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药品详细

Sulpiride(舒必利)

化学结构式图
中文名
舒必利
英文名
Sulpiride
分子式
C15H23N3O4S
化学名
N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-sulfamoylbenzamide
分子量
Average: 341.426
Monoisotopic: 341.140926929
CAS号
15676-16-1
ATC分类
N05A 未知;N05A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed)

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    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference Not Available
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Benzenesulfonamides
    • Benzamides
    Substructures
    • Phenols and Derivatives
    • Amino Ketones
    • Sulfonyls
    • Pyrrolidines
    • Ethers
    • Benzene and Derivatives
    • Carboxylic Acids and Derivatives
    • Benzenesulfonamides
    • Aliphatic and Aryl Amines
    • Heterocyclic compounds
    • Aromatic compounds
    • Anisoles
    • Carboxamides and Derivatives
    • Sulfonamides
    • Benzoyl Derivatives
    • Phenyl Esters
    • Benzamides
    适应症
    药理
    Indication Sulpiride is indicated for the treatment of schizophrenia.
    Pharmacodynamics Sulpiride is a substituted benzamide derivative and a selective dopamine D2 antagonist with antipsychotic and antidepressant activity. Other benzamide derivatives include metoclopramide, tiapride, and sultopride.
    Mechanism of action In contrast to most other neuroleptics which block both dopamine D1 and D2 receptors, Sulpiride is more selective and acts primarily as a dopamine D2 antagonist. Sulpiride appears to lack effects on norepinephrine, acetylcholine, serotonin, histamine, or gamma-aminobutyric acid (GABA) receptors.
    Absorption Sulpiride is absorbed slowly from the gastrointestinal tract. Its oral bioavailability is only 25 to 35% with marked interindividual differences.
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life 6 to 8 hours
    Clearance Not Available
    Toxicity Sulpiride has a relatively low order of acute toxicity. Substantial amounts may cause severe but reversible dystonic crises with torticollis, protrusion of the tongue, and/or trism. In some cases all the classical symptoms typical of severe Parkinson's Disease may be noted; in others, over-sedation/coma may occur.
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 178 dec °C PhysProp
    water solubility 2280 mg/L Not Available
    logP 0.57 HOEGBERG,T ET AL. 1986
    Caco2 permeability -6.16 ADME Research, USCD
    pKa 9.12 EL TAYAR,N ET AL. (1985)
    Predicted Properties
    Property Value Source
    water solubility 5.37e-01 g/l ALOGPS
    logP 1.2 ALOGPS
    logP 0.22 ChemAxon
    logS -2.8 ALOGPS
    pKa (strongest acidic) 10.24 ChemAxon
    pKa (strongest basic) 8.39 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 5 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 101.73 ChemAxon
    rotatable bond count 6 ChemAxon
    refractivity 88.63 ChemAxon
    polarizability 36.18 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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