Synonym |
(3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk |
Species |
Human |
Protein Accession |
P01210 |
Purity |
Greater than 95% as determined by SDS-PAGE |
Endotoxin Level |
Less than 1 EU/μg of protein |
Biological Activity |
Not available |
Expression System |
E. coli |
Fusion Tag |
None |
Predicted Molecular Mass |
6638 Da |
Formulation |
Lyophilized from a 0.2 μm filtered solution in PBS |
Reconstitution |
Reconstitute in water to a concentration of 0.1-1.0 mg/ml |
Storage & Stability |
Store lyophilized protein at -20°C. Aliquot reconstituted protein and store at -20°C. Avoid
repeated freeze-thaw cycles. |
FAQ
What is (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk, and what are its primary uses?
(3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk, commonly referred to among researchers and the
scientific community as a synthetic analog of enkephalins, is a peptide-based compound that has gained
significant attention for its role in acting as an opioid receptor agonist. Enkephalins are naturally
occurring peptides in the brain that modulate nociception in the body's pain pathways. They function by
interacting with the body's opioid receptors, much like how naturally occurring morphine or other
opiates function, rendering them instrumental in pain management studies. However, unlike classical
opiates that are extracted from the opium poppy plant, (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk
is a lab-created compound designed to finely tune the interaction with specific opioid receptors. This
compound's uniqueness lies in its chemical structure, highly modified compared to natural enkephalins to
potentially increase stability, efficacy, and selectivity when engaging with targeted opioid receptors.
In practical terms, one of the key factors in studying such a compound is its potential reduced
side-effect profile compared to traditional opioids. Researchers focus on its analgesic properties,
particularly whether it offers pain relief without the high risk of addiction or other adverse effects
commonly associated with opioid therapies. By altering the active sites of the peptide chain, scientists
aim to achieve receptor selectivity that might limit activity to only desired pathways. This selectivity
is crucial for minimizing unwanted side effects such as respiratory depression, tolerance, and
addiction.
In addition, the implication of this research extends into areas like chronic pain
management, where long-term opioid use poses risks; thus, finding alternatives with effective analgesia
and lower risk profiles is paramount. Therefore, while much of the research is preclinical, meaning it
is conducted through laboratory or animal studies, the findings could eventually inform the development
of safer analgesic medications for human use. Understanding these dynamics is integral to furthering the
development of therapeutics that can revolutionize the treatment landscape for pain and related
conditions.
Is (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk safe for human use?
The
question of safety regarding (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk is a multifaceted one that
hinges on the necessity for extensive research and clinical trials prior to considering any potential
therapeutic application in humans. As of now, this compound is predominantly utilized within scientific
and research circles to explore its biochemical properties, mechanisms of interaction with various
opioid receptors, and potential uses. It's crucial to understand the rigorous process involved in the
approval of any new therapeutic agent for human use, which includes a series of thorough investigations
spanning toxicology, pharmacodynamics, pharmacokinetics, and ultimately, comprehensive clinical trials.
In the initial stages, researchers assess the compound in vitro, meaning they will study its
interactions and effects within controlled environments outside living organisms. These experiments help
scientists understand the fundamental properties of the compound and its preliminary safety profile.
Following successful lab-based tests, the compound is typically evaluated in animal models to assess its
efficacy and safety in a living organism, providing insights into dosage ranges and potential adverse
effects.
Once preclinical investigations indicate a favorable safety and efficacy profile, the
compound might then progress to clinical trials, starting with small-scale Phase I trials in humans to
evaluate safety, dosage tolerance, and side effects. If these are successful, the process advances
through further trial phases, each aiming for larger populations and more detailed investigations into
efficacy and safety over longer durations.
As (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk
currently stands as a compound of interest primarily in the scientific research realm, it has not
undergone the extensive trials that regulatory bodies such as the FDA require before deeming a drug safe
and effective for human use. This high bar for safety and efficacy is crucial to ensuring that any new
medical interventions do more good than harm. Until such studies and trials substantiate the compound's
safety and therapeutic potential, it remains a promising candidate requiring meticulous scientific
scrutiny before any contemplation of human application.
How does
(3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk differ from traditional opioids?
The distinctions
between (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk and traditional opioids are profound, primarily
due to differences in chemical composition, mechanism of action, and potential implications for safety
and efficacy. Traditional opioids, such as morphine, codeine, and oxycodone, are either natural or
semisynthetic derivatives of opium alkaloids that exert their effects primarily by binding
non-selectively to opioid receptors in the brain and other parts of the body. This binding produces the
well-known analgesic effects, but it also brings about a range of unwelcome side effects, such as
respiratory depression, sedation, constipation, and, critically, the potential for addiction and
development of tolerance.
(3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk, on the other hand, is
a synthetic peptide primarily characterized by its tailored structure that aims to interact with opioid
receptors with more precision and potentially less non-specific binding. This specificity is achieved by
altering the natural structure of enkephalins, small peptides within the body that bind to opioid
receptors and modulate pain. The synthetic modification involves substituting certain amino acids to
enhance binding affinity, metabolic stability, and receptor selectivity.
