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  • Amisulpride
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Amisulpride

A dopamine D2 and D3 and 5-HT2B, 5-HT7, and 5-HT7A receptor antagonist

原价
¥612-2062
价格
490-1650
Amisulpride的二维码

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  • 货号: ajci9462
  • CAS: 71675-85-9
  • 别名: 氨磺必利; DAN 2163
  • 分子式: C17H27N3O4S
  • 分子量: 369.48
  • 纯度: >98%
  • 溶解度: ≥ 18.474mg/mL in DMSO
  • 储存: Store at -20°C
  • 库存: 现货

Background

Amisulpride is an atypical antagonist of dopamine D2/D3 receptor with Ki values of 2.8±0.4nM and 3.2±0.3nM for D2 and D3 receptor subtypes, respectively [1].


Amisulpride has shown high affinity to the cloned and stably transfected human dopamine D2 with Ki values of 2.8±0.4nM and 3.2±0.3nM for D2 and D3 receptor subtypes, respectively. Amisulpride has been reported to inhibit radioligand binding to native dopamine D2 receptor in membranes from the rat striatum with an IC50 value of 21nM. Besides, Amisulpride has been revealed to displace [3H]raclopride binding in vivo with an ED50 value of 17.3±1.86mg/kg in the rat limbic system. In addition, Amisulpride has been noted to inhibit quinpirole-induced [3H]thymidine with an IC50 value of 22±3nM [1].

参考文献:
[1] Schoemaker H1, Claustre Y, Fage D, Rouquier L, Chergui K, Curet O, Oblin A, Gonon F, Carter C, Benavides J, Scatton B. 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.

Protocol

Cell experiment:

The functional effects of Amisulpride 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[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): Amisulpride (70 mg/kg) 23.5, 5 and 1 h before the test[2].

参考文献:

[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.
[2]. Pawar GR, et al. 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 May-Jun;66(3):327-31.

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