Synonym |
(D-Ala2)-Met-Enkephalin amide |
Species |
Human |
Protein Accession |
P01210 |
Purity |
≥ 95% |
Endotoxin Level |
< 1.0 EU per µg |
Biological Activity |
The ED50 for this effect is typically 3-10 nM. |
Expression System |
Chemical synthesis |
Fusion Tag |
None |
Predicted Molecular Mass |
471.6 Da |
Formulation |
Lyophilized from a 0.2 µm filtered solution in Acetonitrile and TFA |
Reconstitution |
Reconstitute in water to a concentration of 0.1-1.0 mg/ml. |
Storage & Stability |
Store at -20°C. Store under desiccating conditions. |
FAQ
What is (D-Ala2)-Met-Enkephalin amide, and what are its primary benefits compared to natural
enkephalins?
(D-Ala2)-Met-Enkephalin amide, also commonly referred to as DALA, is a synthetic
peptide analog of the naturally occurring enkephalins produced by the body. Enkephalins belong to a
family of endogenous opioid peptides that play a critical role in modulating pain and promoting
well-being. (D-Ala2)-Met-Enkephalin amide is engineered to enhance certain benefits while minimizing
others, making it potentially more effective in certain scenarios than its natural counterparts. One of
the primary benefits of (D-Ala2)-Met-Enkephalin amide is its increased resistance to enzymatic
degradation. Natural enkephalins are often rapidly broken down in the body by enzymes, which can limit
their effectiveness and duration of action. (D-Ala2)-Met-Enkephalin amide’s synthetic structure is
designed to resist this breakdown, allowing for longer-lasting effects. This prolonged action is
particularly beneficial in therapeutic contexts where sustained peptide activity is desired.
Additionally, (D-Ala2)-Met-Enkephalin amide is specific in its receptor interactions, providing targeted
relief from discomfort. It exhibits high affinity and selectivity for opioid receptors, a characteristic
that reinforces its potency in pain modulation. This can be especially advantageous in scenarios
involving chronic pain management, where precision and sustained relief are pivotal. Moreover, the
altered structure of (D-Ala2)-Met-Enkephalin amide can result in fewer side effects compared to both
natural enkephalins and traditional pharmaceutical options. While naturally occurring enkephalins may
lead to undesired reactions when used therapeutically, (D-Ala2)-Met-Enkephalin amide’s modifications
allow for a reduction in peripheral side effects by focusing its activity centrally within the nervous
system. This balance of efficacy and minimized risk underscores its potential as a therapeutic agent.
Additionally, research has underscored the neuroprotective properties of (D-Ala2)-Met-Enkephalin amide.
This peptide can help in buffering neurons against damage, acting as a safeguard during
neurodegenerative processes or acute neuronal injury. The enhanced stability and efficacy of
(D-Ala2)-Met-Enkephalin amide, combined with its targeted action and neuroprotective qualities, make it
a significant candidate for various therapeutic applications, particularly those involving chronic pain
and neurological health. Its development continues to excite researchers seeking innovative solutions
for conditions linked with pain and neural challenges.
How does the synthetic nature of
(D-Ala2)-Met-Enkephalin amide affect its application in scientific research and potential medical
treatments?
The synthetic nature of (D-Ala2)-Met-Enkephalin amide plays a crucial role in its
applications across scientific research and potential medical treatments. Being a synthetic analog of
natural enkephalins, it presents several unique advantages that enhance its utility in both experimental
and therapeutic settings. First, the synthetic nature ensures controlled and reproducible properties.
Unlike natural compounds, which can vary due to biological inconsistencies, (D-Ala2)-Met-Enkephalin
amide is manufactured to exact specifications, ensuring consistency in research outcomes and potential
treatments. This consistency is critical in scientific investigations, enabling researchers to rely on
uniform data and thereby minimizing variables unrelated to the primary focus of their studies.
