Synonym |
SP (4-11) |
Species |
Human |
Protein Accession |
P20366 |
Purity |
Greater than 95% by HPLC |
Endotoxin Level |
<1.0 EU per 1 μg of protein |
Biological Activity |
The ED50 as determined by the dose-dependent stimulation of IL-8 production by human PBMC is
less than 2 ng/ml. |
Expression System |
E. coli |
Fusion Tag |
N/A |
Predicted Molecular Mass |
1168 Da |
Formulation |
Lyophilized from a 0.2 μm filtered solution of 20% acetonitrile and 0.1% trifluoroacetic acid
|
Reconstitution |
Centrifuge the vial prior to opening. Reconstitute in water to a concentration of 0.1-1.0 mg/ml.
Do not vortex. |
Storage & Stability |
Store at -20°C. For long-term storage, store at -80°C. Once reconstituted, store at 4°C for up
to 7 days. Aliquot to avoid repeated freeze-thaw cycles. |
FAQ
What is Substance P (4-11) and what are its primary functions?
Substance P (4-11) is a specific
fragment of the larger peptide known as Substance P, a neuropeptide that plays a critical role in
transmitting pain information into the central nervous system. The importance of Substance P (4-11) lies
in its ability to elucidate particular segments of Substance P's action, especially in the context of
understanding pain pathways and neurogenic inflammation. This segment refers to a sequence of amino
acids (aa), and it is this sequence that is crucial for its binding affinity to the Neurokinin 1 (NK1)
receptor. The binding is responsible for triggering a cascade of events, primarily focusing on pain
perception, mood regulation, and inflammation.
Substance P is categorized under the group of
tachykinins, which are known for their ability to contract smooth muscles and influence the vascular
system. In understanding Substance P (4-11), researchers often focus on its roles independent of the
full-length Substance P peptide to unravel more specified functions or potential therapeutic angles. For
instance, its major function explored extensively in research is related to pain due to its predominant
presence and role in the nociceptive pathways. Its activities involve modulating the sensitivity of the
nervous system to pain stimuli.
When receptors in the nervous system are activated by Substance P
(4-11), they can modulate responses not only to pain but potentially in emotional responses and
inflammatory processes. This sequence is significant, as it may hold the key to developing targeted
inhibitors that can selectively bind to the NK1 receptors, thereby reducing undesirable effects
associated with chronic pain and inflammatory diseases. Researchers continually explore its specific
interactions and potential as a therapeutic target for conditions such as migraines, arthritis, and
certain mood disorders where Substance P's pathway may be implicated.
How does Substance P (4-11)
impact pain management and treatment research?
The impact of Substance P (4-11) on pain
management and treatment research is profound given its direct involvement in the body's pain pathways.
Research focusing on Substance P (4-11) aims to decipher its role in the transmission and modulation of
pain, particularly chronic pain, which remains a significant challenge in clinical settings. Its unique
interaction with the NK1 receptor is central to this research, as these receptors are among the primary
sites where pain signals are modulated in the nervous system.
Understanding how Substance P
(4-11) functions can pave the way for novel pain management strategies, particularly for chronic,
inflammatory, and neuropathic pain conditions. One of the promising research directions is the
development of NK1 receptor antagonists. By blocking Substance P (4-11) activity at these receptors,
these antagonists can potentially alleviate pain. Previous attempts to create such antagonists have
shown varying degrees of success in clinical trials, highlighting the complexity of pain pathways and
the need for continued research.
Moreover, the study of Substance P (4-11) also sheds light on
its role in acute pain situations and in stress-related disorders, where an overactive pain transmission
system might be at play. By regulating the Substance P pathways, researchers hypothesize a reduction in
exaggerated pain responses seen in chronic pain conditions.
Additionally, the regulatory role of
Substance P (4-11) in inflammatory conditions is a crucial area of interest. Inflammation often coexists
with pain, and Substance P acts as an important mediator linking the two. Research continues to explore
how modulating this peptide's function might reduce inflammation, thus providing another mechanism for
alleviating pain without relying solely on conventional analgesics. This direction in research
highlights an important shift towards understanding and leveraging the body's own peptides and receptors
in managing pain, rather than relying exclusively on external pharmaceuticals.
Substance P
(4-11)'s influence extends beyond pain management into the potential treatment of mood disorders such as
depression and anxiety, which are often comorbid with chronic pain. These insights not only promise
improvements in managing such conditions but also reflect a broader understanding of the
interconnectedness of pain and emotional states mediated by natural neuropeptides like Substance P and
its fragments.
What are the potential side effects or risks associated with targeting Substance P
(4-11) in therapeutic applications?
Targeting Substance P (4-11) in therapeutic applications
involves various considerations, primarily focusing on the potential side effects or risks associated
with manipulating neuropeptide pathways. While the modulation of Substance P (4-11) bears significant
therapeutic promise, this peptide's broad involvement in physiological processes necessitates a cautious
approach.
One of the potential risks in targeting Substance P (4-11), especially through the use
of NK1 receptor antagonists, is the off-target effects. These receptors are not solely involved in pain
transmission but also in mood regulation, stress responses, and even emesis (vomiting mechanisms).
Inhibiting Substance P's action can potentially lead to undesirable effects on these systems. For
instance, since Substance P is involved in stress and mood modulation, there is the risk that long-term
inhibition could potentially affect these aspects, potentially leading to mood alterations or changes in
stress response.
