4'-Dimethylamino-7,8-dihydroxyflavone
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| Clinical data | |
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| ATC code | None |
| Identifiers | |
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| CAS Number | 1205548-04-4 |
| PubChem (CID) | 44610701 |
| ChemSpider | 26630138 |
| ChEMBL | CHEMBL1800922 |
| Chemical and physical data | |
| Formula | C17H15NO4 |
| Molar mass | 297.3053 g/mol |
| 3D model (Jmol) | Interactive image |
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4'-Dimethylamino-7,8-dihydroxyflavone (4'-DMA-7,8-DHF) is a synthetic flavone and selective small-molecule agonist of TrkB, the main receptor of brain-derived neurotrophic factor (BDNF), that was derived from structural modification of 7,8-dihydroxyflavone (7,8-DHF).[1][2][3][4] Relative to 7,8-DHF, 4'-DMA-7,8-DHF possesses higher agonistic activity at TrkB, is significantly more potent than 7,8-DHF both in vitro and in vivo, and has a longer duration of action (peaking at 4 hours and "partially decaying" at 8~16 hours in rodents).[1][3] The compound has been found to produce neuroprotective, neurogenic, and antidepressant-like effects in animals.[1][3][4][5]
See also
References
- 1 2 3 Liu, Xia; Chan, Chi-Bun; Jang, Sung-Wuk; Pradoldej, Sompol; Huang, Junjian; He, Kunyan; Phun, Lien H.; France, Stefan; Xiao, Ge; Jia, Yonghui; Luo, Hongbo R.; Ye, Keqiang (2010). "A Synthetic 7,8-Dihydroxyflavone Derivative Promotes Neurogenesis and Exhibits Potent Antidepressant Effect". Journal of Medicinal Chemistry. 53 (23): 8274–8286. doi:10.1021/jm101206p. ISSN 0022-2623.
- ↑ Liu, Xia; Chan, Chi-Bun; Qi, Qi; Xiao, Ge; Luo, Hongbo R.; He, Xiaolin; Ye, Keqiang (2012). "Optimization of a Small Tropomyosin-Related Kinase B (TrkB) Agonist 7,8-Dihydroxyflavone Active in Mouse Models of Depression". Journal of Medicinal Chemistry. 55 (19): 8524–8537. doi:10.1021/jm301099x. ISSN 0022-2623.
- 1 2 3 Liu, Chaoyang; Chan, Chi Bun; Ye, Keqiang (2016). "7,8-dihydroxyflavone, a small molecular TrkB agonist, is useful for treating various BDNF-implicated human disorders". Translational Neurodegeneration. 5 (1). doi:10.1186/s40035-015-0048-7. ISSN 2047-9158.
- 1 2 Zeng, Yan; Wang, Xiaonan; Wang, Qiang; Liu, Shumin; Hu, Xiamin; McClintock, Shawn (2013). "Small Molecules Activating TrkB Receptor for Treating a Variety of CNS Disorders". CNS & Neurological Disorders - Drug Targets. 12 (7): 1066–1077. doi:10.2174/18715273113129990089. ISSN 1871-5273.
- ↑ Jiang, M.; Peng, Q.; Liu, X.; Jin, J.; Hou, Z.; Zhang, J.; Mori, S.; Ross, C. A.; Ye, K.; Duan, W. (2013). "Small-molecule TrkB receptor agonists improve motor function and extend survival in a mouse model of Huntington's disease". Human Molecular Genetics. 22 (12): 2462–2470. doi:10.1093/hmg/ddt098. ISSN 0964-6906.
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