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4'-Dimethylamino-7,8-dihydroxyflavone

4'-Dimethylamino-7,8-dihydroxyflavone
4'-Dimethylamino-7,8-dihydroxyflavone.svg
Clinical data
ATC code
  • None
Identifiers
CAS Number
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC17H15NO4
Molar mass297.305 g/mol g·mol−1
3D model (JSmol)

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), which 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. ^ a b c 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. PMC 3150605. PMID 21073191.
  2. ^ 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. PMC 3491656. PMID 22984948.
  3. ^ a b c 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): 2. doi:10.1186/s40035-015-0048-7. ISSN 2047-9158. PMC 4702337. PMID 26740873.
  4. ^ a b 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. PMID 23844685.
  5. ^ 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. PMC 3658168. PMID 23446639.