Synonym |
(Des-Tyr1)-Met-Enkephalin |
Species |
Human |
ProteinAccession |
P01210 |
Purity |
Greater than 98% |
EndotoxinLevel |
Less than 1 EU/ug |
BiologicalActivity |
Fully biologically active when compared to standard. |
ExpressionSystem |
E. coli |
FusionTag |
None |
PredictedMolecularMass |
2745 Da |
Formulation |
Lyophilized from a 0.2 µm filtered solution in Acetonitrile and TFA |
Reconstitution |
Centrifuge the vial prior to opening. Reconstitute in sterile distilled water or aqueous buffer
containing 0.1% BSA to a concentration of 0.1-1.0 mg/mL. |
Storage&Stability |
The lyophilized protein is stable for up to 1 year from date of receipt at -20°C. Upon
reconstitution, store at 4°C for up to 1 month or in working aliquots at -20°C to -80°C. |
FAQ
How does (Des-Tyr1)-Met-Enkephalin work in the human body, and what are its potential
applications?
(Des-Tyr1)-Met-Enkephalin primarily functions as an endorphin, which means it acts
as a neurotransmitter influencing the brain and the nervous system. Endorphins like
(Des-Tyr1)-Met-Enkephalin are known for their ability to influence pain perception, elevate mood, and
modulate the immune response. The molecule is a modified version of the naturally occurring enkephalins,
which bind to the opioid receptors in the brain, specifically the delta and mu subtypes. When these
receptors are activated, they can inhibit the release of neurotransmitters such as substance P, which is
involved in transmitting pain signals to the brain. This provides a pain-relieving effect similar to
that of morphine but without as many of the side effects or risks associated with opioid
drugs.
One of the potential applications of (Des-Tyr1)-Met-Enkephalin is in pain management,
especially in scenarios where traditional painkillers are either ineffective or pose a significant risk
of addiction and side effects. Given the global crisis surrounding opioid addiction and the need for
alternative pain management solutions, (Des-Tyr1)-Met-Enkephalin could represent a viable option for
patients struggling with chronic pain. Furthermore, its role in mood regulation opens up potential
therapeutic applications in psychological and psychiatric contexts, such as the treatment of depression
and anxiety disorders.
Research has also suggested that (Des-Tyr1)-Met-Enkephalin can modulate
the immune system, potentially enhancing its functioning. This immunomodulatory effect offers
possibilities for its use in treating conditions where the immune system needs to be regulated or
bolstered, such as in autoimmune diseases or certain types of cancer. The compound’s ability to promote
the release of natural killer cells and cytotoxic T-cells offers promising avenues for research in
cancer therapy, where the goal is often to enhance the body's natural ability to fight cancer
cells.
Moreover, there are studies exploring (Des-Tyr1)-Met-Enkephalin’s potential
neuroprotective properties, indicating possible implications for neurodegenerative diseases such as
Alzheimer's and Parkinson's. Given that these diseases involve the degradation of neurological function
over time, influencing pathways that can protect neurons or reduce inflammation could contribute
significantly to treatment strategies. Research is still ongoing to fully understand all the pathways
impacted by (Des-Tyr1)-Met-Enkephalin and to develop safe and effective therapeutic applications, which
might one day lead to groundbreaking treatments for both somatic and neuropsychological
conditions.
What are the potential side effects or risks associated with the use of
(Des-Tyr1)-Met-Enkephalin?
(Des-Tyr1)-Met-Enkephalin, being a peptide involved in the regulation
of pain and mood, is primarily known for its relatively safer profile compared to traditional opioid
drugs. However, it’s crucial to acknowledge that despite its promising qualities, there may be potential
side effects and risks associated with its usage. Understanding these risks is vital for researchers and
clinicians who are exploring its therapeutic applications.
One of the primary concerns with any
compound interacting with opioid receptors is the risk of developing tolerance, dependency, or
addiction. While (Des-Tyr1)-Met-Enkephalin is generally regarded as having a lower propensity for these
issues compared to more potent opioid compounds, long-term use or high doses could potentially lead to
such risks. The risk of dependency largely stems from the body’s adaptation to the presence of the
peptide, which might result in decreased efficacy over time and a consequential increase in dose
requirements.
Another potential side effect is the modulation of the central nervous system.
Because it interacts with brain pathways that influence mood, users of (Des-Tyr1)-Met-Enkephalin might
experience alterations in emotional states or cognitive function. This can be particularly concerning in
individuals who already have mood disorders or cognitive impairments, as the peptide’s use could
exacerbate these conditions or interact with existing medications in unforeseen ways.
Gastrointestinal issues are a known side effect of most compounds that affect the opioid
receptors. Nausea, vomiting, and constipation are possible side effects when the digestive system is
affected. Although these effects are anticipated to be mild with enkephalin analogues, individual
responses can vary widely.
Additionally, due to its immunomodulatory effects, there is a
potential risk of either overstimulating or suppressing the immune response. An overstimulated immune
system can potentially result in increased inflammation, whereas immune suppression might increase
susceptibility to infections. The precise effects can vary based on individual differences in immune
competence and other underlying health conditions.
