用户名： 密   码：
注册 | 忘记密码？
药品详细

Amisulpride(氨磺必利)

化学结构式图
中文名
氨磺必利
英文名
Amisulpride
分子式
C17H27N3O4S
化学名
4-amino-5-(ethanesulfonyl)-N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxybenzamide
分子量
Average: 369.479
Monoisotopic: 369.172227057
CAS号
53583-79-2
ATC分类
N05A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Amisulpride (trade name Solian) is an antipsychotic drug sold by Sanofi-Aventis. It is not approved for use in the United States, but is approved for use in Europe and Australia for the treatment of psychoses and schizophrenia. Additionally, it is approved in Italy for the treatment of dysthymia (under the brand name Deniban). Amisulpride is a selective dopamine antagonist.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Rosenzweig P, Canal M, Patat A, Bergougnan L, Zieleniuk I, Bianchetti G: A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers. Hum Psychopharmacol. 2002 Jan;17(1):1-13. Pubmed
    2. Moller HJ: Amisulpride: limbic specificity and the mechanism of antipsychotic atypicality. Prog Neuropsychopharmacol Biol Psychiatry. 2003 Oct;27(7):1101-11. Pubmed
    3. Weizman T, Pick CG, Backer MM, Rigai T, Bloch M, Schreiber S: The antinociceptive effect of amisulpride in mice is mediated through opioid mechanisms. Eur J Pharmacol. 2003 Oct 8;478(2-3):155-9. Pubmed
    4. Leucht S, Pitschel-Walz G, Engel RR, Kissling W: Amisulpride, an unusual “atypical” antipsychotic: a meta-analysis of randomized controlled trials. Am J Psychiatry. 2002 Feb;159(2):180-90. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes Not Available
    Substructures Not Available
    适应症
    药理
    Indication Investigated for use/treatment in schizophrenia and schizoaffective disorders, mania in bipolar disorder, and depression.
    Pharmacodynamics Not Available
    Mechanism of action Amisulpride binds selectively to dopamine D(2) and D(3) receptors in the limbic system. Low doses of amisulpride preferentially block presynaptic D(2)/D(3)-dopamine autoreceptors, thereby enhancing dopaminergic transmission, whereas higher doses block postsynaptic receptors, thus inhibiting dopaminergic hyperactivity. It may also have 5-ht7 antagonistic effect, useful in depression treatment.
    Absorption Bioavailability is 48% following oral administration.
    Volume of distribution Not Available
    Protein binding Low (17%)
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life Approximately 12 hours
    Clearance Not Available
    Toxicity Overdoses of amisulpride have been linked with torsades de pointes.
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 181-182 °C PhysProp
    logP 1.06 MANNHOLD,R ET AL. (1990)
    pKa 9.37 Not Available
    Predicted Properties
    Property Value Source
    water solubility 2.93e-01 g/l ALOGPS
    logP 1.5 ALOGPS
    logP 0.25 ChemAxon
    logS -3.1 ALOGPS
    pKa (strongest acidic) 14.03 ChemAxon
    pKa (strongest basic) 7.05 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 6 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 101.73 ChemAxon
    rotatable bond count 7 ChemAxon
    refractivity 99.84 ChemAxon
    polarizability 39.82 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

    返回 | 收藏