Synonym |
Ala2-Leu-enkephalin |
Species |
Human |
Protein Accession |
P01210 |
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 |
574.68 Da |
Formulation |
Lyophilized powder |
Reconstitution |
Reconstitute in water to a concentration of 1mg/ml |
Storage & Stability |
Store at -20°C upon arrival. Can be stored at 4°C for one month. For long-term storage, store at
-20°C. |
FAQ
What is (Ala2)-Leu-Enkephalin and how does it differ from regular
Enkephalin?
(Ala2)-Leu-Enkephalin is a synthetic peptide that resembles the naturally occurring
enkephalins in the human body. Enkephalins are part of the endogenous opioid peptides, which play a
crucial role in pain modulation, among other physiological processes. Enkephalins bind to opioid
receptors in the brain and inhibit the perception of pain by reducing the transmission of pain signals.
The primary distinction lies in the amino acid substitution at the second position; in
(Ala2)-Leu-Enkephalin, alanine replaces the naturally occurring glycine. This substitution is
significant as it alters the peptide's binding affinity to receptor sites, potentially modifying its
stability or resistance to enzymatic degradation.
The modification in (Ala2)-Leu-Enkephalin
could lead to differences in how the peptide interacts with different subtypes of opioid receptors,
namely mu, delta, and kappa receptors. This specific substitution is often pursued in research to
increase the understanding of opioid receptor preferences and to explore potential therapeutic
applications with improved efficacy or reduced side effects compared to natural enkephalins.
Additionally, the synthetic nature of (Ala2)-Leu-Enkephalin allows researchers to study its
pharmacokinetics and dynamics, providing insights into how these peptides can be manipulated for better
therapeutic outcomes.
In terms of practical applications, this modified peptide is often explored
in experimental settings involving pain management, mood regulation, and neurological research.
Researchers are interested in its potential to create new classes of analgesic drugs that can provide
pain relief without the adverse effects associated with opioid usage, such as addiction or tolerance.
The investigation into such analogs aims to balance therapeutic benefits with safety, opening paths for
pain management solutions that address the opioid crisis by reducing dependence on traditional opioid
medications.
Are there potential therapeutic applications for (Ala2)-Leu-Enkephalin?
The
exploration of potential therapeutic applications for (Ala2)-Leu-Enkephalin centers primarily on its
enhanced stability and altered interactions with the body’s opioids receptors due to its synthetic
modification. Researchers are particularly interested in how this peptide can be leveraged to develop
novel analgesic drugs with more favorable safety profiles compared to traditional opioids. The ultimate
goal is to find a balance between effective pain management and reduced risks of side effects such as
tolerance and dependency which are major downsides of current opioid
medications.
(Ala2)-Leu-Enkephalin’s potential extends into various dimensions of therapeutic
research. Its role in pain modulation is especially crucial in addressing chronic pain conditions for
which long-term opioid use is currently a major treatment option. By binding with different affinities
to opioid receptor subtypes, (Ala2)-Leu-Enkephalin offers an opportunity to develop drugs that target
the necessary pathways involved in pain relief while potentially circumventing the pathways that lead to
addiction or other side effects.
Moreover, the study of (Ala2)-Leu-Enkephalin has implications
beyond pain management. The central role of enkephalins in mood regulation and stress response suggests
potential applications in psychiatric or psychological therapeutic areas. Researchers hypothesize that
peptides like (Ala2)-Leu-Enkephalin could be engineered to address disorders such as depression or
anxiety by modulating neurotransmitter systems more precisely than conventional
therapeutics.
Furthermore, in the field of neuroprotection, there’s interest in the potential of
(Ala2)-Leu-Enkephalin for treating neurodegenerative disorders such as Parkinson’s or Alzheimer’s
disease. By modulating synaptic transmission and neuronal health, this peptide could contribute to
strategies aimed at preserving cognitive function and slowing disease progression.
To harness
these therapeutic potentials, ongoing research is needed. Clinical trials must establish efficacy,
optimal dosing regimens, and long-term safety. A successful development of (Ala2)-Leu-Enkephalin-based
therapies could revolutionize how we approach treating conditions traditionally managed by opioid
receptors, offering not only solutions to current pharmacological challenges but also contributing to
the broader landscape of medical research where personalized and precision medicine is
paramount.
What research is currently being conducted on (Ala2)-Leu-Enkephalin?
The
current body of research involving (Ala2)-Leu-Enkephalin spans preclinical studies focused on
understanding its pharmacological properties and potential clinical applications. These studies are
crucial for elucidating how the structural modifications in (Ala2)-Leu-Enkephalin influence its
interactions with opioid receptors and its overall pharmacokinetic profile. Researchers are actively
examining the peptide’s affinity for different opioid receptor subtypes to map out its efficacy and
safety spectrum.
A key area of research is comparing (Ala2)-Leu-Enkephalin to traditional opioid
peptides to evaluate its stability against enzymatic degradation. One of the main challenges with
natural peptides is their rapid breakdown in the body, which can limit their clinical utility. By
substituting alanine in the peptide chain, researchers aim to enhance its metabolic stability,
potentially leading to improved duration of action or bioavailability. Comparative studies are being
utilized to assess these properties, hoping to mark a significant improvement that would make
(Ala2)-Leu-Enkephalin a viable candidate for therapeutic development.
