From Wikipedia, the free encyclopedia
Chemical compound
Eutropoflavin (4'-Dimethylamino-7,8-dihydroxyflavone ) 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
tropoflavin (7,8-DHF).
[1]
[2]
[3]
[4] Relative to tropoflavin, eutropoflavin possesses higher agonistic activity at TrkB, is significantly more potent than tropoflavin 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 and
neurogenic effects in the brain and spinal cord as well as
antidepressant -like effects in animals.
[1]
[3]
[4]
[5]
^
a
b
c Liu X, Chan CB, Jang SW, Pradoldej S, Huang J, He K, et al. (December 2010).
"A synthetic 7,8-dihydroxyflavone derivative promotes neurogenesis and exhibits potent antidepressant effect" . Journal of Medicinal Chemistry . 53 (23): 8274–86.
doi :
10.1021/jm101206p .
PMC
3150605 .
PMID
21073191 .
^ Liu X, Chan CB, Qi Q, Xiao G, Luo HR, He X, Ye K (October 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): 8524–37.
doi :
10.1021/jm301099x .
PMC
3491656 .
PMID
22984948 .
^
a
b
c Liu C, Chan CB, Ye K (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 .
PMC
4702337 .
PMID
26740873 .
^
a
b Zeng Y, Wang X, Wang Q, Liu S, Hu X, McClintock SM (November 2013). "Small molecules activating TrkB receptor for treating a variety of CNS disorders". CNS & Neurological Disorders Drug Targets . 12 (7): 1066–77.
doi :
10.2174/18715273113129990089 .
PMID
23844685 .
^ Jiang M, Peng Q, Liu X, Jin J, Hou Z, Zhang J, et al. (June 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): 2462–70.
doi :
10.1093/hmg/ddt098 .
PMC
3658168 .
PMID
23446639 .
Aglycones
Monohydroxyflavone Dihydroxyflavones Trihydroxyflavones Tetrahydroxyflavones Pentahydroxyflavones O-methylated flavones
Glycosides
of apigenin of baicalein of hypolaetin of luteolin
Acetylated Sulfated glycosides Polymers Drugs
Angiopoietin
CNTF
EGF (ErbB)
FGF
FGFR1
FGFR2
Agonists:
Ersofermin
FGF (
1 ,
2 (bFGF) ,
3 ,
4 ,
5 ,
6 ,
7 (
KGF ),
8 ,
9 ,
10 (KGF2) ,
17 ,
18 ,
22 )
Palifermin
Repifermin
Selpercatinib
Sprifermin
Trafermin
FGFR3
FGFR4 Unsorted
HGF (c-Met)
IGF
LNGF (p75NTR )
PDGF
RET (GFL)
SCF (c-Kit)
TGFβ
Trk
TrkA
Negative allosteric modulators:
VM-902A
TrkB
Agonists:
3,7-DHF
3,7,8,2'-THF
4'-DMA-7,8-DHF
7,3'-DHF
7,8-DHF
7,8,2'-THF
7,8,3'-THF
Amitriptyline
BDNF
BNN-20
Deoxygedunin
Deprenyl
Diosmetin
DMAQ-B1
HIOC
LM22A-4
N-Acetylserotonin
NT-3
NT-4
Norwogonin (5,7,8-THF)
R7
R13
TDP6
TrkC
VEGF Others
Additional growth factors:
Adrenomedullin
Colony-stimulating factors (see
here instead)
Connective tissue growth factor (CTGF)
Ephrins (
A1 ,
A2 ,
A3 ,
A4 ,
A5 ,
B1 ,
B2 ,
B3 )
Erythropoietin (see
here instead)
Glucose-6-phosphate isomerase (GPI; PGI, PHI, AMF)
Glia maturation factor (GMF)
Hepatoma-derived growth factor (HDGF)
Interleukins /
T-cell growth factors (see
here instead)
Leukemia inhibitory factor (LIF)
Macrophage-stimulating protein (MSP; HLP, HGFLP)
Midkine (NEGF2)
Migration-stimulating factor (MSF; PRG4)
Oncomodulin
Pituitary adenylate cyclase-activating peptide (PACAP)
Pleiotrophin
Renalase
Thrombopoietin (see
here instead)
Wnt signaling proteins
Additional growth factor receptor modulators:
Cerebrolysin (neurotrophin mixture)