Research Square (Research Square),
Год журнала:
2022,
Номер
unknown
Опубликована: Июль 25, 2022
Abstract
Increasing
extracellular
levels
of
serotonin
(5-HT)
in
the
brain
ameliorates
symptoms
depression
and
anxiety-related
disorders,
e.g.
social
phobias
post-traumatic
stress
disorder.
Recent
evidence
from
preclinical
clinical
studies
established
potential
drugs
inducing
release
5-HT
via
5-HT-transporter.
Nevertheless,
current
releasing
compounds
under
investigation
carry
risk
for
abuse
deleterious
side
effects.
Here,
we
demonstrate
that
S
-enantiomers
certain
ring-substituted
cathinones
show
preference
ex
vivo
vivo,
exert
5-HT-associated
effects
behavioral
models.
Importantly,
lead
cathinone
(i)
do
not
induce
substantial
dopamine
(ii)
display
reduced
off-target
activity
at
vesicular
monoamine
transporter-2
2B
-receptors;
indicative
low
abuse-liability
adverse
events.
Taken
together,
our
findings
identify
these
agents
as
first-in
class
leads
may
prove
useful
treatment
disorders
where
elevation
has
proven
beneficial.
Current Medicinal Chemistry,
Год журнала:
2021,
Номер
29(19), С. 3366 - 3391
Опубликована: Сен. 13, 2021
Epilepsy
is
a
chronic
brain
disorder
caused
by
the
abnormal
firing
of
neurons.
Up
to
now,
use
antiepileptic
drugs
main
method
epilepsy
treatment.
The
development
lasted
for
centuries.
In
general,
most
agents
entering
clinical
practice
act
on
balance
mechanisms
"excitability-inhibition".
More
specifically,
they
target
voltage-gated
ion
channels,
GABAergic
transmission
and
glutamatergic
transmission.
recent
years,
some
novel
representing
new
action
have
been
discovered.
Although
there
are
about
30
available
in
market,
it
still
urgent
need
discovering
more
effective
safer
drugs.
into
era:
from
serendipitous
discovery
evolutionary
mechanism-based
design.
This
article
presents
an
overview
drug
treatment
epilepsy,
including
series
traditional
Expert Review of Neurotherapeutics,
Год журнала:
2021,
Номер
21(11), С. 1309 - 1316
Опубликована: Сен. 14, 2021
Introduction
Mosaic
variants
arising
in
brain
tissue
are
increasingly
being
recognized
as
a
hidden
cause
of
focal
epilepsy.
This
knowledge
gain
has
been
driven
by
new,
highly
sensitive
genetic
technologies
and
genome-wide
analysis
from
surgical
resection
or
autopsy
small
proportion
patients
with
Recently
reported
novel
strategies
to
detect
mosaic
limited
have
exploited
trace
DNA
obtained
cerebrospinal
fluid
liquid
biopsies
stereo-electroencephalography
electrodes.Areas
covered
The
authors
review
the
data
on
these
innovative
approaches
published
PubMed
before
12
June
2021,
discuss
challenges
associated
their
application,
describe
how
they
likely
improve
detection
provide
new
molecular
diagnoses
therapeutic
targets
for
epilepsy,
potential
utility
other
nonmalignant
neurological
disorders.Expert
opinion
These
cutting-edge
may
reveal
etiology
epilepsies
guidance
precision
medicine.
Aspirantskiy Vestnik Povolzhiya,
Год журнала:
2023,
Номер
23(2), С. 43 - 52
Опубликована: Июнь 16, 2023
The
literature
review
provides
an
update
on
recent
advances
in
antiepileptic
pharmacotherapy.
article
considers
the
mechanisms
of
action
drugs,
range
efficacy,
side
effects
and
enzyme-inducing
properties,
potential
teratogenicity.
A
revealed
some
problems
patients
with
epilepsy
remaining
unresolved
to
this
day.
Despite
increase
number
anticonvulsants
years,
one-third
are
pharmacoresistant
therapy
continue
suffer
from
seizures.
hope
for
reducing
proportion
uncontrolled
seizures
rests
future
therapeutic
developments,
including
targeted
therapies
aimed
at
molecular
underlying
pathogenesis.
Clinical
outcomes
could
also
significantly
improve
development
new
highly
accurate
diagnostic
treatment
methods,
identification
biomarkers
drug
development,
as
well
routine
clinical
follow-up
introduction
truly
innovative
disease-modifying
therapies.
Journal of Education Health and Sport,
Год журнала:
2022,
Номер
12(1), С. 106 - 116
Опубликована: Янв. 14, 2022
Dravet
Syndrome
is
a
severe,
drug-resistant,
and
rare
epileptiform
disorder
that
typically
presented
in
the
first
year
of
life
an
otherwise
healthy
child.
It
characterized
by
prolonged
seizures
are
often
resistant
to
current
anti-epileptic
drug
regimens,
which
made
them
poorly
controlled,
almost
50%
patients
experience
at
least
four
tonic-clonic
per
month.
There
three
new
medicines:
stiripentol,
cannabidiol,
fenfluramine,
with
documented
efficacy
safety
as
adjunctive
therapies
pharmacoresistant
syndrome
treatment.
This
study
aimed
assess
fenfluramine
treatment
syndrome.
Our
material
consisted
publications,
were
found
PubMed,
Google
Scholar,
Embase
databases.
In
order
find
proper
search
has
been
conducted
use
combination
keywords
like:
“fenfluramine”,
“Dravet
syndrome”,
“epilepsy
treatment”,
pediatric
patients”.
The
step
was
publications
from
last
10
years.
second
carry
out
overview
publications.
Results
mentioned
studies
proved
syndrome,
provided
significantly
greater
reduction
convulsive
seizure
frequency
compared
placebo.
No
patient
developed
valvular
heart
disease
or
pulmonary
arterial
hypertension,
side
effects
occurred
during
its
mild
generally
well-tolerated.
bioequivalence
tolerability
single
oral
doses
hydrochloride
solution
fed
fasted
states
support
administration
without
regard
meals.
Fenfluramine
may
represent
important
option
for
Research Square (Research Square),
Год журнала:
2022,
Номер
unknown
Опубликована: Июль 25, 2022
Abstract
Increasing
extracellular
levels
of
serotonin
(5-HT)
in
the
brain
ameliorates
symptoms
depression
and
anxiety-related
disorders,
e.g.
social
phobias
post-traumatic
stress
disorder.
Recent
evidence
from
preclinical
clinical
studies
established
potential
drugs
inducing
release
5-HT
via
5-HT-transporter.
Nevertheless,
current
releasing
compounds
under
investigation
carry
risk
for
abuse
deleterious
side
effects.
Here,
we
demonstrate
that
S
-enantiomers
certain
ring-substituted
cathinones
show
preference
ex
vivo
vivo,
exert
5-HT-associated
effects
behavioral
models.
Importantly,
lead
cathinone
(i)
do
not
induce
substantial
dopamine
(ii)
display
reduced
off-target
activity
at
vesicular
monoamine
transporter-2
2B
-receptors;
indicative
low
abuse-liability
adverse
events.
Taken
together,
our
findings
identify
these
agents
as
first-in
class
leads
may
prove
useful
treatment
disorders
where
elevation
has
proven
beneficial.
