货号:A517016
同义名:
阿米舒必利
/ DAN 2163
Amisulpride是一种选择性的多巴胺 D2/D3 受体拮抗剂,Ki 值分别为 2.8 nM(D2)和 3.2 nM(D3),可用于研究精神分裂症和双相情感障碍。


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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 |
99% | |||||||||||||||||
| Tetrahydroberberine |
+
D2 receptor, pKi: 6.08 |
98+% | |||||||||||||||||
| Prochlorperazine Maleate | ✔ | 98% (HPLC) | |||||||||||||||||
| Olanzapine | ✔ | 99+% | |||||||||||||||||
| Trifluoperazine |
++++
Dopamine D2 receptor, IC50: 1.1 nM |
98% | |||||||||||||||||
| Ropinirole HCl |
++
D2 receptor, Ki: 29 nM |
99% | |||||||||||||||||
| Lurasidone |
++++
D2 receptor, Ki: 1 nM |
98% | |||||||||||||||||
| Levosulpiride | ✔ | 99+% | |||||||||||||||||
| Pridopidine | ✔ | 95% | |||||||||||||||||
| Metoclopramide | ✔ | ✔ | 99+% | ||||||||||||||||
| Molindone HCl | ✔ | 99% | |||||||||||||||||
| Sulpiride | ✔ | 99+% | |||||||||||||||||
| Perospirone |
++++
D2 receptor, Ki: 1.4 nM |
99% | |||||||||||||||||
| Perospirone HCl |
++++
D2 receptor, Ki: 1.4 nM |
99% | |||||||||||||||||
| 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 | ✔ | 99% | |||||||||||||||||
| 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 (human), Ki: 24 nM D2 receptor (bovine), Ki: 26 nM |
+++
D4 receptor (human), Ki: 7.5 nM |
98% | |||||||||||||||
| Chlorprothixene |
+++
D1 receptor, Ki: 18 nM |
+++
D2 receptor, Ki: 2.96 nM |
+++
D3 receptor, Ki: 4.56 nM |
+++
D5 receptor, Ki: 9 nM |
99% | ||||||||||||||
| 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。 | |||||||||||||||||||
| 靶点 |
|
| 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]. |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | 5-HT 7 receptor knock-out mice | Intra-peritoneal injection | 0.1, 1, 3, 10 mg/kg | Single dose, 30 minutes prior to test | To evaluate the antidepressant effects of Amisulpride in 5-HT 7 receptor knock-out mice | Psychopharmacology (Berl). 2009 Jul;205(1):119-28 |
| 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 << | |
| 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 |
|
| CAS号 | 71675-85-9 |
| 分子式 | C17H27N3O4S |
| 分子量 | 369.48 |
| SMILES Code | CCN1C(CNC(C2=CC(S(=O)(CC)=O)=C(N)C=C2OC)=O)CCC1 |
| MDL No. | MFCD00866691 |
| 别名 | 阿米舒必利 ;DAN 2163 |
| 运输 | 蓝冰 |
| InChI Key | NTJOBXMMWNYJFB-UHFFFAOYSA-N |
| Pubchem ID | 2159 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, 2-8°C |
| 溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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