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药品详细

Adinazolam(阿地唑仑)

化学结构式图
中文名
阿地唑仑
英文名
Adinazolam
分子式
C19H18ClN5
化学名
({12-chloro-9-phenyl-2,4,5,8-tetraazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),3,5,8,11,13-hexaen-3-yl}methyl)dimethylamine
分子量
Average: 351.833
Monoisotopic: 351.125073308
CAS号
37115-32-5
ATC分类
N05B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Adinazolam (Deracyn®) is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative, and antidepressant properties. Adinazolam was developed by Dr. Jackson B. Hester, who was seeking to enhance the antidepressant properties of alprazolam, which he also developed.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. Pubmed
    2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. Pubmed
    3. File SE, Pellow S: Triazolobenzodiazepines antagonize the effects of anxiogenic drugs mediated at three different central nervous system sites. Neurosci Lett. 1985 Oct 24;61(1-2):115-9. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Benzodiazepines
    Substructures
    • Benzodiazepines
    • Triazoles
    • Benzene and Derivatives
    • Aryl Halides
    • Halobenzenes
    • Aliphatic and Aryl Amines
    • Heterocyclic compounds
    • Aromatic compounds
    • Diazepines
    • Imines
    • Cyanamides
    • Anilines
    适应症
    药理
    Indication For the treatment of anxiety and status epilepticus.
    Pharmacodynamics Adinazolam is a benzodiazepine derivative used to treat anxiety, status epilepticus, and for sedation induction and anterograde amnesia. Adinazolam binds with high affinity to the GABA benzodiazepine receptor complex. Considerable evidence suggest that the central pharmacologic/therapeutic actions of alprazolam are mediated via interaction with this receptor complex.
    Mechanism of action Adinazolam binds to peripheral-type 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
    Hepatic. The main metabolite is N-desmethyladinazolam. The other two metabolites are alpha-hydroxyalprazolam and estazolam.

    Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

    Substrate Enzymes Product
    Adinazolam
    		desmethyladinazolam Details
    Adinazolam
      		Estazolam Details
      Adinazolam
        		alpha-hydroxyalprazolam Details
        Route of elimination Not Available
        Half life Less than 3 hours.
        Clearance Not Available
        Toxicity Signs of overdose may include muscle weakness, ataxia, dysarthria and particularly in children paradoxical excitement. In more severe cases diminished reflexes, confusion, and coma may ensue.
        Affected organisms
        • Humans and other mammals
        Pathways Not Available
        理化性质
        Properties
        State solid
        Experimental Properties
        Property Value Source
        logP 4.4 Not Available
        Predicted Properties
        Property Value Source
        water solubility 6.72e-02 g/l ALOGPS
        logP 2.57 ALOGPS
        logP 2.24 ChemAxon
        logS -3.7 ALOGPS
        pKa (strongest acidic) 18.38 ChemAxon
        pKa (strongest basic) 6.66 ChemAxon
        physiological charge 0 ChemAxon
        hydrogen acceptor count 4 ChemAxon
        hydrogen donor count 0 ChemAxon
        polar surface area 46.31 ChemAxon
        rotatable bond count 3 ChemAxon
        refractivity 112.31 ChemAxon
        polarizability 37.15 ChemAxon
        药物相互作用
        食物相互作用
        Not Available

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