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Amisulpride

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Chemical Structure| 71675-85-9 同义名 : 阿米舒必利 ;DAN 2163
CAS号 : 71675-85-9
货号 : A517016
分子式 : C17H27N3O4S
纯度 : 98%
分子量 : 369.479
MDL号 : MFCD00866691
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(135.33 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Dopamine receptor
描述 Amisulpride as a specific dopamine receptor antagonist with high and similar affinity for the dopamine D2 and D3 receptor. In vitro, amisulpride has high affinity and selectivity for the human dopamine D2 (Ki = 2.8 nM) and D3 (Ki = 3.2 nM) receptors. Amisulpride has high affinity and selectivity for the human dopamine D2 (Ki = 2.8 nM) and D3 (Ki = 3.2 nM) receptors. At low doses (< or = 10 mg/kg) amisulpride preferentially blocks presynaptic dopamine autoreceptors that control dopamine synthesis and release in the rat, whereas at higher doses (40-80 mg/kg) postsynaptic dopamine D2 receptor occupancy and antagonism is apparent[3]. Amisulpride has an antidepressant like activity comparable to that of olanzapine though the activity was significantly less than that of fluoxetine[4]. Amisulpride 400 to 800 mg/day was more effective than haloperidol, risperidone and flupenthixol in controlling affective symptoms in these patients. In randomised, double-blind trials involving patients with predominantly negative symptoms of schizophrenia, amisulpride 50 to 300 mg/day was more effective than placebo. Amisulpride is effective as maintenance therapy in patients with chronic schizophrenia. Long-term treatment with amisulpride was associated with improvements in quality of life and social functioning. Amisulpride is generally well tolerated[5]. Low-dose amisulpride is effective and well tolerated as a treatment for VLOSLP (Very late-onset (aged ≥ 60 years) schizophrenia-like psychosis), with benefits maintained by prolonging treatment. Potential adverse events include clinically significant extrapyramidal symptoms and falls[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01323205 Schizophrenia Phase 2 Completed - Austria ... 展开 >> Innsbruck, Austria Salzburg, Austria Wien, Austria Belgium Dave, Belgium Duffel, Belgium Kortenberg, Belgium Lede, Belgium Bulgaria Plovdiv, Bulgaria Radnevo N/A, Bulgaria Germany Berlin, Germany Hamburg, Germany Mainz, Germany Mannheim, Germany München, Germany Romania Arad, Romania Brasov, Romania Iasi, Romania Sibiu, Romania Spain Barcelona, Spain Zamora, Spain 收起 <<
NCT02374567 Dementia Depr... 展开 >>ession Schizophrenia Psychosomatic Disorders Anxiety Disorders 收起 << Phase 3 Terminated - Germany ... 展开 >> Bezirkskrankenhaus Augsburg Augsburg, Germany Krankenhaus Hedwigshöhe Berlin, Germany Hannover Medical School Hannover, Germany, 30625 Asklepios Fachklinikum Lübben Lübben, Germany Asklepios Fachklinikum Teupitz Teupitz, Germany 收起 <<
NCT02855229 - Recruiting March 2020 United States, Massachusetts ... 展开 >> McLean Hospital Recruiting Belmont, Massachusetts, United States, 02478 Contact: David J Crowley, ALM    800-333-0338 ext 4432    neurolab@mclean.harvard.edu    Principal Investigator: Diego A Pizzagalli, PhD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.53mL

2.71mL

1.35mL

27.07mL

5.41mL

2.71mL
参考文献

[1]Sarkhel S, Praharaj SK, et al. Amisulpride-induced macrocytic anemia. J Neuropsychiatry Clin Neurosci. 2013 Winter;25(1):E10-1.

[2]Schoemaker H, Claustre Y, et al. Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity. J Pharmacol Exp Ther. 1997 Jan;280(1):83-97.

[3]Schoemaker H, Claustre Y, Fage D, et al. Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity. J Pharmacol Exp Ther. 1997;280(1):83‐97

[4]Pawar GR, Agrawal RP, Phadnis P, Paliwal A, Vyas S, Solanki P. Evaluation of antidepressant like property of amisulpride per se and its comparison with fluoxetine and olanzapine using forced swimming test in albino mice. Acta Pol Pharm. 2009;66(3):327‐331

[5]Curran MP, Perry CM. Amisulpride: a review of its use in the management of schizophrenia. Drugs. 2001;61(14):2123‐2150

[6]Reeves S, Eggleston K, Cort E, et al. Therapeutic D2/3 receptor occupancies and response with low amisulpride blood concentrations in very late-onset schizophrenia-like psychosis (VLOSLP). Int J Geriatr Psychiatry. 2018;33(2):396‐404