Pharmaceuticals,
Journal Year:
2021,
Volume and Issue:
14(12), P. 1329 - 1329
Published: Dec. 18, 2021
Marine
pharmacology
is
an
exciting
and
growing
discipline
that
blends
blue
biotechnology
natural
compound
together.
Several
sea-derived
compounds
are
approved
on
the
pharmaceutical
market
were
discovered
in
sponges,
marine
organisms
particularly
rich
bioactive
metabolites.
This
paper
was
specifically
aimed
at
reviewing
pharmacological
activities
of
extracts
or
purified
from
sponges
collected
Mediterranean
Sea,
one
most
biodiverse
habitats,
filling
gap
literature
about
research
products
this
geographical
area.
Findings
regarding
different
sponge
species
individuated,
reporting
consistent
evidence
efficacy
mainly
against
cancer,
infections,
inflammatory,
neurological
disorders.
The
sustainable
exploitation
as
sources
strongly
encouraged
to
discover
new
compounds.
Expert Opinion on Drug Delivery,
Journal Year:
2024,
Volume and Issue:
unknown, P. 1 - 16
Published: Dec. 3, 2024
Central
nervous
system
(CNS)
disorders
present
major
therapeutic
challenges
due
to
the
presence
of
blood
-
brain
barrier
(BBB)
and
disease
heterogeneity.
The
BBB
impedes
most
agents,
which
restricts
conventional
treatments.
Focused
ultrasound
(FUS)
-assisted
delivery
offers
a
novel
solution
by
temporarily
disrupting
thereby
enhancing
drug
CNS.
Clinical Pharmacology & Therapeutics,
Journal Year:
2022,
Volume and Issue:
111(4), P. 799 - 806
Published: Jan. 16, 2022
Global
regulatory
agencies
have
transformed
their
approach
to
approvals
in
processes
for
formal
review
of
the
safety
and
efficacy
new
drugs.
Opportunities
innovation
expanded
because
coronavirus
disease
2019
(COVID-19)
pandemic.
Several
regulatory-led
initiatives
progressed
rapidly
during
past
year,
including
patient-focused
drug
development,
model-informed
real-world
evidence,
complex
innovative
trial
designs.
Collectively,
these
accelerated
rate
approvals.
Despite
demands
focus
on
urgent
needs
imposed
by
COVID-19
pandemic,
number
over
particularly
rare
diseases,
has
outpaced
expectations.
Advancing
therapeutics
nervous
system
disorders
requires
adaptive
strategies
that
align
with
rapid
developments
field.
Three
relentlessly
progressive
amyotrophic
lateral
sclerosis,
Duchenne
muscular
dystrophy,
Parkinson's
are
need
treatments.
Herein,
we
propose
initiatives,
designs
development
accelerate
clinical
conduct
while
meeting
critical
requirements
therapeutic
approval.
Fundamental and Clinical Pharmacology,
Journal Year:
2023,
Volume and Issue:
38(2), P. 290 - 306
Published: Oct. 16, 2023
Abstract
Background
Anxiety
disorders
represent
the
complex
interaction
between
biological,
psychological,
temperamental,
and
environmental
factors;
drugs
available
to
treat
anxiety
such
as
benzodiazepines
(BZDs)
are
associated
with
several
unwanted
side
effects.
Although
there
useful
treatments,
is
still
a
need
for
more
effective
anxiolytics
better
safety
profiles
than
BZDs.
Chalcones
or
1,3‐diphenyl‐2‐proper‐1‐ones
can
be
an
alternative
since
this
class
of
compounds
has
shown
therapeutic
potential
mainly
due
interactions
GABA
A
receptors
serotonergic
system.
Objectives
This
study
evaluated
anxiolytic
chalcone
(
E
)‐3‐(4‐(dimethylamino)phenyl)‐1‐(2‐hydroxyphenyl)prop‐2‐en‐1‐one
(C2OHPDA)
in
adult
zebrafish
Danio
rerio
)
(ZFa).
Methods
Each
animal
n
=
6/group)
was
treated
intraperitoneally
(i.p.;
20
μL)
(4,
20,
40
mg/kg)
vehicle
(DMSO
3%;
μL),
being
submitted
tests
locomotor
activity
96‐h
acute
toxicity.
The
light/dark
test
also
performed,
mechanism
(5‐HT)
through
antagonists
5‐HTR
1
,
2A/2C
3A/3B
receptors.
It
investigated
prediction
chalcone's
position
preferential
orientation
concerning
its
receptor,
well
pharmacokinetic
parameters
(ADMET)
involved
process
after
administration.
Results
As
result,
C2OHPDA
not
toxic
reduced
ZFa.
Furthermore,
demonstrated
effect
on
central
nervous
system
(CNS),
mediated
by
system,
action
5‐HT
2A
R
3A
confirmed
molecular
docking
study,
affinity
energy
observed
−8.7
−9.1
kcal/mol,
respectively.
Conclusion
Thus,
adds
new
evidence
highlights
that
potentially
used
develop
properties.
Pharmaceutical Research,
Journal Year:
2020,
Volume and Issue:
37(8)
Published: Aug. 1, 2020
Abstract
Purpose
TAK-831
is
a
highly
selective
and
potent
inhibitor
of
D-amino
acid
oxidase
(DAAO)
currently
under
clinical
development
for
schizophrenia.
In
this
study,
mechanistic
multilayer
quantitative
model
that
parsimoniously
connects
pharmacokinetics
(PK),
target
occupancy
(TO)
D-serine
concentrations
as
pharmacodynamic
(PD)
readout
was
established
in
mice.
Methods
PK,
TO
PD
time-profiles
were
obtained
mice
analyzed
by
binding
kinetics
connected
with
an
indirect
response
step
wise
fashion.
Brain
distribution
investigated
to
elucidate
possible
mechanism
driving
the
hysteresis
between
PK
TO.
Results
The
observed
nonlinear
PK/TO/PD
relationship
well
captured
modeling
framework
within
wide
dose
range
Remarkably
different
brain
reference
regions,
suggesting
target-mediated
slow
rather
than
penetration
through
blood
barrier
caused
distinct
Conclusion
A
concentration-
time-dependent
accounting
rate-determining
process.
will
provide
means
biomarker-assisted
multiple
central
nervous
system
indications.
Pharmaceuticals,
Journal Year:
2021,
Volume and Issue:
14(12), P. 1329 - 1329
Published: Dec. 18, 2021
Marine
pharmacology
is
an
exciting
and
growing
discipline
that
blends
blue
biotechnology
natural
compound
together.
Several
sea-derived
compounds
are
approved
on
the
pharmaceutical
market
were
discovered
in
sponges,
marine
organisms
particularly
rich
bioactive
metabolites.
This
paper
was
specifically
aimed
at
reviewing
pharmacological
activities
of
extracts
or
purified
from
sponges
collected
Mediterranean
Sea,
one
most
biodiverse
habitats,
filling
gap
literature
about
research
products
this
geographical
area.
Findings
regarding
different
sponge
species
individuated,
reporting
consistent
evidence
efficacy
mainly
against
cancer,
infections,
inflammatory,
neurological
disorders.
The
sustainable
exploitation
as
sources
strongly
encouraged
to
discover
new
compounds.
