Synonym |
(Lys7)-Dermorphin |
Species |
Synthetic peptide |
Protein Accession |
NA |
Purity |
≥ 95% |
Endotoxin Level |
< 1.0 EU per 1 μg of the protein |
Biological Activity |
NA |
Expression System |
Chemical synthesis |
Fusion Tag |
NA |
Predicted Molecular Mass |
1094.30 Da |
Formulation |
Lyophilized from a 0.2 μm filtered solution of 20% acetonitrile and 0.1% TFA |
Reconstitution |
It is recommended to reconstitute the lyophilized (Lys7)-Dermorphin in sterile 18MΩ-cm H2O not
less than 100 µg/ml, which can then be further diluted to other aqueous solutions. |
Storage & Stability |
Lyophilized (Lys7)-Dermorphin although stable at room temperature for 3 weeks, should be stored
desiccated below -18°C. Upon reconstitution (Lys7)-Dermorphin should be stored at 4°C between
2-7 days and for future use below -18°C. For long term storage it is recommended to add a
carrier protein (0.1% HSA or BSA). Please prevent freeze-thaw cycles. |
FAQ
What is (Lys7)-Dermorphin, and how does it work in the body?
(Lys7)-Dermorphin is a synthetic
peptide analog derived from dermorphin, a naturally occurring opioid peptide isolated from the skin of
certain species of South American frogs. Dermorphin itself is known for its high affinity and
selectivity for the mu-opioid receptor, which is a critical target for managing pain and producing
analgesic effects. (Lys7)-Dermorphin acts by binding to these receptors with high specificity, resulting
in potent analgesic effects. The peptide specifically acts on the central nervous system, where it
modulates the perception of pain by altering neurotransmission. By mimicking the actions of endorphins,
which are the body’s natural pain relievers, (Lys7)-Dermorphin can provide significant analgesic
properties.
The mechanism through which (Lys7)-Dermorphin exerts its effects involves the
inhibition of adenylate cyclase activity, leading to a decrease in neuronal excitability and
neurotransmitter release. This action results in a reduction of pain signals being transmitted through
the nervous system. Additionally, its high lipid solubility allows it to cross the blood-brain barrier
efficiently, ensuring rapid onset of action. This characteristic is particularly advantageous for
managing acute pain episodes where timely intervention is critical.
Furthermore,
(Lys7)-Dermorphin also impacts emotional and psychological aspects of pain. By engaging the mu-opioid
receptors within the limbic system, it influences emotional states, which can enhance subjective
feelings of well-being while reducing stress and anxiety associated with pain. These combined actions
make (Lys7)-Dermorphin a potent tool for pain management in various clinical scenarios.
However,
like all opioid agonists, the prolonged use of (Lys7)-Dermorphin could lead to tolerance, where
increasing doses may be required to achieve the same therapeutic effect, and potentially to dependence.
Therefore, understanding its pharmacokinetics and pharmaco-dynamics is crucial in optimizing its
therapeutic use while minimizing potential adverse effects. Researchers are continuing to explore its
efficacy and safety profile in an effort to expand therapeutic options for conditions requiring
effective pain management with a potentially lower risk of side effects compared to traditional
opioids.
What are the potential therapeutic applications of (Lys7)-Dermorphin?
The potential
therapeutic applications of (Lys7)-Dermorphin are diverse, primarily owing to its strong analgesic
properties and mechanism of action that involves the mu-opioid receptor. One of the primary applications
is in the management of acute and chronic pain. For conditions such as post-operative pain,
cancer-related pain, or severe injury, (Lys7)-Dermorphin offers a potent alternative to traditional
opioid medications. Due to its high selectivity for mu-opioid receptors and its ability to provide rapid
pain relief, it can be especially beneficial in acute pain situations where immediate relief is
required.
