Synonym |
Sar9,Met(O2)11-Substance P |
Species |
Human |
Protein Accession |
P20366 |
Purity |
Greater than 95% as determined by SEC-HPLC |
Endotoxin Level |
Less than 1 EU/μg as determined by LAL method |
Biological Activity |
The biological activity is determined by the ability to induce calcium flux in RBL-2H3 cells and
is typically between 2-10 ng/mL |
Expression System |
E. coli |
Fusion Tag |
His tag at N-terminus |
Predicted Molecular Mass |
Approximately 1.6 kDa |
Formulation |
Lyophilized from a 0.2 μm filtered solution of 20mM PB,150mM NaCl,pH 7.2 |
Reconstitution |
Centrifuge vial before opening. When reconstituting the product, gently pipet and wash down the
sides of the vial to ensure full recovery of the protein into solution |
Storage & Stability |
Store at -20°C. Aliquot and store at -80°C for long-term storage. Avoid repeated freeze-thaw
cycles. |
FAQ
What is (Sar9, Met(O2)11)-Substance P and how does it function in the body?
(Sar9,
Met(O2)11)-Substance P is a synthetic analog of the naturally occurring neuropeptide Substance P, which
is part of the tachykinin family of peptides. It has been specifically modified at the 9th and 11th
positions with sarcosine (Sar) and oxidized methionine (Met(O2)), respectively. These modifications are
intended to enhance its stability and binding affinity, making it more potent in its biological
activity. Substance P is primarily known for its role in transmitting pain and inflammatory signals in
the central and peripheral nervous systems. It exerts these effects by binding to the neurokinin-1 (NK1)
receptors, which are widely distributed in both the brain and other tissues throughout the body. By
binding to these receptors, Substance P can influence a variety of physiological processes, including
mood regulation, stress responses, and immune function.
The analog (Sar9, Met(O2)11)-Substance P
specifically interacts with the NK1 receptor with greater efficacy, leading to stronger and potentially
longer-lasting responses compared to its natural counterpart. This can be crucial in research and
therapeutic contexts where enhanced receptor activation is desired. The modified peptide is particularly
useful in experimental studies focusing on neurogenic inflammation, pain pathways, and other conditions
related to NK1 receptor activity. Researchers find it beneficial for exploring the mechanisms of chronic
pain syndromes, as its robust interaction with NK1 receptors can help elucidate how neuronal pathways
modulate pain perception and response. Additionally, the detailed investigation into its effects on mood
and stress-related disorders is of significant interest, as alterations in Substance P levels and
function have been implicated in conditions such as depression, anxiety, and PTSD. Through this enhanced
form of Substance P, scientists aim to better understand its comprehensive role in neurobiological
processes, paving the way for potential new therapeutic approaches that target these critical pathways.
Ultimately, the use of (Sar9, Met(O2)11)-Substance P represents a significant advancement in
neuropeptide research, offering researchers a powerful tool to dissect the complex interactions between
neurotransmission, pain modulation, and emotional regulation.
What are the potential benefits of
using (Sar9, Met(O2)11)-Substance P in scientific research?
The utilization of (Sar9,
Met(O2)11)-Substance P in scientific research presents numerous advantages, particularly in
understanding the vast and complex roles of neuropeptides in human physiology. First and foremost, this
analog offers enhanced stability and binding affinity compared to natural Substance P, which means it
can engage more effectively with NK1 receptors. This property is particularly advantageous when
conducting studies that aim to mimic or amplify natural biological processes, as researchers can obtain
more consistent and reliable results. Enhanced receptor binding also allows for a more detailed study of
the downstream effects triggered by NK1 receptor activation, opening avenues for deeper insights into
various biological pathways.
One of the primary areas of interest is pain management. With the
ongoing challenges in treating chronic pain, there is a significant interest in exploring new pathways
that could offer safer and more effective treatments. (Sar9, Met(O2)11)-Substance P provides researchers
with an opportunity to investigate how activating NK1 receptors more potently and precisely might lead
to novel pain management strategies. This is particularly relevant in conditions such as fibromyalgia,
chronic migraines, and neuropathic pain, where conventional treatments often fall short. Moreover, the
analog's potential to further elucidate the role of Substance P in neurogenic inflammation is
invaluable, as this could lead to breakthroughs in understanding inflammatory diseases and developing
anti-inflammatory drugs.