Lastly, any immunomodulation or involvement
with pain pathways creates the risk of unintended effects on chronic conditions. For example, in
autoimmune diseases, carefully balancing immune modulation is critical to ensure that the disease does
not worsen due to an improperly activated or suppressed immune response. Furthermore, chronic pain
conditions that involve complex interactions between neuroimmune systems might present unforeseen
challenges when treated with such compounds.
While (Des-Tyr1)-Met-Enkephalin holds immense
promise and generally has a favorable safety profile, comprehensive clinical trials and additional
research are necessary to fully characterize its safety, develop precise dosing guidelines, and mitigate
any risks associated with its long-term or widespread use. This ensures that its deployment in clinical
settings maximizes benefit without undue harm.
How does (Des-Tyr1)-Met-Enkephalin compare to
traditional opioid analgesics in terms of efficacy and safety?
(Des-Tyr1)-Met-Enkephalin
represents a class of compounds known as enkephalins, which are natural peptides that mimic certain
actions of the body's own endorphins. Their primary allure is their potential to provide analgesic, or
pain-relieving effects, without the pronounced risks associated with traditional opioid medications,
which are often used to manage moderate to severe pain. Understanding how (Des-Tyr1)-Met-Enkephalin
compares to traditional opioid analgesics demands an exploration of both its efficacy in pain relief and
its safety profile, especially given the current opioid epidemic.
In terms of efficacy,
(Des-Tyr1)-Met-Enkephalin functions by binding to the same opioid receptors that traditional opioids
target, specifically the delta and mu receptors located in the central nervous system. These receptors,
when activated, are responsible for the reduction of pain signals and the subsequent perception of pain.
Studies suggest that while (Des-Tyr1)-Met-Enkephalin is effective in reducing pain, it may not achieve
the same level of immediate or intense pain relief that some stronger opioids like morphine can provide.
However, its analgesic capacity is still significant enough, making it a potential alternative or
adjunct in pain management, particularly for individuals who cannot tolerate stronger opioids or for
those who require long-term pain management solutions.
On the safety front,
(Des-Tyr1)-Met-Enkephalin is considered to be significantly safer when compared to traditional opioids.
Traditional opioids are infamous for their high risk of addiction and the development of tolerance and
dependence. In contrast, (Des-Tyr1)-Met-Enkephalin is expected to have a reduced likelihood of these
side effects. The peptide’s action tends to be more targeted and possibly results in fewer changes in
receptor density or neuronal plasticity, which are often responsible for tolerance and dependence with
chronic opioid use.
Furthermore, traditional opioids are associated with several severe side
effects, including respiratory depression, severe constipation, sedation, and the risk of overdose,
which can be life-threatening. (Des-Tyr1)-Met-Enkephalin, due to its different pharmacological profile
and the body's capacity to break down peptides more efficiently, shows a reduced risk for these critical
side effects. This safety profile enhances its potential as a safer pain management option, particularly
for vulnerable populations, such as the elderly or those with compromised respiratory
systems.
Nonetheless, while its improved safety profile is promising, caution is still advised.
The effects of any opioid receptor agonist on individual physiology can vary, and long-term impacts
still require thorough study. Although (Des-Tyr1)-Met-Enkephalin offers many potential benefits over
traditional opioids, clinical trials are essential to fully establish its efficacy relative to its
safety in diverse patient populations. Ultimately, as we search for safer and more effective solutions
for pain management, (Des-Tyr1)-Met-Enkephalin illustrates the innovative potential of peptides as a
class of therapeutics that might reduce dependency on conventional opioids, thus providing a crucial
addition to pain management strategies.
What kind of research has been conducted on
(Des-Tyr1)-Met-Enkephalin, and what are the results?
Research into (Des-Tyr1)-Met-Enkephalin has
been conducted across various domains, focusing on its pharmacological properties and potential
therapeutic applications. Such research, stretching over several decades, has unearthed valuable
insights into how this endorphin analogue functions within biological systems.
Initially, studies
on (Des-Tyr1)-Met-Enkephalin concentrated on its basic pharmacological effects, particularly its
affinity for opioid receptors and its efficacy as an analgesic. Early research demonstrated that
(Des-Tyr1)-Met-Enkephalin has a strong affinity for the delta and mu opioid receptors, similar to other
enkephalins and natural endorphins. These findings supported its analgesic potential, providing a
scientific basis for its development as a pain management solution. In experimental models,
(Des-Tyr1)-Met-Enkephalin successfully alleviated various pain types, which helped establish its
fundamental efficacy.
As research progressed, animal studies provided a more comprehensive
picture of its in vivo effects. These studies revealed that (Des-Tyr1)-Met-Enkephalin can modulate pain
perception pathways effectively, showcasing longer duration pain relief with fewer side effects than
traditional opioid compounds. However, it was noted that while its analgesic effects were promising,
they were modest compared to more potent opioid medications like morphine, albeit with a markedly safer
profile.