Moreover, there are
exploratory studies aimed at detailing the mechanism by which (Ala2)-Leu-Enkephalin affects pain
modulation pathways. Understanding these pathways can help to identify additional therapeutic targets
and refine mechanisms to further customize pain management strategies. Animal models are frequently used
in these studies to measure analgesic effects and side effect profiles, providing foundational data that
could one day translate into human clinical trials.
Beyond pain modulation, research into
(Ala2)-Leu-Enkephalin also delves into potential roles in mood regulation and neuroprotection.
Investigators analyze its interactions with brain regions involved in emotional processing and neuronal
health, considering its potential to influence mood disorders or neurodegenerative diseases. This is
complemented by molecular and genetic techniques used to understand the expression patterns and
regulation of receptors affected by the peptide, providing deeper insights into its multifaceted roles
in central nervous system functioning.
Regulatory and ethical aspects of this research also form
a significant component, as aligning studies with medical guidelines ensures safety and efficacy
standards are met. The dynamic field of research on (Ala2)-Leu-Enkephalin is thus foundational not only
in therapeutic innovations but also in enhancing scientific understandings of peptide therapeutics in
general.
What challenges are associated with developing (Ala2)-Leu-Enkephalin-based
therapies?
Developing therapies based on (Ala2)-Leu-Enkephalin involves addressing several
complex challenges. A primary hurdle is the inherent instability and propensity for rapid degradation of
peptide-based drugs in the human body. Naturally occurring enkephalins are quickly broken down by
enzymes, limiting their practical use in pharmacotherapy. Therefore, while (Ala2)-Leu-Enkephalin’s
alanine substitution aims to improve stability, it remains necessary to confirm whether this
modification sufficiently prolongs the peptide's active duration in clinical settings. Enhancing the
peptide’s stability could potentially be achieved with further chemical modifications or by developing
advanced drug delivery systems that protect the peptide from premature degradation.
The
pharmacokinetics and bioavailability of (Ala2)-Leu-Enkephalin present additional challenges. Peptides
often suffer from poor absorption when administered orally due to their size and structural complexity.
As such, alternative administration routes, such as intravenous, transdermal, or intranasal pathways,
may be explored, each coming with their own logistical and compliance considerations. Ensuring
consistent and efficient delivery of the peptide to target sites in the body is crucial to harness its
therapeutic potential.
The development process must also address any potential for side effects
or unintended interactions with opioid receptors. While one goal of developing (Ala2)-Leu-Enkephalin is
to decrease the side effects associated with traditional opioids, such as addiction or tolerance,
studies must demonstrate that it indeed has a more favorable safety profile. This requires extensive
preclinical and clinical research to monitor not only efficacy but also potential off-target effects
throughout long-term administration.
Moreover, regulatory pathways for approving peptide-based
therapies can be intricate, often requiring extensive documentation regarding safety, manufacturing
processes, and efficacy outcomes. Conducting robust clinical trials that meet regulatory standards and
demonstrate the therapeutic benefits over existing treatment options is a key part of overcoming these
challenges.
Intellectual property considerations and a competitive research landscape are also
factors to consider. Developing new treatments requires navigating patents and legal aspects to ensure
innovation is protected, contributing to the financial viability and market potential of new
therapies.
Addressing these challenges involves a multidisciplinary approach, combining
advancements in biotechnology, pharmacology, and regulatory science to pave the way for successful
(Ala2)-Leu-Enkephalin-based therapies, potentially transforming pain management and neurological
treatments in the future.
How does (Ala2)-Leu-Enkephalin potentially contribute to solutions for
the opioid crisis?
The opioid crisis is characterized by widespread misuse of prescription and
non-prescription opioid drugs, leading to addiction, overdoses, and substantial public health impacts.
(Ala2)-Leu-Enkephalin offers a potential innovative approach to mitigating this crisis by providing
alternative pathways for pain management without the severe risks associated with traditional opioid
use.
(Ala2)-Leu-Enkephalin holds promise as it potentially maintains the analgesic efficacy of
opioids while offering a reduced risk of addiction. By modulating pain through targeted receptor
interactions, particularly focusing on minimizing actions at mu-opioid receptors, associated with high
dependency risk, (Ala2)-Leu-Enkephalin might mitigate abuse potential. If proven effective, this
therapeutic profile can provide clinicians with alternatives that fulfill analgesic needs while reducing
the risk of developing substance use disorders.
Furthermore, one strategy in combatting the
opioid crisis is minimizing the side effects of pain therapies. Synthetic modifications like those seen
in (Ala2)-Leu-Enkephalin aim to increase peptide stability and target receptor selectivity to achieve
more predictable and safer interaction profiles. An important aspect is to maintain or enhance
therapeutic effects on pain while reducing likelihood for abuse and other common opioid-associated side
effects such as constipation or respiratory depression.
The research and development of
(Ala2)-Leu-Enkephalin also reflect a broader shift toward addressing pain management through precision
medicine. By innovating opioid receptor biology with specific peptides, there is an opportunity to craft
personalized medicine approaches that consider individual patient profiles, optimizing therapeutic
outcomes and further reducing the incidence of adverse effects.
Implementing such therapies
requires not only scientific and clinical validation but also systemic changes in healthcare practices
and prescription habits. Education and awareness among healthcare providers and patients are crucial to
ensure such novel treatments are adopted in a manner consistent with their intended use. By integrating
therapies like those potentially offered by (Ala2)-Leu-Enkephalin into comprehensive pain management
strategies, there is hope for tangible contributions to solving the opioid crisis, aligning patient
treatment needs with public health goals for safety and sustainability.