Additionally, its synthetic origin allows for tailored modifications to improve specific
characteristics. For instance, (D-Ala2)-Met-Enkephalin amide has been designed to resist enzymatic
breakdown, as a result of modifications like the substitution of D-Alanine at position 2. This is
pivotal in extending the peptide's half-life within the body, thus making it a more practical candidate
for sustained therapeutic effects, as it can remain active in the system longer than its natural
counterparts. The enhanced stability also translates to less frequent dosing in potential medical
applications, which is advantageous in a clinical context as it could lead to improved patient
compliance. The synthetic design further provides a platform for derivative compounds. Researchers can
experiment with additional modifications to explore new potential uses of the compound, adapting its
structure to target different pathways or conditions more effectively. This flexibility provides a
robust basis for expanding therapeutic avenues and understanding complex physiological mechanisms.
Furthermore, synthetic production often lessens the risk of immune reactions. Natural peptides can
sometimes trigger immune responses when administered therapeutically due to their recognition as foreign
by the host's immune system. The synthetic variations like (D-Ala2)-Met-Enkephalin amide can be designed
to minimize these responses, potentially offering safer treatment options. In medical research, the
insight into how synthetic peptides interact with cellular systems can inform the development of novel
drug delivery methods and formulations that further enhance bioavailability and efficacy. The
exploration of (D-Ala2)-Met-Enkephalin amide’s interaction with neurological systems also holds promise
in addressing neurodegenerative conditions or neuronal trauma, expanding its applicability beyond pain
management. This synthetic peptide represents a pivotal blend of innovative design and practical
application, propelling research forward and offering promising therapeutic potential.
In what
ways can (D-Ala2)-Met-Enkephalin amide contribute to advancements in pain management therapies?
(D-Ala2)-Met-Enkephalin amide holds immense potential in revolutionizing pain management therapies,
primarily due to its unique properties as a stable and potent synthetic analog of natural enkephalins.
This synthetic peptide interacts with the opioid receptors in the human body, which are crucial in
relaying pain signals and modulating the perception of pain. The primary advantage of
(D-Ala2)-Met-Enkephalin amide in pain management lies in its high affinity and selectivity for these
opioid receptors, particularly the delta and mu subtypes. By strongly binding to these receptors, the
peptide can effectively interrupt pain signal transmission in the body, providing substantial relief.
This mechanism parallels common pain medications yet promises decreased dependency and lower addiction
potential due to its distinct interaction profile, a characteristic highly beneficial in the context of
long-term pain management strategies. Moreover, its resistance to enzymatic degradation prolongs its
effective duration. In traditional pain management, drugs may require frequent administration to
maintain their efficacy, burdensome for patients, especially those with chronic conditions.
(D-Ala2)-Met-Enkephalin amide, however, has a longer half-life, ensuring sustained pain relief without
needing as frequent dosing. This aspect could significantly improve patient adherence to therapy
regimens, enhancing overall outcomes. Also, its central mode of action minimizes peripheral side effects
typical of many conventional painkillers, such as gastrointestinal issues, sedation, or cardiac effects.
The minimized side effect profile makes it a compelling choice for replacing or supplementing existing
pain management strategies, particularly for individuals at risk of complications from standard
treatments. This impact can be crucial for pain patients with a significant burden of medication-related
side effects. Additionally, (D-Ala2)-Met-Enkephalin amide’s neuropathic pain relief potential is a
promising area of development. Neuropathic pain, resulting from nerve damage or dysfunction, often
proves resistant to traditional analgesics and poses significant treatment challenges. The specific
interaction of the peptide with opioid receptors can modulate this pain more effectively, suggesting a
novel pathway for exploring neuropathic pain therapies. Its potential neuroprotective effects add
another layer of benefit, contributing to the protection and recovery of nerve structures, an essential
factor in addressing the mechanisms of chronic pain at their source. Clinical research and trials can
further solidify (D-Ala2)-Met-Enkephalin amide’s role in pain medicine, offering new insights into
personalized medicine approaches that optimize treatment regimens for individual pain profiles. Its
integration into current pain management paradigms could spearhead a transformative shift towards more
sustainable and effective therapies, empowering patients with chronic and acute pain to maintain better
quality of life.
How does (D-Ala2)-Met-Enkephalin amide differ from other pain relief substances
derived from the opioid family in terms of receptors and side effect profile?
