Synonym |
(Phe7)-Dynorphin A (1-7) |
Species |
Human |
Protein Accession |
P01210 |
Purity |
Greater than 95% |
Endotoxin Level |
Less than 1 EU/µg |
Biological Activity |
Not specified |
Expression System |
Chemical synthesis |
Fusion Tag |
None |
Predicted Molecular Mass |
876.03 Da |
Formulation |
Lyophilized powder |
Reconstitution |
Reconstitute in water to a concentration of 0.1-1.0 mg/ml |
Storage & Stability |
Store lyophilized protein at -20°C. Aliquot reconstituted protein and store at -80°C for
long-term storage. |
FAQ
What is (Phe7)-Dynorphin A (1-7) and how does it function in the body?
(Phe7)-Dynorphin A (1-7) is a
synthetic peptide that is derived from the endogenous opioid peptide called dynorphin A. It primarily
belongs to a class of compounds known as kappa opioid receptor agonists. Dynorphins are a type of opioid
peptide produced naturally within the body. They are part of the body’s internal pain-modulating system,
interacting with opioid receptors found in the central and peripheral nervous systems, notably the
kappa-opioid receptors. These interactions are crucial for modulating pain, stress, and mood.
The
primary function of (Phe7)-Dynorphin A (1-7) in the body is to interact specifically with kappa-opioid
receptors, which are widely distributed throughout the brain, spinal cord, and peripheral nerves. Upon
activating these receptors, the peptide can induce a range of physiological responses. Notably, the
kappa-opioid system is involved in pain modulation, mood regulation, and stress response. Kappa opioid
receptor activation has been shown to produce analgesic effects, reduce stress-induced emotional states,
and alter mood. However, unlike other opioid receptors, activation of kappa receptors by dynorphins
tends to produce dysphoric and sedative effects rather than euphoria, which is commonly associated with
mu-opioid receptor activation by peptides like endorphins.
Moreover, recent studies have proposed
that (Phe7)-Dynorphin A (1-7) may play a role in neuroprotection and inflammatory response modulation.
There is ongoing research into its potential for treating conditions related to neurodegeneration and
chronic inflammation. The peptide's ability to modulate inflammatory pathways and potentially reduce
oxidative stress at a cellular level provides a promising potential therapeutic approach for managing
neurodegenerative diseases such as Alzheimer's or Parkinson's, though extensive human trials and further
evidence are needed to substantiate these effects. Understanding (Phe7)-Dynorphin A (1-7) involves
appreciating its biological activity and therapeutic potential, all of which hinge on its specific
receptor interactions and their subsequent physiological responses.
Are there any documented
benefits of (Phe7)-Dynorphin A (1-7) in scientific research?
Numerous scientific studies have
explored the potential benefits of (Phe7)-Dynorphin A (1-7), albeit much of the research is still in
preliminary stages and often conducted on animal models. One notable area of interest is its potential
analgesic properties. The peptide’s main activity involves modulation of pain pathways via kappa-opioid
receptor activation. Studies have documented that activation of these receptors by (Phe7)-Dynorphin A
(1-7) can decrease pain perception, showcasing its potential as a target for pain management therapies.
These findings are particularly valuable in circumstances where traditional pain medications, such as
nonsteroidal anti-inflammatory drugs or mu-opioid receptor agonists, might be less effective or produce
undesirable side effects.
In addition to pain modulation, another key area where (Phe7)-Dynorphin
A (1-7) has shown potential benefits is in mood and stress regulation. Animal studies have suggested
that it can influence emotional responses, providing stress relief and reducing anxiety-like symptoms.
While kappa-opioid receptor activation is traditionally associated with dysphoria, the derivative
modifications in (Phe7)-Dynorphin A (1-7) are hypothesized to mitigate this effect, offering a more
balanced mood-regulating profile. This modulation of mood and stress response implies potential
applications in treating mood disorders or stress-related conditions.
