R13 is a
small-molecule
Within the fields of 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 ar ...
flavonoid and
orally active,
potent, and
selective agonist of the
tropomyosin receptor kinase B
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 recep ...
(TrkB) – the main
signaling receptor for the
neurotrophin 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 canon ...
(BDNF) – which is under development for the potential treatment of
Alzheimer's disease.
It is a
structural modification and
prodrug of
tropoflavin (7,8-DHF) with improved potency and
pharmacokinetics, namely
oral
The word oral may refer to:
Relating to the mouth
* Relating to the mouth, the first portion of the alimentary canal that primarily receives food and liquid
**Oral administration of medicines
** Oral examination (also known as an oral exam or or ...
bioavailability
In pharmacology, bioavailability is a subcategory of absorption and is the fraction (%) of an administered drug that reaches the systemic circulation.
By definition, when a medication is administered intravenously, its bioavailability is 100%. Ho ...
and
duration
Duration may refer to:
* The amount of time elapsed between two events
* Duration (music) – an amount of time or a particular time interval, often cited as one of the fundamental aspects of music
* Duration (philosophy) – a theory of time and ...
.
The compound is a replacement for the earlier tropoflavin prodrug
R7 and has similar properties to it.
It was developed because while R7 displayed a good drug profile in animal studies, it showed almost no
conversion
Conversion or convert may refer to:
Arts, entertainment, and media
* "Conversion" (''Doctor Who'' audio), an episode of the audio drama ''Cyberman''
* "Conversion" (''Stargate Atlantis''), an episode of the television series
* "The Conversion" ...
into tropoflavin in human
liver
The liver is a major organ only found in vertebrates which performs many essential biological functions such as detoxification of the organism, and the synthesis of proteins and biochemicals necessary for digestion and growth. In humans, it ...
microsome
In cell biology, microsomes are heterogeneous vesicle-like artifacts (~20-200 nm diameter) re-formed from pieces of the endoplasmic reticulum (ER) when eukaryotic cells are broken-up in the laboratory; microsomes are not present in healthy, liv ...
s.
In contrast to R7, R13 is readily
hydrolyzed into tropoflavin in human liver microsomes.
See also
*
List of investigational antidepressants
This is a list of investigational antidepressants, or antidepressants that are currently under development for clinical use in the treatment of mood disorders but are not yet approved. ''Chemical/generic names are listed first, with developmental ...
*
Tropomyosin receptor kinase B § Agonists
References
External links
7,8-Dihydoxyflavone and 7,8-substituted flavone derivatives, compositions, and methods related thereto (US9975868B2)
Antidementia agents
Carbamates
Esters
Experimental drugs
Flavones
Neuroprotective agents
Nootropics
Prodrugs
TrkB agonists
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