Another potential application is in neuropathic pain, a chronic pain condition
resulting from nerve damage. This form of pain is notoriously difficult to treat with standard pain
medications. By targeting specific pathways related to pain transmission and modulation,
(Lys7)-Dermorphin may address some neurobiological aspects that are resistant to other treatments. This
has significant implications for improving the quality of life for patients with conditions affecting
the nervous system such as multiple sclerosis or diabetic neuropathy.
Beyond pain management,
researchers are investigating the use of (Lys7)-Dermorphin in psychological disorders due to its action
on the limbic system. Conditions such as anxiety and depression are often co-morbid in patients with
chronic pain, and traditional treatments sometimes fail to deliver comprehensive relief. By positively
affecting mood and emotional response, (Lys7)-Dermorphin holds potential as a complementary treatment to
enhance overall psychological wellness in these individuals.
Additionally, (Lys7)-Dermorphin’s
efficacy in reducing severe migraine episodes is being explored. Migraines present a complex interplay
of neurological and vascular phenomena, and existing treatments are not always effective for all
patients. The unique mechanism of (Lys7)-Dermorphin may offer a new avenue for mitigating such
debilitating episodes, heralding a promising future in neuropharmacology.
It is important to
acknowledge that while (Lys7)-Dermorphin presents numerous potential therapeutic benefits, thorough
clinical evaluations and trials are essential to fully understand its safety profile and efficacy in
different patient populations. Its potential for side effects, tolerance, and dependence necessitates
careful consideration of dosing regimens and patient selection to maximize benefits while minimizing
risks.
How does (Lys7)-Dermorphin compare to other opioid analgesics?
(Lys7)-Dermorphin
stands out among opioid analgesics due to its distinctive properties and mechanism of action. Compared
to traditional opioids like morphine, oxycodone, and fentanyl, (Lys7)-Dermorphin offers several
advantages that could potentially translate into superior therapeutic outcomes for pain management. One
notable feature is its high potency and efficacy at much lower doses, which could reduce the risk of
side effects typically associated with higher doses of opioids. This makes it particularly promising for
patients who are sensitive to opioids or who experience adverse reactions at lower
thresholds.
The selectivity of (Lys7)-Dermorphin for the mu-opioid receptor is another
significant aspect that distinguishes it from other opioids. Most conventional opioids have a broader
receptor target profile, often interacting with kappa and delta opioid receptors, which can lead to
undesirable effects such as dysphoria and hallucinations. By specifically targeting the mu-opioid
receptor with greater affinity, (Lys7)-Dermorphin may produce fewer of these non-analgesic side effects,
resulting in a better-tolerated treatment. Such precision in receptor targeting could potentially
mitigate common opioid-induced adverse effects like sedation, nausea, and constipation.
Moreover,
(Lys7)-Dermorphin may also offer a more rapid onset of analgesia. This is intrinsic to its ability to
cross the blood-brain barrier efficiently, a feature that not all opioids possess to the same extent. In
scenarios where immediate pain relief is crucial, such as acute injury or post-operative settings, this
rapid action could improve patient outcomes and satisfaction significantly.
While there are
promising aspects of (Lys7)-Dermorphin, it is crucial to consider that any opioid agonist, including
this peptide, carries inherent risks of addiction, tolerance, and physical dependence. In comparison to
other opioids, the development of these conditions may be attenuated due to the lower dosage
requirements, but they remain possible. Therefore, its use would necessitate careful monitoring and
regulation, similar to other opioids, to avoid potential misuse and abuse.
In sum, while
(Lys7)-Dermorphin presents potential advantages over traditional opioids, more extensive research and
controlled clinical trials are necessary to confirm its benefits and establish comprehensive safety
guidelines. Its eventual role in pain management will depend on striking a balance between effective
analgesia and minimizing the risks associated with opioid therapy.
What research is currently
being conducted on (Lys7)-Dermorphin?
Research on (Lys7)-Dermorphin is ongoing, focusing on several
key areas that aim to elucidate its pharmacological properties, therapeutic potential, and safety
profile. Scientists and medical researchers are particularly interested in its highly selective binding
to the mu-opioid receptor and its implications for pain management. One prominent area of research is
understanding the precise molecular interactions that underlie its potent analgesic effects. Structural
biology studies are employed to map the binding sites and determine how alterations in peptide structure
could impact affinity and efficacy. These findings can pave the way for designing analogs with optimized
characteristics for therapeutic use.
