7,8,3′-Trihydroxyflavone (7,8,3'-THF) is a
flavone
Flavone is an organic compound with the formula . A white solid, flavone is a derivative of chromone with a phenyl (Ph) substituent adjacent to the ether group. The compound is of little direct practical importance, but substituted derivatives, ...
and
small-molecule
In molecular biology and pharmacology, a small molecule or micromolecule is a low molecular weight (≤ 1000 daltons) organic compound that may regulate a biological process, with a size on the order of 1 nm. Many drugs are small molecules; t ...
agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...
of
TrkB
Tropomyosin receptor kinase B (TrkB), also known as tyrosine receptor kinase B, or BDNF/NT-3 growth factors receptor or neurotrophic tyrosine kinase, receptor, type 2 is a protein that in humans is encoded by the ''NTRK2'' gene. TrkB is a recept ...
, the main
receptor
Receptor may refer to:
* Sensory receptor, in physiology, any neurite structure that, on receiving environmental stimuli, produces an informative nerve impulse
*Receptor (biochemistry), in biochemistry, a protein molecule that receives and respond ...
of
brain-derived neurotrophic factor
Brain-derived neurotrophic factor (BDNF), or abrineurin, is a protein found in the and the periphery. that, in humans, is encoded by the ''BDNF'' gene. BDNF is a member of the neurotrophin family of growth factors, which are related to the can ...
(BDNF), that was derived from
tropoflavin (7,8-DHF).
Relative to tropoflavin, 7,8,3'-THF is 2–3-fold more potent ''in vitro'' as a TrkB agonist.
(7,3'-DHF) is also more potent than tropoflavin ''in vitro'', indicating that a 3'-hydroxy group on the B-ring enhances TrkB agonistic activity.
7,8,3'-THF has been tested ''in vivo'' and was found to produce TrkB-dependent
neuroprotective effects in mice similarly to tropoflavin.
See also
*
Tropomyosin receptor kinase B § Agonists
References
Flavones
Neuroprotective agents
TrkB agonists
Triols
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