(D-Ala2)-Met-Enkephalin amide stands out within the opioid family due to its unique affinity for
specific opioid receptors and its differentiated side effect profile. As an analog of naturally
occurring enkephalins, this synthetic peptide exhibits high specificity toward delta and mu opioid
receptors, which are integral to pain perception and modulation within the central nervous system.
Compared to traditional opioids, which often non-selectively target all opioid receptor subtypes
including kappa, leading to a broad spectrum of effects, (D-Ala2)-Met-Enkephalin amide's focused action
results in more targeted therapeutic outcomes. This selective receptor interaction means that
(D-Ala2)-Met-Enkephalin amide potentially provides effective pain relief with reduced incidence of
certain side effects commonly associated with classic opioids. Traditional opioids, while effective in
pain control, often engage the kappa opioid receptors, contributing to undesirable effects such as
dysphoria and sedation. (D-Ala2)-Met-Enkephalin amide’s reduced action on these receptors helps in
minimizing such effects, making it potentially more tolerable over prolonged use. Focusing its action on
the delta and mu receptors, especially, can lead to potent analgesia with a decreased propensity for
common opioid-related drawbacks like respiratory depression, a critical concern in opioid
administration. Furthermore, the risk for addiction and dependency, prominent issues with traditional
opioids, might be lower with (D-Ala2)-Met-Enkephalin amide, at least theoretically. Its distinct
receptor interactions and structural resilience against enzyme actions imply less frequent need and a
different physiological response profile that deviates from the typical euphoria-driven addiction
pathway seen with many conventional opioids. This attribute is particularly beneficial in chronic pain
settings, where long-term medication safety is paramount. Additionally, (D-Ala2)-Met-Enkephalin amide's
chemistry provides inherent advantages in crossing the blood-brain barrier effectively, ensuring central
nervous system penetration without contributing to peripheral side effects, which can include nausea,
muscle rigidity, or gastrointestinal complications. By concentrating its effects on pain modulating
centers in the brain and spinal cord, the peptide aims to isolate its analgesic actions, reducing
systemic side effects that diminish patient quality of life. Research into (D-Ala2)-Met-Enkephalin amide
continues to explore these benefits, with promising insights suggesting its capacity to function as part
of overarching strategies designed to reduce reliance on traditional opioids. Its nuanced receptor
engagement could supplement existing treatments, providing balanced pain control while advocating a
sensible approach to managing the risks typical of opioid use. This characteristics profile positions
(D-Ala2)-Met-Enkephalin amide as a critical exploratory compound moving forward in the quest for
efficacious and safer pain relief options.
What role does (D-Ala2)-Met-Enkephalin amide play in
neurological studies, particularly related to addiction and neuroprotection?
(D-Ala2)-Met-Enkephalin
amide emerges as a significant compound in neurological studies, especially concerning addiction
pathways and neuroprotection mechanisms. Its synthetic structure and specific receptor affinities render
it an interesting subject for exploring these intricate neurological phenomena. In terms of addiction,
(D-Ala2)-Met-Enkephalin amide contributes to understanding the engagement of opioid receptors and how
these interactions influence addictive behaviors. Unlike traditional opioids that indiscriminately
activate mu, delta, and kappa receptors, thereby establishing a broad basis for addiction through
euphoria and reinforcement pathways, (D-Ala2)-Met-Enkephalin amide offers more precise receptor
targeting. This specificity provides insight into how delta and mu receptor pathways can modulate
rewards and dependence separately from the full opioid engagement. Research involving
(D-Ala2)-Met-Enkephalin amide aids in delineating these pathways, offering potential clues for
developing therapies that mitigate addiction while preserving analgesic efficacy. Additionally, the role
of (D-Ala2)-Met-Enkephalin amide in neuroprotection is becoming increasingly recognized. Due to its
modulation of neurotransmitter release and receptor activity, this peptide engages pathways that can
shield neurons from excitotoxicity, a condition commonly linked with overactivity during injury or
neurodegenerative diseases such as Alzheimer's or Parkinson's. By tempering the excessive release of
excitatory neurotransmitters, (D-Ala2)-Met-Enkephalin amide might prevent or reduce neuronal damage,
fostering a protective environment conducive to healthy neural function. This neuroprotective potential
