Synonym |
SP(5-11) |
Species |
Human |
Protein Accession |
P20366 |
Purity |
Greater than 95% as determined by HPLC analysis |
Endotoxin Level |
< 0.1 EU per 1 μg of the protein by the LAL method |
Biological Activity |
Fully biologically active when compared to standard. The specific activity is determined by the
dose-dependent stimulation of the proliferation of murine 3T3 cells. |
Expression System |
E. coli |
Fusion Tag |
N/A |
Predicted Molecular Mass |
8647 Da |
Formulation |
Lyophilized from a 0.2 μm filtered solution in Acetonitrile and TFA |
Reconstitution |
Centrifuge the vial prior to opening. Reconstitute in 100 µl of water to a concentration of
0.1-1.0 mg/ml. Do not vortex. For extended storage, it is recommended to further dilute in a
buffer containing a carrier protein (example 0.1% BSA) and store in working aliquots at -20°C to
-80°C. |
Storage & Stability |
Store at -20°C to -80°C. It is recommended to store the product in working aliquots at -20°C to
-80°C. Avoid repeated freeze-thaw cycles. |
FAQ
What is (Pyr5)-Substance P (5-11) and how does it work?
(Pyr5)-Substance P (5-11) is a derivative of
the naturally occurring peptide, Substance P, which is part of the tachykinin family. It plays a crucial
role in the neurotransmission of pain and other sensory functions, commonly associated with inflammation
and the body's response to stress. (Pyr5)-Substance P (5-11) is a truncated form that retains the
biological activity of the full-length peptide but often with different or enhanced properties. This
particular derivative involves the replacement of certain residues which increases its binding affinity
and potency for neurokinin receptors, primarily the NK1 receptor. The parent compound, Substance P, has
been widely studied for its role in the central nervous system and its effects on mood regulation,
stress tolerance, pain perception, and nausea. Its potential in treating a variety of disorders from
depression to ulcerative colitis has been a topic of interest.
The mechanism of action for
(Pyr5)-Substance P (5-11) involves its interaction with NK1 receptors, which are G-protein-coupled
receptors prominently expressed in the central and peripheral nervous systems. By binding to these
receptors, (Pyr5)-Substance P (5-11) can modulate various physiological responses, including
vasodilation, pain transmission, and smooth muscle contraction. Researchers are interested in this
derivative due to its potential therapeutic benefits, including influencing disease progression in
conditions like chronic pain syndromes and inflammatory diseases. The derivative of Substance P may
interact differently with other components in the pain pathway, leading to potentially fewer side
effects or interactions compared to traditional treatments that often rely on broader systemic effects.
While the precise therapeutic impacts and mechanisms continue to be elucidated, its targeted receptor
interaction suggests a promising avenue for developing highly specific treatments with potentially fewer
side effects compared to more generalized pharmacological interventions.
What are the potential
applications of (Pyr5)-Substance P (5-11) in medical research?
(Pyr5)-Substance P (5-11) holds
significant potential across various domains of medical research due to its role in modulating the
neurokinin pathways associated with pain, inflammation, and stress responses. One key area of focus is
pain management. Traditional pain relief methods often present challenges such as addiction, tolerance,
and undesirable side effects. (Pyr5)-Substance P (5-11) provides a promising alternative by specifically
targeting the NK1 receptor, which is known to play an integral part in pain pathways. Through animal
studies and preliminary clinical research, scientists explore its efficacy in treating chronic pain
conditions, like neuropathic pain and inflammatory diseases, providing a potentially novel therapeutic
option that minimizes the use of opioids.
Another major application of (Pyr5)-Substance P (5-11)
in medical research is within the realm of inflammatory and autoimmune disorders. Given its influence on
the processes of inflammation and immunity, it is being studied for conditions such as rheumatoid
arthritis, inflammatory bowel disease, and multiple sclerosis. The specific action on NK1 receptors
suggests potential modification of immune cell activity and cytokine release, crucial factors in the
pathogenesis of these diseases. By potentially modulating inflammatory responses, (Pyr5)-Substance P
(5-11) may alleviate symptoms and alter disease progression, offering a novel approach to treatment
paradigms currently dominated by broad-based immunosuppressive therapies.
Additionally,
psycho-behavioral disorders, including depression and anxiety, have attracted research interest due to
the peptide’s involvement in stress and emotional processing. (Pyr5)-Substance P (5-11) might influence
neurotransmitter systems involved in mood regulation, presenting an alternative for treating affective
disorders. This aligns with the increased focus on understanding the gut-brain axis and how neuroactive
peptides like Substance P derivatives might influence both gastrointestinal and emotional health. Hence,
(Pyr5)-Substance P (5-11) serves as a versatile tool in research, potentially offering multifaceted
therapeutic benefits across pain management, inflammatory diseases, and mental health disorders,
transcending traditional treatment methodologies.
How does (Pyr5)-Substance P (5-11) compare to
full-length Substance P in terms of effectiveness and application?
(Pyr5)-Substance P (5-11)
represents a truncated and often more specialized version of the full-length Substance P peptide. The
modification in (Pyr5)-Substance P (5-11) often enhances the binding affinity and specificity for the
neurokinin-1 (NK1) receptor. This receptor is a critical mediator in processes such as pain perception,
stress responses, and inflammatory pathways. By tailoring the peptide structure, (Pyr5)-Substance P
(5-11) delivers potentially enhanced therapeutic benefits with fewer side effects. While full-length
Substance P can activate a broad range of physiological responses due to its interaction with all three
types of neurokinin receptors (NK1, NK2, NK3), (Pyr5)-Substance P (5-11) is focused predominantly on NK1
receptor pathways. This specificity can result in more targeted therapeutic outcomes, particularly in
disorders where NK1 plays a central role.