Furthermore, research
interest is growing in the area of neuroprotection, with some studies indicating that (Phe7)-Dynorphin A
(1-7) might aid in protecting neuronal cells against damage. Its potential neuroprotective effects are
attributed to its influence on inflammatory responses and neuronal oxidative stress. By modulating these
biological pathways, (Phe7)-Dynorphin A (1-7) may help in slowing the progression of neurodegenerative
diseases. Although animal and in vitro studies provide promising insights, translation into human
clinical benefits requires more rigorous trials. The documented benefits of (Phe7)-Dynorphin A (1-7) in
scientific research underscore its promising role in medical science, highlighting the need for
continued investigation to fully understand its therapeutic applications and efficacy in
humans.
What are the potential side effects or risks associated with (Phe7)-Dynorphin A (1-7)
use?
As with any pharmacological agent, (Phe7)-Dynorphin A (1-7) carries potential side effects and
risks, which require careful consideration, particularly given its activity at the kappa-opioid
receptors. A well-documented effect of kappa-opioid receptor agonists is the induction of dysphoria,
which can manifest as a general state of unease, dissatisfaction, or mood disturbance. This dysphoric
effect can potentially counteract any mood stabilization benefits if not properly managed or if
experienced to a significant degree.
Another potential side effect involves sedative effects, as
opioids, in general, can lead to sedation and a decrease in alertness. This could potentially impair a
person's ability to perform tasks that require full cognitive function and focus. While sedative effects
are dose-dependent, they are an important consideration when evaluating the safety profile of
(Phe7)-Dynorphin A (1-7). It is crucial to determine optimal dosing that maximizes therapeutic benefits
while minimizing sedative side effects.
Opioid peptides, including (Phe7)-Dynorphin A (1-7), may
also pose risks related to altered sensory perception and motor functions, as they heavily influence
central nervous system activities. Another line of concern is the potential for inducing
gastrointestinal disturbances, as opioids are known to impact gut motility, possibly leading to
constipation or other digestive irregularities.
Although evidence on tolerance, dependency, and
addiction potential for (Phe7)-Dynorphin A (1-7) specifically is limited, caution is warranted due to
its mechanism of action akin to other opioid compounds. Any substance modulating opioid receptors incurs
the risk of tolerance buildup, necessitating increased doses over time to achieve the same therapeutic
effect.
Furthermore, due to the peptide’s influence on inflammatory and immune responses, there
could be unanticipated effects when administered for chronic conditions. Human studies are crucial to
painting a complete picture of these risks, as most available evidence comes from animal models.
Therefore, safety assessments in human trials are necessary to confirm these observations and ensure
that the risk profile is understood and manageable for therapeutic contexts. Engaging in a cautious
approach with comprehensive monitoring will be key in assessing the safety and managing any potential
side effects associated with (Phe7)-Dynorphin A (1-7) use.
How does (Phe7)-Dynorphin A (1-7)
compare to other opioid peptides in therapeutic application?
(Phe7)-Dynorphin A (1-7), as a
kappa-opioid receptor agonist, presents a distinct profile compared to other opioid peptides, such as
those targeting the mu-opioid receptors like endorphins. This difference offers both unique advantages
and challenges in therapeutic applications. A distinguishing aspect of (Phe7)-Dynorphin A (1-7) lies in
its receptor specificity, primarily acting on the kappa-opioid receptors, which does not typically lead
to the intense euphoria often associated with mu-opioid receptor activation. This lack of euphoria
reduces the potential for abuse and addiction, making it a more promising candidate for therapeutic use
where the risk of dependency is a concern.
In terms of analgesic properties, (Phe7)-Dynorphin A
(1-7) provides an alternative pathway for pain modulation without the significant addiction liability
seen in mu-opioid receptor agonists like morphine. However, the use of kappa receptor agonists
traditionally comes with the challenge of managing dysphoric effects, a side effect not central to
mu-receptor agonists. This side effect often requires careful management and individualized dosing to
ensure that the therapeutic benefit outweighs the negative mood effects.
