| CAS NO: | 71675-85-9 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 50mg | 询价 |
| 100mg | 询价 |
| 250mg | 询价 |
| 500mg | 询价 |
| 1g | 询价 |
| 2g | 询价 |
| Molecular Weight (MW) | 369.48 |
|---|---|
| Formula | C17H27N3O4S |
| CAS No. | 71675-85-9 (free base); |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 74 mg/mL (200.3 mM) |
| Water: <1 mg/mL | |
| Ethanol: 74 mg/mL (200.3 mM) | |
| Other info | Chemical Name: 4-amino-N-[(1-ethylpyrrolidin-2-yl)methyl]-5-ethylsulfonyl-2-methoxybenzamide InChi Key: NTJOBXMMWNYJFB-UHFFFAOYSA-N InChi Code: InChI=1S/C17H27N3O4S/c1-4-20-8-6-7-12(20)11-19-17(21)13-9-16(25(22,23)5-2)14(18)10-15(13)24-3/h9-10,12H,4-8,11,18H2,1-3H3,(H,19,21) SMILES Code: CCN1CCCC1CNC(=O)C2=CC(=C(C=C2OC)N)S(=O)(=O)CC |
| Synonyms | DAN-2163; Solian; Amazeo; Amipride; Amival; Soltus; Aminosultopride; DAN 2163; DAN2163; Deniban; Amisulprida; Sulpitac; Sulprix |
| In Vitro | In vitro activity: 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. Cell Assay: 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. |
|---|---|
| In Vivo | Only the highest dose of Amisulpride (100 mg/kg) significantly reduces dopamine levels in the striatum or limbic system. Amisulpride significantly increases the synthesis of dopamine in the rat striatum and limbic system at doses of 20 and 100 mg/kg. Amisulpride (0.5 to 75 mg/kg) fails to provoke an additional increase in dopa accumulation in the striatum but slightly accelerates, at 75 mg/kg, dopamine synthesis in the limbic system. In comparison with vehicle-treated controls, Amisulpride (10 mg/kg) increases extracellular dopamine levels. The administration of Amisulpride (0.5 to 15 mg/kg s.c.) provokes a time- and dose-dependent increase in the stimulation-evoked dopamine release. Amisulpride decreases striatal ACh levels significantly at 30 and 100 mg/kg (87.5% and 56.3% of control levels, respectively)[1]. In both acute study, Amisulpride (70 mg/kg, p.o.) significantly increases the duration of swimming behavior [F(3,28)=45.90, p<0.01]. |
| Animal model | Mice |
| Formulation & Dosage | 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 |
| References | J Pharmacol Exp Ther. 1997 Jan;280(1):83-97.; Acta Pol Pharm. 2009 May-Jun;66(3):327-31. |
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