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药品详细

Remoxipride(瑞莫必利)

化学结构式图
中文名
瑞莫必利
英文名
Remoxipride
分子式
C16H23BrN2O3
化学名
3-bromo-N-{[(2S)-1-ethylpyrrolidin-2-yl]methyl}-2,6-dimethoxybenzamide
分子量
Average: 371.269
Monoisotopic: 370.089205259
CAS号
80125-14-0
ATC分类
N05A 未知
药物类型
small molecule
阶段
approved, withdrawn
商品名
同义名
基本介绍

An antipsychotic agent that is specific for dopamine D2 receptors. It has been shown to be effective in the treatment of schizophrenia. [PubChem]

生产厂家
    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
    • Phenols and Derivatives
    • Ethers
    • Anisoles
    • Benzoyl Derivatives
    • Benzamides
    Substructures
    • Phenols and Derivatives
    • Amino Ketones
    • Pyrrolidines
    • Ethers
    • Benzene and Derivatives
    • Carboxylic Acids and Derivatives
    • Aliphatic and Aryl Amines
    • Aryl Halides
    • Heterocyclic compounds
    • Aromatic compounds
    • Anisoles
    • Carboxamides and Derivatives
    • Benzoyl Derivatives
    • Phenyl Esters
    • Benzamides
    • Halobenzenes
    适应症
    药理
    Indication Remoxipride is an atypical antipsychotic once used for the treatment of schizophrenia.
    Pharmacodynamics Remoxipride, a substituted benzamide, is a selective D2 receptor antagonist. It has been shown to be effective in the treatment of schizophrenia. Some antipsychotics block domapinergic receptors as well as cholinergic, noradrenergic and histaminergic receptors. Remoxipride was developed to act specifically on the dopamine D2 receptor. As a consequence, several undesired side effects can occur. Patients often feel they are not taking any antipsychotic drug. It has a potent affinity for the sigma receptor, but it is unclear whether it is a sigma agonist or antagonist. The contribution of this property to its clinical profile is unknown. Blocking the D2 dopamine receptor is known to cause relapse in patients that have achieved remission from depression, and such blocking also counteracts the effectiveness of SSRI medication.
    Mechanism of action Remoxipride acts as an antagonist at the D2 dopamine receptor. It is believed that overactivity of dopamine systems in the mesolimbic pathway may contribute to the "positive symptoms" of schizophrenia (such as delusions and hallucinations), whereas problems with dopamine function in the mesocortical pathway may be responsible for the "negative symptoms", such as avolition, flat emotional response and alogia. Therefore, by decreasing the levels of dopamine in these pathways, it is thought that remoxipride is able to reduce the symptoms of schizophrenia, particularily the "positive symptoms".
    Absorption Rapidly absorbed. Absolute bioavailability is 90%.
    Volume of distribution Not Available
    Protein binding 89-98%
    Metabolism
    No active metabolites
    Route of elimination Not Available
    Half life 4-7 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
    water solubility 74 mg/L Not Available
    logP 2.10 HOEGBERG,T ET AL. 1986
    Predicted Properties
    Property Value Source
    water solubility 1.27e-01 g/l ALOGPS
    logP 2.94 ALOGPS
    logP 2.34 ChemAxon
    logS -3.5 ALOGPS
    pKa (strongest acidic) 13.06 ChemAxon
    pKa (strongest basic) 8.4 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 4 ChemAxon
    hydrogen donor count 1 ChemAxon
    polar surface area 50.8 ChemAxon
    rotatable bond count 6 ChemAxon
    refractivity 90.56 ChemAxon
    polarizability 36.25 ChemAxon
    药物相互作用
    食物相互作用
    • Take without regard to meals.

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