Compared to other opioid
peptides that might cross the blood-brain barrier more freely, (Phe7)-Dynorphin A (1-7) could offer a
level of neuroprotection, as evidenced by studies evaluating its potential to modulate neuroinflammatory
conditions. Its focus on kappa receptors could make it suitable for neurodegenerative disease models
where inflammation is a component. It further differentiates itself in neurological applications due to
its reduced euphoric effect, making long-term management more feasible within clinical settings that
balance efficacy with patient compliance and overall quality of life.
(Phe7)-Dynorphin A (1-7)'s
sedative effects also need comparison with other opioid peptides. While some level of sedation is a
common trait among opioids, degree and manageability differ. The peptide's sedative profile might be
akin to that of other opioid-derived agents but requires optimization in clinical settings to ensure
patient safety and functional activity are preserved.
Ultimately, (Phe7)-Dynorphin A (1-7) offers
distinct advantages and disadvantages in therapeutic applications compared to other opioid peptides,
necessitating a strategic approach in its development and use. Its unique receptor profile offers
specific advantages in certain therapeutic areas, like pain management and neurodegenerative conditions,
where opioid dependency and cognitive side effects are serious concerns. Understanding and leveraging
its uniqueness in receptor interaction, side effect management, and therapeutic targeting will be key in
differentiating its clinical applications among opioid peptide therapies.
What are future
research directions for (Phe7)-Dynorphin A (1-7)?
Research into (Phe7)-Dynorphin A (1-7) is still
evolving, and several promising directions are being pursued to better understand and exploit its
therapeutic potential. One of the primary avenues of research involves delineating its precise
mechanisms of action within the central nervous system. Comprehensive mechanism studies can aid in
understanding the full spectrum of kappa opioid receptor-mediated activities, particularly how these
might be modulated to enhance therapeutic benefits while minimizing side effects such as dysphoria and
sedation.
Additionally, research is focused on optimizing the delivery mechanisms of
(Phe7)-Dynorphin A (1-7). Due to the peptide’s size and structural properties, exploring advanced
delivery systems such as nano-formulations or conjugated molecules could improve its stability,
bioavailability, and targeted effects. Enhancing the pharmacokinetic profile ensures efficient crossing
of physiological barriers like the blood-brain barrier, maximizing central nervous system concentration
with minimal peripheral side effects.
Further investigations are also keen on exploring its
impact on neuroinflammation and neurodegenerative diseases. Current studies are evaluating the
hypothesis that by modulating kappa-opioid receptors, (Phe7)-Dynorphin A (1-7) could counteract
inflammatory and oxidative stress pathways involved in conditions like Alzheimer’s and Parkinson’s
diseases. These studies involve not only animal models but also translational clinical trials to confirm
efficacy and safety in humans.
Moreover, given the opioid crisis and the search for
non-addictive pain relief alternatives, significant research efforts are being directed at understanding
how modifications to (Phe7)-Dynorphin A (1-7) or its analogs could optimize pain relief without the
dependency risks associated with classical opioids. This entails structure-activity relationship studies
to develop analogs with improved safety and efficacy profiles tailored for chronic pain
management.
Lastly, expanding research into combination therapies where (Phe7)-Dynorphin A (1-7)
is used alongside other therapeutic agents could open new treatment paradigms. Investigating synergistic
effects in combination with other peptides or pharmacological agents might reveal enhanced therapeutic
outcomes for complex conditions.
Future research directions for (Phe7)-Dynorphin A (1-7) thus
focus on refining its therapeutic profile, optimizing delivery mechanisms, expanding its application to
inflammatory and neurodegenerative diseases, and ensuring that its use remains safe and effective. The
next decade of research is likely to yield crucial insights that will inform clinical applications and
potentially broaden its use across multiple therapeutic domains.