One notable intent of
these structural modifications is to minimize the side effects seen with traditional opioids.
Non-selective binding of traditional opioids can lead to widespread receptor activation, whereas
designing molecules like (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk seeks to fine-tune this
interaction, ideally achieving analgesia with reduced risk of addiction, tolerance, or other side
effects.
Moreover, the increased stability inherent in such synthetic peptides may result in
reduced administration frequency. Traditional opioids often require frequent dosing due to their
metabolic breakdown, leading to peaks and troughs in drug levels that can exacerbate side effects. A
compounded design in (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk that resists rapid degradation
might thus offer a smoother pharmacokinetic profile, potentially providing consistent pain relief over
extended periods.
Scientific exploration into such compounds signifies an effort to address the
current opioid crisis by innovating pain management solutions that maintain high efficacy, minimize side
effects, and importantly, reduce the potential for abuse and dependency. While promising, these
characteristics of (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk require comprehensive validation
through research to fully establish these benefits over traditional opioids.
What potential
advantages does (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk offer over existing therapies?
The
scientific interest surrounding (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk is driven by its
potential to offer advantages over current therapies, primarily within the domain of pain management.
Its design as a synthetic analog allows for optimization aimed at addressing some of the long-standing
challenges associated with traditional opioids and other analgesics. One of the chief advantages posited
by researchers is the enhanced receptor selectivity of this compound. By selectively targeting specific
opioid receptors, particularly those implicated in pain relief without significantly affecting others
associated with negative side effects, (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk could
theoretically reduce the risk of side effects such as addiction, tolerance, and respiratory depression.
This improvement in receptor selectivity is a significant leap forward in the design of safer
analgesics.
Furthermore, the structural modifications leading to increased stability can be seen
as another advantage. Traditional opioids can be subject to rapid metabolism, necessitating frequent
dosing and potentially leading to fluctuations in pain management. An enhanced half-life in the body
leads to more consistent drug levels, potentially improving patient compliance and overall pain control
while reducing abuse potential, as slower metabolism might mitigate the "reward" sensation some opioids
confer.
The compound's synthetic nature allows for intentional alterations that could improve
penetration across the blood-brain barrier, an essential factor in ensuring that adequate concentrations
reach the central nervous system to confer analgesia. Additionally, adjustments in the peptide’s
structure might offer increased resistance to enzymatic degradation, both during circulation and at the
receptor level, sustaining its therapeutic effects longer than some conventional
counterparts.
Aside from its analgesic potential,
(3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk's scaffolding also opens the door for exploring broader
neurological applications, such as in conditions related to mood disorders or neurodegeneration, where
central nervous system targeting with lower side effects could offer novel therapeutic
opportunities.
However, it is crucial to reiterate that while the theoretical benefits are
compelling, empirical validation through rigorous research is necessary. Exploration in both preclinical
and clinical settings will determine whether these potential advantages translate into real-world
efficacy and safety improvements. Optimizing the delicate balance between efficacy and safety remains at
the forefront of (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk’s potential advantages over existing
pain management therapies.
How is (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk synthesized in
the laboratory?
The synthesis of (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk in the laboratory
is a complex process involving precise chemical and biochemical techniques. Peptide synthesis, the
method used, is an intricate endeavor due to the requirements for purity and correct sequence alignment
essential for biological activity. Typically, solid-phase peptide synthesis (SPPS) is employed, a method
renowned for its efficacy in forming peptides with complex sequences such as
(3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk.
The process commences with the selection of a
suitable protective resin; these resins serve as the backbone to which the carboxyl terminus of the
incoming peptide sequence will anchor. Coupling reactions then form peptide bonds between the individual
amino acids. For (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk, each amino acid in its specific
sequence must be carefully integrated and protected during synthesis to ensure structural integrity.
Protecting groups are used to temporarily block reactive sites on amino acids that shouldn't participate
in unwanted side reactions.
Synthesis proceeds in a stepwise manner with each cycle involving the
addition of new amino acids to the growing chain, typically activated by coupling agents, facilitating
the formation of peptide bonds. After each addition, the newly added amino acid's protective group is
removed to allow for the bond formation with the next. This careful addition and deprotection process
ensures the sequence integrity required for (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk's
biological activity.
Once the full peptide chain is assembled, cleavage from the resin liberates
the peptide, often accompanied by the removal of side-chain protective groups. The next step
necessitates purification, typically through high-performance liquid chromatography (HPLC), given the
need to isolate the desired peptide from by-products and contaminants. The purity of any
pharmacologically active compound is pivotal, particularly for research applications where the presence
of impurities could alter biological readings or effects.
The precise synthesis and purification
of (3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk exemplify the skill and technological precision
required in modern peptide chemistry. Such advancements in synthetic methodologies have greatly expanded
the toolkit available to researchers, empowering the exploration of therapeutic peptides like
(3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk with hopes of discovering novel therapeutic pathways in
medicine.