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R13 (drug)
R13
is a
small-molecule
flavonoid
and
orally active
,
potent
, and
selective agonist
of the
tropomyosin receptor kinase B
– the main
signaling receptor
for the
neurotrophin
brain-derived neurotrophic factor
– which is
under development
for the potential
treatment
of
Alzheimer's disease
. It is a
structural modification
and
prodrug
of
7,8-dihydroxyflavone
with
improved
potency and
pharmacokinetics
,
namely
oral bioavailability
and
duration
.
The compound
is a
replacement
for the earlier 7,8-DHF 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
into 7,8-DHF in
human liver
microsomes
. In
contrast
to R7, R13 is readily
hydrolyzed
into 7,8-DHF in
human
liver
microsomes.