Biased Opioid Receptor Agonists: Balancing Analgesic Efficacy and Side-Effect Profiles
International Journal of Molecular Sciences,
Год журнала:
2025,
Номер
26(5), С. 1862 - 1862
Опубликована: Фев. 21, 2025
Opioids
are
the
most
effective
option
for
severe
pain.
However,
it
is
well
documented
that
side
effects
associated
with
prolonged
opioid
use
significantly
constrain
dosage
in
clinical
setting.
Recently,
researchers
have
concentrated
on
development
of
biased
receptor
agonists
preferentially
activate
G
protein
signaling
pathway
over
β-arrestin
signaling.
This
approach
based
hypothesis
mediates
analgesic
effects,
whereas
implicated
adverse
effects.
Although
certain
studies
demonstrated
absence
or
inhibition
can
mitigate
incidence
recent
research
appears
to
challenge
these
earlier
findings.
In-depth
investigations
into
signal
transduction
been
conducted,
potentially
offering
novel
insights
receptors.
Consequently,
this
review
elucidates
contradictory
roles
reactions
activation.
Furthermore,
a
comparative
analysis
was
conducted
evaluate
efficacy
classic
protein-biased
agonists,
TRV130
and
PZM21,
relative
traditional
non-biased
agonist
morphine.
aims
inform
drugs
optimize
therapeutic
safety,
while
minimizing
greatest
extent
possible.
Язык: Английский
A Bibliometric and Visual Analysis of Oliceridine Research (2013–2024)
Drug Design Development and Therapy,
Год журнала:
2025,
Номер
Volume 19, С. 1305 - 1321
Опубликована: Фев. 1, 2025
To
explore
and
analyze
the
current
research
progress,
hotspots,
future
trends
in
oliceridine
using
bibliometric
methods.
We
searched
Web
of
Science
(WOS)
database
utilizing
keywords
TS
=
("oliceridine*"
OR
"TRV
130*"
"TRV-130*"
"olinvyk*"
"TRV130*"
"C22H31CIN2O2S*")
for
relevant
literature
on
from
its
inception
to
June
16,
2024.
Bibliometric
methods
were
applied,
analysis
software
such
as
VOSviewer
CiteSpace
used
visualize
publication
timeline,
authors,
countries
regions,
keywords,
sources
literature,
co-cited
documents
related
oliceridine.
Co-occurrence
aggregation
analyses
conducted,
maps
institutional
cooperation
generated.
A
total
151
articles
retrieved
included
final
analysis.
Most
published
between
2020
2021.
The
United
States
has
highest
number
publications
citations
this
field.
Molecular
structure
development
is
a
pivotal
point
Research
hotspots
diverse,
including
acute
pain,
opioid
receptors,
β-arrestin,
postoperative
therapeutic
window,
respiratory
depression,
clinical
trials,
chronic
pain.
Oliceridine,
newly
developed
analgesic,
garnered
global
interest.
USA
leading
contributor
Recent
shifted
basic
studies
practice.
Язык: Английский
Biased agonism of G protein-coupled receptors as a novel strategy for osteoarthritis therapy
Bone Research,
Год журнала:
2025,
Номер
13(1)
Опубликована: Май 12, 2025
Abstract
Osteoarthritis
(OA)
is
a
prevalent
degenerative
joint
disorder
marked
by
chronic
pain,
inflammation,
and
cartilage
loss,
with
current
treatments
limited
to
symptom
relief.
G
protein-coupled
receptors
(GPCRs)
play
pivotal
role
in
OA
progression
regulating
chondrocyte
survival,
matrix
homeostasis.
However,
their
multifaceted
signaling,
via
proteins
or
β-arrestins,
poses
challenges
for
precise
therapeutic
targeting.
Biased
agonism,
where
ligands
selectively
activate
specific
GPCR
pathways,
emerges
as
promising
approach
optimize
efficacy
reduce
side
effects.
This
review
examines
biased
signaling
OA-associated
GPCRs,
including
cannabinoid
(CB
1
,
CB
2
),
chemokine
(CCR2,
CXCR4),
protease-activated
(PAR-2),
adenosine
(A
R,
A
2A
2B
3
R),
melanocortin
(MC
MC
bradykinin
(B
prostaglandin
E
(EP-2,
EP-4),
calcium-sensing
(CaSR).
We
analyze
clinical
trials
explore
natural
products
from
Traditional
Chinese
Medicine
potential
agonists.
These
compounds,
diverse
structures
bioactivities,
offer
novel
avenues.
By
harnessing
this
underscores
the
developing
targeted,
safer
therapies
that
address
its
complex
pathology,
bridging
molecular
insights
translation.
Язык: Английский
Opioid Enantiomers: Exploring the Complex Interplay of Stereochemistry, Pharmacodynamics, and Therapeutic Potential
Journal of Medicinal Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Июнь 3, 2025
Opioids
have
been
essential
in
pain
management,
particularly
when
other
analgesics
prove
insufficient,
but
their
use
is
complicated
by
risks
of
addiction,
tolerance,
and
a
range
adverse
effects.
These
challenges
are
further
exacerbated
the
presence
opioid
enantiomers
that
interact
variety
ways
with
biological
systems.
This
Perspective
provides
comprehensive
exploration
enantiomers,
focusing
on
synthesis,
pharmacodynamics,
potential
therapeutic
applications
beyond
traditional
management.
It
highlights
complexity
synthesizing
morphine
additional
producing
less-studied
(+)-morphine.
The
also
examines
structure-activity
relationship
studies
(+)-opioid
compounds,
revealing
modulating
neuroinflammatory
responses
through
non-opioid
pathways
suggesting
new
avenues
for
conditions
like
neuropathic
drug
addiction.
Furthermore,
it
discusses
differential
safety
profiles
emphasizing
need
future
research
to
advance
precision
medicine
therapy,
ultimately
aiming
develop
safer
more
effective
management
strategies.
Язык: Английский