Synonym |
(D-Ala2)-Leu-enkephalin amide |
Species |
Human |
Protein Accession |
P01201 |
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 |
586.71 Da |
Formulation |
Supplied as a lyophilized powder |
Reconstitution |
Reconstitute in water to a concentration of 0.1-1.0 mg/mL |
Storage & Stability |
Store at -20°C. Stable for up to 3 years |
FAQ
What is (D-Ala2)-Leu-Enkephalin amide, and how does it work in the body?
(D-Ala2)-Leu-Enkephalin
amide is a synthetic opioid peptide, which is a derivative of one of the naturally occurring enkephalins
in the body. Enkephalins are part of a broader group of molecules called endorphins, which are
neurotransmitters responsible for mitigating pain and stress. More specifically, enkephalins interact
with the opioid receptors in the brain and nervous system, namely the mu, delta, and kappa receptors,
which influence various physiological responses, including pain modulation, mood regulation, and immune
functions.
The modification in (D-Ala2)-Leu-Enkephalin amide, specifically the substitution of
the second amino acid with D-Alanine (D-Ala2), enhances its stability and affinity for the opioid
receptors, especially the delta receptors. This change in molecular structure prevents the rapid
degradation of the peptide by enzymes in the body, ensuring that it remains active for a longer
duration, thus providing more sustained effects. This characteristic is a critical factor in research
and therapeutic applications, as it allows for more potent and longer-lasting pain relief compared to
its naturally occurring counterparts.
Once administered, (D-Ala2)-Leu-Enkephalin amide mimics the
action of endogenous opioids by binding to the opioid receptors, which triggers a series of
intracellular events leading to the reduction of neurotransmitter release responsible for pain pathways.
This action contributes to the peptide's potential as an analgesic or painkiller. Additionally, by
interacting with delta receptors, this peptide offers promising effects beyond analgesia, such as mood
enhancement and potential protective effects against neurological disorders.
The scientific
exploration of (D-Ala2)-Leu-Enkephalin amide is still ongoing, and it is studied for its role in pain
management and its therapeutic potential in treating various neuropathological conditions. Enthusiasm
surrounds its application in clinical settings, given its enhanced receptor interaction profile.
However, despite its promise, like other opioids, the potential for side effects and the need for
precise dosing warrants a cautious and well-monitored approach in its application.
What potential
benefits does (D-Ala2)-Leu-Enkephalin amide offer for pain management?
In the realm of pain
management, (D-Ala2)-Leu-Enkephalin amide offers a range of potential benefits, primarily driven by its
enhanced ability to bind to the body's opioid receptors due to its molecular modification. This peptide
presents a promising option for individuals seeking alternative analgesic treatments, especially those
who might not respond well to traditional opioid therapies.
One significant advantage of
(D-Ala2)-Leu-Enkephalin amide is its increased specificity and affinity towards delta opioid receptors,
which translates into effective pain relief with potentially reduced side effects often associated with
mu receptor activation, such as respiratory depression and addiction potential. This selectivity makes
it a compelling candidate for developing medications that target chronic pain conditions, which often
require long-term management strategies.
Furthermore, the stability provided by the D-Alanine
substitution ensures that (D-Ala2)-Leu-Enkephalin amide is not rapidly decomposed by enzymes, allowing
for more sustained effects compared to natural enkephalins. This property is particularly advantageous
in clinical scenarios where prolonged pain relief is desired without the necessity for frequent
administration, enhancing patient compliance and reducing the burden of constant medication
management.
In addition, (D-Ala2)-Leu-Enkephalin amide's role extends beyond immediate pain
alleviation; it has been studied for its potential to influence mood disorders. By interacting with
opioid receptors that mediate mood and emotional response, this peptide might offer dual benefits in
treating conditions that co-present with both pain and depressive symptoms, making it a multifaceted
tool in comprehensive pain management strategies.
Moreover, ongoing research explores its
neuroprotective effects, suggesting its utility in treating neurodegenerative diseases where pain is a
significant component. Preliminary studies indicate that (D-Ala2)-Leu-Enkephalin amide might help
mitigate neuroinflammation and neuron damage, contributing to its multifaceted therapeutic profile.
However, despite these promising benefits, it is crucial to approach its application with rigorous
scientific validation to ascertain efficacy, safety, and best practice guidelines in therapeutic
contexts.
Are there any known side effects associated with (D-Ala2)-Leu-Enkephalin
amide?
As with many compounds, especially those interfacing with the body's complex nervous
system like (D-Ala2)-Leu-Enkephalin amide, there are potential side effects and challenges associated
with its use, although research is still elucidating the full spectrum of these effects because of the
detailed nature of investigations required. Being a compound that operates on the opioid receptors, some
expected side effects could mirror those observed with opioid-based medications, albeit potentially with
differences due to its unique receptor target profile and modified stability.
Common opioid side
effects include nausea, dizziness, constipation, and the risk of addiction or dependency. However, due
to its specific action on delta receptors, (D-Ala2)-Leu-Enkephalin amide might demonstrate a distinct
side effect profile compared to traditional mu-opioids. This specificity has sparked interest in its
potential to offer effective pain relief while minimizing more severe and dangerous side effects such as
respiratory depression. Yet, such benefits are currently theoretical and require extensive clinical
validation.
There is also the need to consider the context of administration. Patients with
pre-existing conditions or concurrent use of other medications might experience different side effect
profiles or intensities, which stresses the importance of tailored medical oversight. Moreover, due to
its synthetic nature, allergic reactions, though not extensively documented, are a possibility with any
peptide-based treatment, necessitating awareness and preparedness for any hypersensitivity
reactions.