The nuanced difference in application also extends to
research focus areas. Full-length Substance P is widely studied in contexts of general pain, mood
disorders, and broad-spectrum inflammatory responses. Meanwhile, the modified (Pyr5)-Substance P (5-11)
may show greater promise in conditions where the precise regulation of the NK1 receptor could make a
significant impact. This includes targeted pain relief in neuropathic pain or focused intervention in
inflammatory bowel diseases, potentially providing a more tailored therapeutic model. The enhanced
receptor specificity might not only improve efficacy but also potentially reduce the likelihood of
adverse effects commonly associated with broader receptor activation. Additionally, the pharmacokinetic
and pharmacodynamic profiles of (Pyr5)-Substance P (5-11) might offer advantages over its full-length
counterpart. Often, such modified peptides exhibit improved stability and longer duration of action,
attributes that can result in improved patient compliance and therapeutic success in clinical
settings.
These distinctions underscore the potential of (Pyr5)-Substance P (5-11) as a more
refined option for treatments involving the neurokinin pathways, promising more efficient and safer
therapeutic strategies. By focusing on select mechanisms, it leverages the benefits of traditional
Substance P while innovating through reduced risk profiles and potentially superior clinical
outcomes.
What are the benefits and drawbacks of using (Pyr5)-Substance P (5-11) for pain
management?
Utilizing (Pyr5)-Substance P (5-11) in pain management presents both promising
advantages and notable considerations. One of the primary benefits lies in its specificity for the NK1
receptor. This specificity allows for targeted modulation of pain pathways, potentially alleviating pain
without the extensive side effects associated with traditional pain medications like opioids. The opioid
crisis has highlighted the urgent need for alternatives that do not carry the risk of addiction and
tolerance. By providing a mechanism of pain relief through a distinct pathway, (Pyr5)-Substance P (5-11)
could offer a safer, non-opioid option. Furthermore, because of its specific action, there may be fewer
systemic side effects, which is a significant improvement over non-steroidal anti-inflammatory drugs
(NSAIDs) that can affect gastrointestinal and cardiovascular systems.
However, (Pyr5)-Substance P
(5-11) is not without potential drawbacks. While promising, research is still in its early stages
compared to more established pain management therapies. This can lead to concerns about the long-term
safety and efficacy of the peptide. Many of the studies have been preclinical, with more extensive human
trials needed to fully ascertain its overall impact. Additionally, the cost of producing peptide-based
treatments can be higher than traditional small molecule drugs, potentially impacting accessibility and
affordability for patients. Also, its precise effectiveness can vary based on the type of pain and
individual patient response, necessitating careful calibration and potential combination with other
therapies to achieve optimal results.
Despite these challenges, (Pyr5)-Substance P (5-11) stands
as a burgeoning candidate in the realm of pain management, offering a novel approach that could redefine
how chronic and neuropathic pain is addressed. The ability to provide targeted relief with a favorable
side effect profile makes it a significant focus for ongoing research and development in pain
therapeutics. As the understanding of its pharmacology broadens, strategies to counteract current
limitations, such as cost and production, are likely to emerge, making it a viable alternative in modern
pain management landscapes.
What stage of research is currently being done on (Pyr5)-Substance P
(5-11), and what are its future prospects in clinical applications?
Research on (Pyr5)-Substance P
(5-11) is currently transitioning from exploratory preclinical studies towards early-stage clinical
trials. Initial investigations are focused on elucidating its pharmacological profile, with animal
models being crucial in understanding its therapeutic potential and safety. These studies are key in
demonstrating efficacy within controlled environments, observing impacts on various physiological and
pathological processes linked to NK1 receptor modulation. The transition to human clinical trials
represents an exciting phase where its potential benefits identified in preclinical stages are tested
for safety and efficacy in a patient setting.
As research progresses, its future prospects in
clinical applications are promising. For chronic pain management, (Pyr5)-Substance P (5-11) could emerge
as a radical development in non-opioid treatments, a crucial advancement given the current opioid
dependency crisis. Additionally, its application in inflammatory diseases represents significant
potential not only in reducing symptoms but also in impacting disease progression. With an increasing
focus on personalized medicine, the specificity of (Pyr5)-Substance P (5-11) might offer tailored
treatments for individuals based on their unique physiological responses, especially in diseases where
inflammation plays a critical role.
Furthermore, collaborations between academic institutions,
pharmaceutical companies, and regulatory bodies are anticipated to drive the research and development
forward. This multidisciplinary approach will ensure a robust pipeline from basic research to potential
clinical application. Researchers are keen on uncovering additional receptor interactions and
delineating metabolic pathways which could improve the peptide’s application across a broader array of
disorders, enhancing its therapeutic versatility.
With ongoing advancements in peptide synthesis
and bioengineering, (Pyr5)-Substance P (5-11) could leverage cutting-edge techniques to improve its
stability, delivery, and cost-effectiveness. While there remains a journey to full clinical adoption,
the potential for (Pyr5)-Substance P (5-11) as a therapeutic agent is strong, buoyed by increasing
investment and scientific interest. Ongoing research aims to address current limitations and fully
establish its role in modern therapeutic mangement, offering new hope across a spectrum of diseases with
unmet clinical needs.