In addition to structural and interaction studies,
preclinical experiments are conducted to assess the pharmacokinetics of (Lys7)-Dermorphin. Understanding
how the peptide is absorbed, distributed, metabolized, and excreted in the body is crucial for
developing appropriate dosing regimens. These studies are complemented by in vivo efficacy and safety
evaluations in animal models that simulate various pain conditions, from neuropathic to inflammatory
pain. These models help to identify the therapeutic window of (Lys7)-Dermorphin and its potential side
effects at different doses.
Aside from its role in pain management, there is a growing interest
in exploring the broader therapeutic applications of (Lys7)-Dermorphin. For example, its potential use
in treating substance use disorders is being investigated, given that its action might modulate reward
pathways related to addiction. Research is also looking at its effects on mood and behavior to evaluate
its utility in psychiatric disorders that may benefit from opioid system modulation.
The
translation of preclinical findings to clinical settings is a significant step that entails rigorous
clinical trials. These trials aim to assess the safety and efficacy of (Lys7)-Dermorphin in diverse
patient populations while identifying any potential adverse effects. The dosage forms being explored
include both injectable and nasal formulations, which could offer flexibility in administration routes
to suit patient needs.
Overall, the research on (Lys7)-Dermorphin is both extensive and
promising, with the goal of making it a viable therapeutic option. However, the peptide is not without
its challenges. Establishing a comprehensive understanding of its long-term effects, potential for
abuse, and interaction with other medications remains a priority. Ensuring that its benefits outweigh
the risks is crucial before (Lys7)-Dermorphin can be fully integrated into clinical
practice.
What are the possible side effects associated with (Lys7)-Dermorphin?
As with any
opioid agonist, (Lys7)-Dermorphin may produce a range of side effects that are largely influenced by its
interaction with the mu-opioid receptor. One of the most prevalent side effects experienced by
individuals using opioids is sedation. The modulation of the central nervous system's activity to
diminish pain perception frequently results in a decrease in alertness and cognitive function, leading
to drowsiness or increased sleepiness. For some patients, this effect may be relatively mild, but for
others, it could impair daily activities, especially those requiring alertness, such as driving or
operating machinery.
Another common side effect is respiratory depression, a known risk
associated with opioid use. Opioids can alter normal respiratory patterns by diminishing the brain's
response to carbon dioxide levels in the blood, potentially leading to dangerously slow or shallow
breathing. This risk underscores the need for careful dosing and monitoring, particularly in populations
more vulnerable to compromised respiratory function, such as the elderly or those with pre-existing
respiratory conditions.
Nausea and vomiting are also standard side effects due to the activation
of the chemoreceptor trigger zone in the brain and changes in gastrointestinal motility. These symptoms
can affect patient compliance and overall comfort, which might require additional management strategies,
such as co-administration with antiemetic agents.
Moreover, as with other opioids, long-term or
inappropriate use of (Lys7)-Dermorphin could lead to the development of tolerance and physical
dependence. Increasing doses may be required over time to achieve the same analgesic effects,
potentially escalating the risk of side effects and complicating treatment regimens. Withdrawal symptoms
may occur if the medication is abruptly discontinued or if the body becomes accustomed to its presence
and physiological changes ensue.
Lastly, though less common, some patients might experience
adverse skin reactions, mood alterations, or dysphoria depending on individual susceptibility and the
broader interactions of (Lys7)-Dermorphin within various systems in the body.
Managing these side
effects necessitates judicious prescriber practices that tailor opioid therapy to the individual while
considering factors such as concurrent medical conditions, overall health status, and potential
interactions with other medications. As research progresses, efforts to develop strategies that mitigate
these side effects continue in order to enhance the safety profile of (Lys7)-Dermorphin while
capitalizing on its potential benefits.