Beyond pain management, research began to explore (Des-Tyr1)-Met-Enkephalin's broader
biological impacts. Its potential role in regulating mood led researchers to investigate its effects on
conditions such as depression and anxiety. Initial findings suggested that through its action on
endogenous opioid systems, it could play a role in elevating mood and reducing symptoms of anxiety. This
opened the door to further studies examining its potential as a therapeutically relevant agent in
psychological conditions.
Another significant area of investigation has been its immunomodulatory
effects. By interacting with the immune system, (Des-Tyr1)-Met-Enkephalin could potentially bolster
immune responses or modulate them in conditions such as cancer or autoimmune diseases. Early-stage
research has indicated that the peptide may promote immune surveillance by enhancing the activity of
natural killer cells and cytotoxic lymphocytes. However, while preliminary results are promising, more
extensive, controlled human clinical trials are needed to fully ascertain its potential in
immunotherapy.
Further research has also looked into its neuroprotective capabilities. Interest
in using (Des-Tyr1)-Met-Enkephalin for neurodegenerative diseases arose from its ability to cross the
blood-brain barrier and impact neuronal health positively. Studies suggested its potential in reducing
neuroinflammation and possibly protecting neural networks from age-related degeneration. Yet, despite
substantial preclinical success, transitioning these applications into clinical utility requires further
detailed investigation.
Overall, research into (Des-Tyr1)-Met-Enkephalin underscores its
potential as a multifunctional peptide with applications extending beyond mere analgesia. While the
results so far are promising, they represent the preclinical and early clinical phases. Given the
complex nature of these conditions and the human body’s diverse responses, ongoing research is focused
on ensuring that these preliminary insights translate into tangible benefits in patient care. The
constant drive toward innovative therapeutic solutions means that (Des-Tyr1)-Met-Enkephalin remains a
topic of vibrant research, with the hope that it may soon provide viable alternatives in several areas
of medicine.
How is (Des-Tyr1)-Met-Enkephalin synthesized or produced, and what are the
challenges involved?
The synthesis of (Des-Tyr1)-Met-Enkephalin, like many peptides, is an
intricate process that typically involves a combination of chemical and biotechnological methods. This
reflects both the complexity of the peptide structure itself and the precision required to create a
biologically active compound.
Generally, the production of (Des-Tyr1)-Met-Enkephalin is carried
out through solid-phase peptide synthesis (SPPS), a method that has become a cornerstone technique in
peptide chemistry. SPPS involves the sequential addition of protected amino acids to a solid resin-bound
chain, building the peptide from the C-terminal to the N-terminal one residue at a time. Each amino acid
added is initially protected to prevent unwanted side reactions, which are common due to the many
reactive groups in amino acids. This protection is crucial for ensuring that the peptide chain grows in
a controlled manner, with the correct sequence and chirality.
The synthesis process also includes
careful deprotection and activation steps, which allow for the next amino acid in the sequence to couple
effectively. SPPS offers significant advantages in purity and yield, making it the go-to method for
laboratory-scale syntheses of peptides, including experimental and developmental batches for research
purposes. Moreover, SPPS supports large-scale production by automating many sequential steps, which
increases reproducibility and efficiency.
However, there are challenges inherent in peptide
synthesis, particularly for biologically active compounds such as (Des-Tyr1)-Met-Enkephalin. One primary
challenge is the accurate synthesis of peptide bonds in the correct stereochemistry. Any deviation might
result in a mixture of different isomeric forms, which could have significantly different biological
activities or none at all. Thus, maintaining high fidelity in the stereochemistry is crucial for
preserving the intended therapeutic effects of the peptide.
Purification is another significant
challenge. Peptide synthesis typically results in not only the desired peptide but also a range of
by-products, side-products, and unreacted starting materials that must be separated from the final
product. Purification usually involves techniques like high-performance liquid chromatography (HPLC),
which can effectively isolate the desired peptide but requires optimization and is
resource-intensive.
Another aspect involves the stability and storage of peptides.
(Des-Tyr1)-Met-Enkephalin, like other peptides, can be prone to degradation under certain conditions,
like exposure to light, heat, or hydrolysis. Effective lyophilization and storage methods are crucial
for maintaining its stability until it reaches its point of use.
Manufacturing
(Des-Tyr1)-Met-Enkephalin presents logistical and regulatory challenges. Large-scale production must
adhere to stringent guidelines ensuring consistency, safety, and efficacy, especially as the peptide
progresses through clinical trials and into potential therapeutic use. The production needs to align
with Good Manufacturing Practice (GMP) standards to ensure it meets the necessary safety and quality
controls required for pharmacological therapeutics.
Overall, while advances in synthesis
techniques like SPPS have greatly streamlined the production of (Des-Tyr1)-Met-Enkephalin, the intricate
nature of peptide chemistry and the necessity for high purity and stability levels continue to present
both challenges and opportunities in optimizing its production for therapeutic uses.