| 产品描述: | TrkB拮抗剂;TrkB antagonist;ANA-12是有效,选择性的 TrkB 拮抗剂,对高亲和力和低亲和力位点的IC50 分别为45.6 nM和41.1 μM。;ANA-12 is an effective and selective TrkB antagonist with IC50 of 45.6 nM and 41.1 μM for high affinity and low affinity sites respectively. |
| 体内研究: |
ANA-12 (0.5 mg/kg,ip) 部分抑制小鼠全脑的总内源性 TrkB 活性。注射到小鼠体内的 ANA-12 在 0.5 mg/kg 时表现出抗焦虑和抗抑郁活性。ANA-12 (0.5、1.0 和 2.0 mg/kg) 不影响神经元存活。ANA-12 (0.5 mg/kg) 对脂多糖 (LPS) 诱导的抑郁样行为具有抗抑郁作用。ANA-12 (0.5 mg/kg) 显著减弱抑郁小鼠不动时间的增加。在 TST、FST 和 SPT 中,ANA-12 (0.5 mg/kg) 在对照小鼠中未显示出抗抑郁样作用。 ANA-12 (0.5 mg/kg,腹腔注射) 逆转 CocSired 大鼠中可卡因的自我给药减少。 |
| 参考文献: |
1. Cazorla M, et al. Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice. J Clin Invest. 2011 May;121(5):1846-57. 2. Fang X, et al. Brain-derived neurotrophic factor-TrkB signaling in the medial prefrontal cortex plays a role in the anhedonia-like phenotype after spared nerve injury. Eur Arch Psychiatry Clin Neurosci. 2018 Jun 7. 3. Zhang JC, et al. Comparison of ketamine, 7,8-dihydroxyflavone, and ANA-12 antidepressant effects in the social defeat stress model of depression. Psychopharmacology (Berl). 2015 Dec;232(23):4325-35. 4. Vassoler FM, et al. Epigenetic inheritance of a cocaine-resistance phenotype. Nat Neurosci. 2013 Jan;16(1):42-7. |
| 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 |
2.454 ml |
12.27 ml |
24.54 ml |
| 5 mM |
0.491 ml |
2.454 ml |
4.908 ml |
| 10 mM |
0.245 ml |
1.227 ml |
2.454 ml |
| 50 mM |
0.049 ml |
0.245 ml |
0.491 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。 |