| 产品描述: | Bifemelane hydrochloride (MCI-2016) is a potent, selective and competitive inhibitor of monoamine oxidase A (MAO-A), with a Ki of 4.20 μM. Bifemelane hydrochloride also inhibits MAO-B noncompetitively with a Ki of 46.0 μM. Bifemelane hydrochloride has a potent antidepressant activity and can be used for the research of cognitive and emotional disturbances related to cerebrovascular disease |
| 靶点: |
MAO-A:4.2 μM (Ki);MAO-B:46 μM (Ki) |
| 体外研究: |
Bifemelane inhibits MAO-A in a dose-dependent manner, with Kis of 4.2±0.2 and 14.1±0.7 μM in human brain synaptosomes and human liver mitochondria respectively. Bifemelane inhibits MAO-B activities in a dose-dependent manner, with Kis of 46.0±3.6 and 65.2±7.0 μM in human brain synaptosomes and human liver mitochondria respectively. |
| 体内研究: |
Bifemelane (20-80 mg/kg; i.p.) dose-dependently decreases exploratory activity in the open field test. Bifemelane (20-80 mg/kg; i.p.) decreases immobility time in the forced swim test, although is not clearly dosedependent and has already reached ceiling at 20 mg/kg. Animal Model: Wistar male rats (230-270 g) are induced hypothermia by Reserpine Dosage: 20, 40, 80 mg/kg Administration: A single i.p. Result: Attenuated the Reserpine-induced hypothermia by a maximum of 10 ℃. |
| 参考文献: |
1. Naoi M, et, al. 4-(O-benzylphenoxy)-N-methylbutylamine (bifemelane) and other 4-(O-benzylphenoxy)-N-methylalkylamines as new inhibitors of type A and B monoamine oxidase. J Neurochem. 1988 Jan; 50(1): 243-7. 2. Fasipe OJ, et, al. The emergence of new antidepressants for clinical use: Agomelatine paradox versus other novel agents. IBRO Rep. 2019 Jan 9; 6:95-110. 3. Moryl E, et, al. Potential antidepressive properties of amantadine, memantine and bifemelane. Pharmacol Toxicol. 1993 Jun; 72(6): 394-7. |
| 溶解性: |
Soluble in DMSO |
| 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 |
3.27 ml |
16.348 ml |
32.696 ml |
| 5 mM |
0.654 ml |
3.27 ml |
6.539 ml |
| 10 mM |
0.327 ml |
1.635 ml |
3.27 ml |
| 50 mM |
0.065 ml |
0.327 ml |
0.654 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。 |