Another promising frontier is mental health research. Given the
implication of Substance P in mood regulation and stress responses, exploring the effects of its more
potent analog could significantly enhance our understanding of psychiatric conditions. Researchers can
delve into how modulations in Substance P activity influence mood disorders such as depression and
anxiety. This insight might lead to alternative therapeutic targets, especially for patients who do not
respond to traditional treatments. Besides, detailed studies could shed light on how Substance P and its
analogs impact neurodevelopment and neuroplasticity, further widening the scope of potential
applications.
Lastly, the use of (Sar9, Met(O2)11)-Substance P holds promise for advancing drug
development. By comprehensively understanding its action, researchers can better predict how similar
molecules might behave in the human body, potentially leading to the development of more effective drug
candidates. This process of learning from nature, while enhancing the stability and efficacy of
biological molecules, demonstrates a sophisticated approach to drug design and therapy. Overall, the
introduction of such a potent analog of Substance P into research paradigms invites exciting progress
across multiple domains, making it an invaluable tool in modern scientific inquiry.
Are there any
known side effects or risks associated with (Sar9, Met(O2)11)-Substance P?
As with any biologically
active compound, understanding the potential side effects and risks associated with (Sar9,
Met(O2)11)-Substance P is crucial, particularly for its safe use in research settings and any future
therapeutic applications. Due to the nature of its action—specifically its potent interaction with NK1
receptors—researchers must thoroughly assess both the desired and undesired physiological responses
resulting from its administration. One of the primary considerations is based on its mechanism of action
through the NK1 receptors, which are implicated in various bodily responses, including pain
transmission, stress, and emotional regulation. While enhanced receptor binding can be beneficial for
targeted outcomes, such as pain relief or mood regulation, there is the possibility of overstimulation
or dysregulation of these pathways.
Potential side effects might mirror those observed with
excessive stimulation of natural Substance P receptors, such as increased sensitivity to pain or
heightened inflammatory responses. As research into analogs like (Sar9, Met(O2)11)-Substance P is still
developing, much of the concern focuses on theoretical risks of exacerbating conditions such as chronic
pain, migraines, or inflammatory diseases, if not calibrated correctly. Additionally, as Substance P is
known to play a role in mood and anxiety, unregulated application could potentially lead to mood
disturbances or exacerbated stress responses. These effects would need careful monitoring in any
therapeutic or experimental contexts, ensuring that dosages are optimized to achieve desired benefits
without triggering adverse reactions.
Another consideration is the immune system modulation
aspects of NK1 receptor activity. Substance P has been noted for its role in immune responses,
suggesting the possibility that its analogs could influence immune function either beneficially or
detrimentally. Overactivity could potentially lead to autoimmune-like responses, while inadequate
activity might suppress normal immune responses. Hence, any comprehensive application of (Sar9,
Met(O2)11)-Substance P in research or treatment scenarios would necessitate a thorough understanding of
these dynamics, including dose-response relationships and long-term effects.
Moreover, the
specificity of its action in different tissues is crucial, given that NK1 receptors are distributed
throughout the body, including the central nervous system and peripheral organs. This widespread
presence necessitates comprehensive studies to determine if there's differential sensitivity or response
in various tissues, which could present challenges in targeting specific systems without affecting
others adversely. Taken together, while (Sar9, Met(O2)11)-Substance P holds significant promise for
advancing scientific understanding and potential therapeutic innovation, careful consideration of
dosage, administration routes, and patient or subject monitoring is essential to mitigating any side
effects or risks associated with its use.
How does (Sar9, Met(O2)11)-Substance P compare to other
pain relief options?
Analyzing the efficacy and application of (Sar9, Met(O2)11)-Substance P in
comparison to traditional pain relief options requires a nuanced understanding of how different
compounds affect pain pathways. Unlike conventional non-steroidal anti-inflammatory drugs (NSAIDs) or
opioids, which operate via more generalized mechanisms, (Sar9, Met(O2)11)-Substance P offers a targeted
approach by primarily interacting with NK1 receptors. This specificity allows it to modulate pain at the
level of neurotransmitter regulation directly associated with inflammation and nociception (the sensory
perception of pain). As a result, it provides a unique prospective advantage, especially in dealing with
pain types where other medications might not be as effective or where chronic administration leads to
significant side effects.
NSAIDs, for example, function by inhibiting enzymes involved in the
production of prostaglandins, which are mediators of inflammation and pain. While effective for minor
pain and inflammation, they do not target the central nervous pain pathways and can lead to
gastrointestinal, kidney, or cardiovascular issues when used long-term. On the other hand, opioids bind
to specific receptors in the brain and spinal cord to block pain perception. Despite their potency,
opioids carry a high risk of addiction, tolerance, and significant side effects like respiratory
depression, making them less desirable for long-term management of chronic pain.
