Taiy Chemical
(Lys7)-Dermorphin
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.
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