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药品详细

Alizapride(阿立必利)

化学结构式图
中文名
阿立必利
英文名
Alizapride
分子式
C16H21N5O2
化学名
6-methoxy-N-{[1-(prop-2-en-1-yl)pyrrolidin-2-yl]methyl}-2H-1,2,3-benzotriazole-5-carboxamide
分子量
Average: 315.3702
Monoisotopic: 315.169524941
CAS号
59338-93-1
ATC分类
A03F 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Alizapride is a dopamine antagonist with prokinetic and antiemetic effects used in the treatment of nausea and vomiting, including postoperative nausea and vomiting.

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    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Bleiberg H, Gerard B, Dalesio O, Crespeigne N, Rozencweig M: Activity of a new antiemetic agent: alizapride. A randomized double-blind crossover controlled trial. Cancer Chemother Pharmacol. 1988;22(4):316-20. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Phenols and Derivatives
    • Ethers
    • Anisoles
    • Benzoyl Derivatives
    • Benzamides
    Substructures
    • Alkanes and Alkenes
    • Phenols and Derivatives
    • Amino Ketones
    • Triazoles
    • Pyrrolidines
    • Ethers
    • Benzene and Derivatives
    • Carboxylic Acids and Derivatives
    • Aliphatic and Aryl Amines
    • Heterocyclic compounds
    • Aromatic compounds
    • Anisoles
    • Carboxamides and Derivatives
    • Benzoyl Derivatives
    • Phenyl Esters
    • Benzamides
    适应症
    药理
    Indication Alizapride is used in the treatment of nausea and vomiting, including postoperative nausea and vomiting.
    Pharmacodynamics Alizapride is a dopamine antagonist.
    Mechanism of action The anti-emetic action of Alizapride is due to its antagonist activity at D2 receptors in the chemoreceptor trigger zone (CTZ) in the central nervous system (CNS)—this action prevents nausea and vomiting triggered by most stimuli. Structurally similar to metoclopramide and, therefore, shares similar other atributres related to emesis and prokinetics.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Not Available
    Route of elimination renal
    Half life 3 hours
    Clearance Not Available
    Toxicity Not Available
    Affected organisms Not Available
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 139 °C PhysProp
    logP 1.79 MANNHOLD,R ET AL. (1990)
    Predicted Properties
    Property Value Source
    water solubility 4.95e-01 g/l ALOGPS
    logP 1.81 ALOGPS
    logP 1.12 ChemAxon
    logS -2.8 ALOGPS
    pKa (strongest acidic) 8.86 ChemAxon
    pKa (strongest basic) 7.77 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 5 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 83.14 ChemAxon
    rotatable bond count 6 ChemAxon
    refractivity 89.21 ChemAxon
    polarizability 33.92 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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