma-aminobutyric acid receptor subunit delta;Gamma-aminobutyric acid receptor subunit |
| 酶 | Cytochrome P450 3A4 |
| 药物类型 | Small Molecule |
| 研发阶段 | Approved |
| 药物描述 | Ketazolam is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Ketazolam is not approved for sale in the United States or Canada. |
| 结构式 |
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| 药物别名 | Ketazolam;Ketazolamum |
| 治疗类别 | Anti-Anxiety Agents;Benzazepines;Benzodiazepines and benzodiazepine derivatives;Central Nervous System Agents;Central Nervous System Depressants;Cytochrome P-450 CYP3A Inhibitors;Cytochrome P-450 CYP3A Substrates;Cytochrome P-450 CYP3A4 Inhibitors;Cytochrome P-450 CYP3A4 Substrates;Cytochrome P-450 Enzyme Inhibitors;Nervous System;P-glycoprotein/ABCB1 Substrates;Psycholeptics;Psychotropic Drugs;Tranquilizing Agents |
| UNII号 | 92A214MD7Y |
| CAS号 | 27223-35-4 |
| 分子量 | 368.814 |
| 分子式 | C20H17ClN2O3 |
| 适应症 | Ketazolam could be used for the treatment of anxiety. In approved countries, it is indicated for the treatment of anxiety, tension, irritability and similar stress related symptoms. |
| 药效学 | Benzodiazepines enhance the effect of the neurotransmitter gamma-aminobutyric acid (GABA), which results in sedative, hypnotic, anxiolytic, anticonvulsant, muscle relaxant and amnesic action.Benzodiazepines bind nonspecifically to benzodiazepine receptors which mediate sleep, affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell. |
| 作用机制 | Benzodiazepines share a similar chemical structure and their effects in humans are mainly produced by the allosteric modification of a specific kind of neurotransmitter receptor, the GABAA receptor, which increases the conductance of this inhibitory channel; this results in the various therapeutic effects as well as adverse effects of benzodiazepines. Binding of benzodiazepines to this receptor complex promotes binding of GABA, which in turn increases the conduction of chloride ions across the neuronal cell membrane. This increased conductance raises the membrane potential of the neuron resulting in inhibition of neuronal firing. In addition, different GABAA receptor subtypes have varying distributions within different regions of the brain and therefore control distinct neuronal circuits. Hence, activation of different GABAA receptor subtypes by benzodiazepines may result in distinct pharmacological actions. |
| 代谢 | Ketazolam is metabolized to diazepam, followed by demoxepam, and finally desmethyldiazepam. |
| 排泄 | Diazepam and its metabolites are excreted mainly in the urine, predominantly as their glucuronide conjugates. |
| 半衰期 | 26-200 hours |
| 毒理 | Symptoms of overdose include somnolence, confusion, coma, and diminished reflexes. Respiration, pulse and blood pressure should be monitored. |
| ATC代码 | N05BA10 |
Ketazolam靶点信息
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