Amisulpride hydrochloride
(Synonyms: 氨磺必利盐酸盐; DAN 2163 hydrochloride) 目录号 : GC35323
A dopamine D2 and D3 and 5-HT2B, 5-HT7, and 5-HT7A receptor antagonist
Cas No.:81342-13-4
Sample solution is provided at 25 µL, 10mM.
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Amisulpride is a dopamine D2 and D3 receptor antagonist (Kis = 3 and 3.5 nM, respectively).1 It is also an antagonist of the serotonin (5-HT) receptor subtypes 5-HT2B, 5-HT7, and 5-HT7A (Kis = 13, 11.5, and 135.5 nM, respectively). It is selective for these receptors over a panel of 39 additional receptors, ion channels, and transporters (Kis = >1,000 nM for all). Amisulpride increases 7-OH-DPAT-induced decreases in dopamine and acetylcholine release in electrically stimulated rat striatal slices (EC50s = 2.2 and 1.2 nM, respectively).2 It increases the levels of dopamine and the dopamine metabolite 3,4-dihydroxyphenylacetic acid (DOPAC) in rat striatum and nucleus accumbens when administered intraperitoneally at a dose of 10 mg/kg. Amisulpride decreases immobility time in the forced swim test in rats, as well as increases stress-induced decreases in sucrose consumption in a rat model of depression induced by chronic mild stress.3
1.Abbas, A.I., Hedlund, P.B., Huang, X.P., et al.Amisulpride is a potent 5-HT7 antagonist: Relevance for antidepressant actions in vivoPsychopharmacology (Berl.)205(1)119-128(2009) 2.Schoemaker, H., Claustre, Y., Fage, D., et al.Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivityJ. Pharmacol. Exp. Ther.280(1)83-97(1997) 3.Papp, M., and Wieronska, J.Antidepressant-like activity of amisulpride in two animal models of depressionJ. Psychopharmacol.14(1)46-52(2000)
Cell experiment: | The functional effects of Amisulpride hydrochloride at the dopamine D3 receptor subtype are assessed. Briefly, the mitogenic response elicited in NG108-15 neuroblastoma-glioma cells stably transfected with human dopamine D3 receptor cDNA by the addition of 10 nM quinpirole in the presence of 1 μM forskolin is quantified by the incorporation of [3H]thymidine. Antagonism of quinpirole-induced mitogenesis is measured in the presence of increasing (0.1 to 100 nM) concentrations of Amisulpride hydrochloride[1]. |
Animal experiment: | A total of 64 male Swiss albino mice weighing between 20 to 30 g are used. The animals are fed with standard pellet diet and water ad libitum. The mice are divided in different groups (n=8 in each group) and drug administration is done as follows: Group 1 (control): distilled water (1 mL/kg) 23.5, 5 and 1 h before the test. Group 3 (Amisulpride hydrochloride): Amisulpride hydrochloride (70 mg/kg) 23.5, 5 and 1 h before the test[2]. |
References: [1]. Schoemaker H, 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. | |
| Cas No. | 81342-13-4 | SDF | |
| 别名 | 氨磺必利盐酸盐; DAN 2163 hydrochloride | ||
| Canonical SMILES | CCN1C(CNC(C2=CC(S(=O)(CC)=O)=C(N)C=C2OC)=O)CCC1.Cl | ||
| 分子式 | C17H28ClN3O4S | 分子量 | 405.94 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4634 mL | 12.3171 mL | 24.6342 mL |
| 5 mM | 0.4927 mL | 2.4634 mL | 4.9268 mL |
| 10 mM | 0.2463 mL | 1.2317 mL | 2.4634 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet