Taiy Chemical
(3,5-Diiodo-Tyr1,D-Ala2,N-Me-Phe4,glycinol5)-Enk
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.
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