产品描述: | Anavex 2-73 is a Sigma-1 Receptor agonist (IC50: 860 nM) |
靶点: |
Sigma receptor;Sigmareceptor |
体内研究: |
The pretreatment of Anavex 2-73 (1/3 mg/kg) dose-dependently reduces the scopolamine-induced alternation deficit. The pretreatment with Anavex 2-73 (>0.3 mg/kg) dose-dependently and significantly attenuates the impairments of step-through latency. The Anavex 2-73 (1mg/kg) dose-dependently blocks the recognition memory deficit. One day after injections, the significant Aβ25-35-induced decrease in Akt phosphorylation is significantly attenuated by Anavex 2-73 (0.1/1mg/kg). Seven days after injections, Anavex 2-73 attenuates the decrease in Ser9 phosphorylation induced by the peptide (0.3/1mg/kg) |
动物实验: |
Drugs (including Anavex 2-73) are solubilized in physiological saline at the concentration of 5mg/mL.Male mice aged 7-9 weeks and weighing 32±2?g are used. Drugs (including Anavex 2-73) are brought up to each dose by dilution and injected in a volume of 100μL/20g body weight. Animals are used between days 1 and 9 after i.c.v. injections for behavioral testing or killed before biochemical measures. |
参考文献: |
1. Valentine Lahmy, et al. Blockade of Tau Hyperphosphorylation and Aβ1-42 Generation by the Aminotetrahydrofuran Derivative ANAVEX2-73, a Mixed Muscarinic andσ1 Receptor Agonist, in a Nontransgenic Mouse Model of Alzheimer's Disease. Neuropsychopharmacology. 2013 Aug; 38(9): 1706-1723. 2. Villard V, et al. Anti-amnesic and neuroprotective potentials of the mixed muscarinic receptor/sigma 1 (σ1) ligand ANAVEX2-73, a novel aminotetrahydrofuran derivative. J Psychopharmacol. 2011 Aug;25(8):1101-17. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
3.146 ml |
15.731 ml |
31.461 ml |
5 mM |
0.629 ml |
3.146 ml |
6.292 ml |
10 mM |
0.315 ml |
1.573 ml |
3.146 ml |
50 mM |
0.063 ml |
0.315 ml |
0.629 ml |
|
注意: |
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