Furthermore, understanding long-term effects is vital, as prolonged usage could lead
to tolerance, where increasing doses might be required to achieve the same therapeutic effect, and
withdrawal symptoms upon cessation might be challenging experiences, echoing the complexity found in
opioid use scenarios.
Despite these concerns, the nuanced difference in receptor selectivity
provides a landscape rich for developing safer, more tolerable opioid analgesics. Continuous
comprehensive clinical trials and research efforts are crucial in exposing any latent side effects not
previously encountered and in defining guidelines that maximize therapeutic benefits while minimizing
risks associated with (D-Ala2)-Leu-Enkephalin amide use. As scientific understanding grows, clearer
insights will emerge about its safety profile, thereby establishing a more robust framework for
effective and safe utilization in medical settings.
How does (D-Ala2)-Leu-Enkephalin amide
compare to traditional opioid medications?
(D-Ala2)-Leu-Enkephalin amide stands out in several
ways compared to traditional opioid medications due to its unique molecular structure and receptor
interactions. Traditional opioids such as morphine, oxycodone, and fentanyl primarily exert their
effects by binding to mu-opioid receptors, which are highly effective in modulating severe pain but also
come with significant drawbacks, such as high potential for addiction, respiratory depression, and
tolerance development.
In contrast, (D-Ala2)-Leu-Enkephalin amide is designed to have a
preferential binding affinity towards delta opioid receptors in the body. This selective interaction is
intended to provide effective analgesic properties while mitigating some of the adverse side effects
associated with mu-opioid receptor activation. For instance, delta receptor stimulation has been linked
to fewer incidences of respiratory depression and lower addictive potential compared to mu receptor
engagement, making it a potential candidate for reducing the risks associated with chronic opioid
therapies.
Additionally, the modification involving the substitution of the second amino acid
with D-Alanine enhances the stability of (D-Ala2)-Leu-Enkephalin amide against enzymatic degradation,
allowing it to remain active for longer durations in the body compared to natural peptides. This
stability potentially reduces the frequency of administration required to maintain therapeutic effects,
which can enhance patient compliance and decrease the chances of withdrawal symptoms associated with
drug cycling.
When considering efficacy, (D-Ala2)-Leu-Enkephalin amide holds promise in
addressing chronic pain and complex conditions that involve neuropathic pain mechanisms, offering a new
avenue that traditional opioids might not effectively manage due to their broad receptor activation.
Moreover, traditional opioids often lead to negative effects on emotional health when used long-term,
whereas studies suggest that delta receptor agonists may have mood-enhancing effects, providing dual
benefits for patients who might suffer from both chronic pain and associated mood
disorders.
Despite this promising profile, the use of (D-Ala2)-Leu-Enkephalin amide must be
assessed with comprehensive scientific understanding to address any unforeseen complexities and side
effects fully. While it offers significant advantages over traditional opioids in hypothesis and
preliminary studies, rigorous clinical trials are essential to substantiate these benefits and to
fine-tune its use safely in medical practices. As such, its comparison to traditional opioids is
fundamentally optimistic but requires further validation and a nuanced understanding by the medical
community.
What is the future potential of (D-Ala2)-Leu-Enkephalin amide in medical
treatments?
The future potential of (D-Ala2)-Leu-Enkephalin amide in medical treatments is a
subject of significant interest and ongoing research, given its distinctive structural and functional
properties which align with modern pharmacological goals of providing effective treatment with minimal
side effects. As a synthetic peptide, it offers a pioneering approach in the development of analgesics
that deviate from the traditional reliance on opium-derived compounds. Its modified design, which allows
for enhanced stability and selectivity towards delta opioid receptors, positions it as a promising lead
compound in the quest for advanced pain management solutions.
One of the most compelling avenues
for its potential use lies in treating chronic pain conditions, which are notoriously difficult to
manage with existing medications due to the side effect profiles and the risk of dependency. By
targeting delta receptors more preferentially, (D-Ala2)-Leu-Enkephalin amide represents a novel approach
that could yield effective relief for patients with fewer adverse consequences. This specificity is
particularly vital for individuals who require long-term pain management strategies but are at risk of
opioid misuse or experiencing severe side effects like respiratory depression linked to standard
opioids.
Furthermore, its role in neuroprotective strategies is gaining traction, with research
exploring its ability to attenuate neuroinflammation and potentially slow the progression of
neurodegenerative diseases. Conditions such as Alzheimer's disease, Parkinson's disease, and even
multiple sclerosis, where pain and novel therapeutic pathways are areas of high interest, might benefit
from compounds like (D-Ala2)-Leu-Enkephalin amide that offer multi-faceted effects beyond pure
analgesia.
Moreover, the mood-enhancing properties associated with delta receptor activation
present an exciting prospect in treating complex comorbid conditions where chronic pain and mood
disorders intersect. It opens pathways for integrative approaches that address both physical and
psychological dimensions of pain-related conditions, offering a more holistic patient care
strategy.
Despite these promising attributes, the progression from potential to practical
application hinges on rigorous scientific research to fully understand its pharmacodynamics, efficacy,
safety, and potential long-term effects. Clinical trials will be instrumental in mapping out its utility
across various conditions and demographics, setting standards for its application in diverse therapeutic
contexts. As the understanding of (D-Ala2)-Leu-Enkephalin amide deepens, its role could fundamentally
shift treatment paradigms, offering a compelling alternative in the biomedical arsenal for tackling some
of the most persistent challenges in pain management and neurological therapy.