fuels studies into its utility in treating neurodegenerative conditions or as a preventive therapy for
susceptible individuals. Its integration into neural mechanisms also suggests its contribution to
synaptic plasticity and cognitive functions, relevant areas in both health and disease states. Another
crucial aspect of research with (D-Ala2)-Met-Enkephalin amide is its impact on inflammatory pathways
within the nervous system. Neuroinflammation plays a pivotal role in various neural disorders; thus,
assessing how synthetic enkephalins modulate inflammatory responses opens doors to novel
anti-inflammatory strategies that can complement neuroprotection efforts. Explorations in this domain
reveal (D-Ala2)-Met-Enkephalin amide’s potential in modifying microglial activity, which may help manage
chronic pain, neurodegeneration, and conditions exacerbated by ongoing inflammation. These studies
position (D-Ala2)-Met-Enkephalin amide as a versatile tool in the laboratory, elucidating the delicate
balance of neural receptor activities and offering glimpses into new therapeutic landscapes for
neurological conditions. By unraveling mechanisms associated with opioid receptors and neuroprotection,
researchers aim to design better interventions for addiction, safeguarding neurological health while
harnessing comprehensive therapeutic benefits of compounds like (D-Ala2)-Met-Enkephalin amide.
What implications does the use of (D-Ala2)-Met-Enkephalin amide have for future developments in
synthetic peptide therapeutics?
The development and use of (D-Ala2)-Met-Enkephalin amide herald
significant implications for the future of synthetic peptide therapeutics, serving as a blueprint for
extending the capabilities of such therapies across various medical domains. As a synthetic analog,
(D-Ala2)-Met-Enkephalin amide sets a precedent in peptide engineering, emphasizing the value of
structural modification in achieving desired pharmacological properties while minimizing unwanted
effects, a challenge commonly encountered in drug development. Its design showcases how specific amino
acid substitutions and structural optimization can enhance stability, prolong activity, and improve
receptor selectivity. In doing so, it paves the way for designing other peptides with improved
therapeutic indices, facilitating more effective and targeted treatments. This innovation holds promise
for addressing complex pathologies where traditional small-molecule drugs might fall short, either due
to their lack of specificity or adverse side effect profiles. Furthermore, the successful exploration of
(D-Ala2)-Met-Enkephalin amide in preclinical and clinical studies can encourage the pharmaceutical
industry to invest more in this sector, potentially accelerating the development of first-in-class or
best-in-class drugs for numerous conditions, including chronic pain, neurodegeneration, and immune
disorders. The research surrounding (D-Ala2)-Met-Enkephalin amide highlights the therapeutic viability
of modulating endogenous peptide systems, further justifying exploration into other peptide systems like
tachykinins, bradykinins, and others – each with roles in critical physiological processes. Expanding
our toolkit with such analogs can revolutionize treatment strategies, primarily through targeted therapy
approaches that leverage the inherent capabilities of peptides to interact specifically and intimately
with biological systems. Additionally, (D-Ala2)-Met-Enkephalin amide encourages advancements in delivery
technologies. Given its improved stability and resistance to degradation, continued research and
breakthroughs in this area can further enhance its effectiveness and convenience, soothing patient
concerns related to administration and dosing. Future delivery systems, potentially leveraging
nanotechnology or novel biomaterials, could enhance tissue targeting, bioavailability, and patient
compliance, pivotal factors in the success of peptide-based therapies. Moreover, the evolution of
(D-Ala2)-Met-Enkephalin amide highlights ethical and regulatory considerations surrounding synthetic
therapeutics. As its use becomes more widespread, it will propel discussions on regulatory frameworks
that ensure patient safety while accommodating the innovative pace of peptide drug development. The
trajectory of (D-Ala2)-Met-Enkephalin amide underscores the transformative potential of synthetic
peptides, thus shaping a future where precision medicine thrives, offering personalized solutions
tailored to individual genetic and biochemical profiles, premised on cutting-edge peptide science. The
legacy of (D-Ala2)-Met-Enkephalin amide might soon resonate within new therapeutic categories, defining
a revolutionary era in medicine where tailored peptide solutions play essential roles in healthcare.