In contrast,
(Sar9, Met(O2)11)-Substance P offers a potential alternative by impacting the nociceptive pathways more
directly. Substance P and its analogs are pivotal in transmitting pain from peripheral tissues to the
central nervous system. By modulating NK1 receptor activity specifically, researchers hope to develop a
mechanism that curtails chronic pain signaling without the systemic effects associated with NSAIDs or
the addiction potential seen with opioids. Additionally, its use in the regulation of neurogenic
inflammation presents therapeutic avenues in conditions like arthritis, migraines, and neuropathic pain,
where typical treatments might fall short.
Potential comparative advantages also include reduced
systemic effects and possibly lower chances of developing tolerance or dependence, given its role as
part of the body’s natural pain management system rather than as an external suppressor of pain signals.
However, this also hinges on understanding its full pharmacokinetic and pharmacodynamic profiles, which
remain under investigation.
In conclusion, while research is ongoing to determine the full
efficacy and safety profile of (Sar9, Met(O2)11)-Substance P compared to established pain relief
options, the distinct and specific mechanisms it represents point toward a promising advancement in pain
management therapies. The exploration of this analog highlights a crucial shift towards more precise and
potentially safer therapeutic interventions that could complement or even replace existing medications,
offering better tailored and patient-specific solutions in the process. Nevertheless, comprehensive
clinical trials and studies are vital to fully validate these benefits and understand any limitations
associated with its use.
What are the implications of (Sar9, Met(O2)11)-Substance P on future
medical treatments?
The development and study of (Sar9, Met(O2)11)-Substance P herald significant
implications for future medical treatments, particularly in the realms of pain management,
neuropsychiatric disorders, and inflammatory conditions. As researchers continue to deepen their
understanding of this analog, its potential as a therapeutic agent becomes more apparent, propelling a
shift towards more targeted and specific medical interventions. With its enhanced binding affinity and
stability, (Sar9, Met(O2)11)-Substance P offers a promising alternative to conventional treatment
modalities that often come with significant limitations, such as side effects and limited
efficacy.
One of the most promising implications lies in the treatment of chronic pain.
Traditional analgesics like NSAIDs and opioids, while effective, are fraught with challenges, including
systemic side effects, risk of addiction, and tolerance development. By providing a more focused
approach through the modulation of NK1 receptors, (Sar9, Met(O2)11)-Substance P could lead to pain
relief methods that are both effective and minimize these common pitfalls. Its specific action might
offer relief to patients suffering from complex pain syndromes—such as fibromyalgia, chronic neuropathic
pain, and intractable migraines—where current treatments are inadequate. This would represent a
significant advancement in chronic pain management, improving quality of life for many
patients.
In addition to pain management, the implications of (Sar9, Met(O2)11)-Substance P
extend to psychosocial health. Substance P has been implicated in mood and anxiety disorders, with
altered levels observed in conditions such as depression and PTSD. As such, the analog could play a
pivotal role in the development of novel psychopharmacological treatments that harness its regulatory
effects on mood and emotional states. This offers hope for patients who may not respond well to
traditional antidepressants or anxiolytics, providing a tailored approach to managing mental
health.
Moreover, given its involvement in inflammatory processes, (Sar9, Met(O2)11)-Substance P
could contribute to the treatment of various inflammatory and autoimmune disorders. Its ability to
modulate NK1 receptor pathways may help in devising interventions that control inflammation without
suppressing the immune system as a whole, a common downside of many current therapies. Such targeted
treatment could revolutionize how conditions like rheumatoid arthritis, multiple sclerosis, and other
inflammatory diseases are managed, reducing reliance on broad-spectrum anti-inflammatory drugs and
corticosteroids.
Finally, this analog may also pave the way for the discovery and development of
other tachykinin-based therapies. By understanding its action and potential in clinical settings,
scientists can explore similar modifications in other neuropeptides, leading to a new class of
therapeutic agents. These advancements could create a ripple effect, influencing drug development
processes across various fields in pharmacology and biomedicine.
Overall, the implications of
(Sar9, Met(O2)11)-Substance P on future medical treatments are profound, offering innovative solutions
to some of the most challenging conditions faced in modern medicine. Its progression from laboratory
research to clinical application could lead to breakthroughs that not only enhance therapeutic efficacy
but also improve the overall safety and specificity of treatment regimens, setting a new standard in
personalized medicine and patient care.