| 产品描述： | Sunifiram (DM-235) is a piperazine derived ampakine-like drug which has nootropic effects in animal studies with significantly higher potency than piracetam. IC50 value: Target: in vitro: DM 232 and DM 235 are novel antiamnesic compounds structurally related to ampakines. The involvement of AMPA receptors in the mechanism of action of DM 232 and DM 235 was, therefore, investigated in vivo and in vitro. Both compounds (0.1 mg/kg i.p.) were able to reverse the amnesia induced by the AMPA receptor antagonist NBQX (30 mg/kg i.p.) in the mouse passive avoidance test. At the effective doses, the investigated compounds did not impair motor coordination, as revealed by the rota rod test, nor modify spontaneous motility and inspection activity, as revealed by the hole board test. In mouse hippocampal slices, sunifiram at 10-100 nM significantly enhanced LTP in a bell-shaped dose-response relationship which peaked at 10 nM. The enhancement of LTP by sunifiram treatment was inhibited by 7-chloro-kynurenic acid (7-ClKN), an antagonist for glycine-binding site of NMDAR, but not by ifenprodil, an inhibitor for polyamine site of NMDAR. in vivo: OBX mice were administered once a day for 7-12 days with sunifiram (0.01-1.0 mg/kg p.o.) from 10 days after operation with or without gavestinel (10 mg/kg i.p.), which is glycine-binding site inhibitor of N-methyl-d-aspartate receptor (NMDAR) |
| 靶点： |
AMPA Receptor |
| 体内研究： |
Sunifiram (0.001-0.1 mg/kg, 口服或腹腔注射, 单次给药, 给药时长 20 分钟) 能够在东莨菪碱 引起的失忆小鼠模型中发挥防止失忆的作用，且效果显著优于吡拉西坦 、茴拉西坦 和咯利普兰 。 |
| 参考文献： |
1. Galeotti N, et al. AMPA-receptor activation is involved in the antiamnesic effect of DM 232 (unifiram) and DM 235 (sunifiram). Naunyn Schmiedebergs Arch Pharmacol. 2003 Dec;368(6):538-45. 2. Moriguchi S, et al. Novel nootropic drug sunifiram enhances hippocampal synaptic efficacy via glycine-binding site of N-methyl-D-aspartate receptor. Hippocampus. 2013 Jun 3. 3. Moriguchi S, et al. Novel nootropic drug sunifiram improves cognitive deficits via CaM kinase II and protein kinase C activation in olfactory bulbectomized mice. Behav Brain Res. 2013 Apr 1;242:150-7. |
| 溶解性： |
Soluble in DMSO、H2O |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
4.06 ml |
20.3 ml |
40.601 ml |
| 5 mM |
0.812 ml |
4.06 ml |
8.12 ml |
| 10 mM |
0.406 ml |
2.03 ml |
4.06 ml |
| 50 mM |
0.081 ml |
0.406 ml |
0.812 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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