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氨磺必利 /Amisulpride {[allProObj[0].p_purity_real_show]}

货号:A517016 同义名: 阿米舒必利 / DAN 2163

Amisulpride is a selective dopamine antagonist wit Ki of 2.8 nM for D2 receptor and Ki of 3.2 nM D3 receptor, it's used as an antipsychotic drug.

Amisulpride 化学结构 CAS号:71675-85-9
Amisulpride 化学结构
CAS号:71675-85-9
Amisulpride 3D分子结构
CAS号:71675-85-9
Amisulpride 化学结构 CAS号:71675-85-9
Amisulpride 3D分子结构 CAS号:71675-85-9
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Amisulpride 纯度/质量文件 产品仅供科研

货号:A517016 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 D1 receptor D2 receptor D3 receptor D4 receptor D5 receptor DAT Dopamine receptor 其他靶点 纯度
Penfluridol +

Dopamine receptor, Ki: 1.6 μM

98%
Ansofaxine HCl ++

Dopamine receptor, IC50: 491 nM

98%
Tetrahydroberberine,THB +

D2 receptor, pKi: 6.08

98+%
Prochlorperazine Maleate 95%
Olanzapine 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

98%
Ropinirole hydrochloride ++

D2 receptor, Ki: 29 nM

99%
Lurasidone ++++

D2 receptor, Ki: 1 nM

98%
Levosulpiride 99+%
Pridopidine 95%
Metoclopramide 99+%
Molindone HCl 98%
Sulpiride 99+%
Perospirone ++++

D2 receptor, Ki: 1.4 nM

99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

98+%
Phenothiazine 98%
Pimozide +

Dopamine D1 receptor, Ki: 6600 nM

+++

Dopamine D2 receptor, Ki: 3.0 nM

++++

Dopamine D3 receptor, Ki: 0.83 nM

98%
Rotundine ++

D1 receptor, IC50: 166 nM

+

D2 receptor, IC50: 1.47 μM

+

D3 receptor, IC50: 3.25 μM

98%
Domperidone 99+%
ONC206 97%
Pimethixene maleate ++

Dopamine D1 Receptor, pKi: 6.37

+++

Dopamine D2 Receptor, pKi: 8.19

++

Dopamine D4.4 Receptor, pKi: 7.54

97%
Loxapine succinate ++

D2 receptor (Human), Ki: 62 nM

D1 receptor (human), Ki: 26 nM

++

D2 receptor (bovine), Ki: 26 nM

D2 receptor (human), Ki: 24 nM

+++

D4 receptor (human), Ki: 7.5 nM

99%
Chlorprothixene +++

D1 receptor, Ki: 18 nM

+++

D2 receptor, Ki: 2.96 nM

+++

D3 receptor, Ki: 4.56 nM

+++

D5 receptor, Ki: 9 nM

98%
SCH-23390 HCl ++++

D1 dopamine receptor, Ki: 0.2 nM

++++

D5 dopamine receptor, Ki: 0.3 nM

98%
MPP+ iodide 97%
σ1 Receptor antagonist-1 +

DAT, pKi: 5.8

97%
Benztropine mesylate ++

DAT, IC50: 118 nM

98%
Azaperone 98%
Ziprasidone HCl 98+%
Paliperidone 98%
Alizapride HCl 99+%
Amisulpride 98%
Quetiapine hemifumarate Adrenergic Receptor 98%
Clozapine N-oxide 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Amisulpride 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].

Amisulpride 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 <<

Amisulpride 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

Amisulpride 实验方案

计算器
存储液制备 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

Amisulpride 技术信息

CAS号71675-85-9
分子式C17H27N3O4S
分子量 369.479
别名 阿米舒必利 ;DAN 2163
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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
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