Additionally, since Substance P has a known role in immune response and
inflammatory processes, there's a concern that modifying its action could inadvertently dampen necessary
inflammatory responses, potentially impacting immune function. This alteration could lead to an
increased risk of infections or impaired wound healing, given that inflammation is a crucial component
of the body's defense and repair mechanisms.
Further, Substance P is implicated in
gastrointestinal function, especially in regulating gastric motility and secretion. Hence, modulating
its activity could pose the risk of gastrointestinal side effects, such as changes in secretion,
motility issues, or other digestive system irregularities.
Furthermore, the complexity of pain
pathways means that targeting one component, such as Substance P (4-11), might not address all aspects
of chronic pain, leading to incomplete relief or compensation through other pathways. This complexity
underscores the necessity for tailored therapeutic approaches that consider individual variability in
pain pathways and responses to treatment.
Lastly, as with any new therapeutic approach, there is
the overarching concern of long-term safety and effectiveness. The possibility of unforeseen effects
over prolonged periods remains a significant consideration and highlights the need for extensive
clinical trials to thoroughly assess the safety profile of therapeutic agents targeting Substance P
(4-11).
In conclusion, while targeting Substance P (4-11) presents innovative avenues for
treating pain and related conditions, it requires a meticulously balanced approach to mitigate potential
side effects and harness its therapeutic potential effectively. Ongoing research and clinical evaluation
remain critical in understanding and optimizing these therapeutic strategies.
In what ways is
Substance P (4-11) involved in mood regulation and emotional response?
Substance P (4-11) is
intricately involved in mood regulation and emotional responses due to its interaction with the NK1
receptor, which is widely expressed in the brain regions associated with emotional processing, such as
the amygdala and hippocampus. This neuropeptide fragment's relationship with mood is partly explained by
its presence and function in these areas, where it participates in complex neurotransmitter systems
involved in regulating affective states.
Research has indicated that Substance P and its
fragments, including Substance P (4-11), have a significant role in modulating stress and anxiety, which
are critical components of mood regulation. The interaction with NK1 receptors influences emotional
behavior and stress-related responses by affecting neurotransmitter release and receptor sensitivity.
For example, animal studies have demonstrated that blocking the NK1 receptor can produce antidepressant
and anxiolytic effects, suggesting its potential role in developing new treatments for mood
disorders.
Furthermore, Substance P is known to interact with the serotonergic system, which is
vital for maintaining mood balance. This interaction is particularly significant because imbalances in
serotonin levels are often linked to depression and anxiety disorders. By modulating serotonin release
and reuptake, Substance P (4-11) might indirectly influence the overall emotional state and contribute
to mood regulation. This mechanism is an active area of research with implications for the development
of targeted therapies for mood disorders.
Another interesting area of investigation is the role
of Substance P in response to stress. During heightened stress responses, Substance P levels may
fluctuate, impacting both behavior and emotional reactions. It seems to act as a biological marker of
stress levels, and its modulation could potentially adjust an individual's stress response, thus
presenting a novel strategy for controlling pathological anxiety or stress-related
disorders.
Additionally, clinical observations and experimental data have suggested a connection
between elevated Substance P levels and mood disorders in humans. Targeted therapies that modify
Substance P activity, including Substance P (4-11), are being examined for their potential to stabilize
mood and manage symptoms associated with depression and anxiety.
Understanding the precise
mechanisms underlying these actions is essential for developing more effective interventions that
leverage the modulation of Substance P activity. This insight not only enhances our comprehension of
mood disorders but also refines our approach to targeting the NK1 receptor pathway for therapeutic
benefits, offering promising prospects for those coping with mood-related conditions.
How has
research on Substance P (4-11) influenced the development of new pharmacological
treatments?
Research on Substance P (4-11) has significantly influenced the development of new
pharmacological treatments, particularly in areas of pain management, mood regulation, and inflammation.
By elucidating the specific roles and mechanisms of this peptide fragment within the broader context of
Substance P's biological activities, researchers have identified promising new targets for drug
development. This exploration was pivotal in devising more targeted therapies with potentially fewer
side effects as compared to broader-spectrum agents.
One of the most notable influences of
research in this area is the impetus it has given to developing NK1 receptor antagonists. These
antagonists directly block the receptor that Substance P (4-11) and other related peptides bind to,
which is crucial in modulating pain and inflammation. Several of these have made it into clinical
trials, with some already used as antiemetic drugs to prevent chemotherapy-induced nausea and vomiting,
endorsed by their effectiveness in modulating the NK1 receptor. Such triumphs underscore how pivotal
Substance P research is in translating basic scientific findings into clinical
applications.
Additionally, the exploration into the Substance P pathway has opened up new
avenues for antidepressant development. The implication of Substance P (4-11) in mood regulation through
its effect on NK1 receptors suggests possible new pharmacotherapeutic tools for managing depression and
anxiety disorders. Various pharmaceutical companies have pursued NK1 antagonists as potential new
classes of antidepressants and anxiolytics, driven by the novel mechanism that Substance P (4-11)
elucidates.
The challenges tackled in understanding the nuances of Substance P (4-11) have also
fueled advancements in developing more selective and specific drugs. By targeting only the critical
receptors or pathways associated with particular symptoms or diseases, these drugs can potentially
provide effective treatment with minimized adverse reactions. For instance, distinguishing the different
roles of full-length Substance P versus its smaller active segments like Substance P (4-11) enables the
refinement of such therapies to be more effective.
Moreover, ongoing research continues to
influence the identification of biomarkers associated with Substance P pathways, which can predict how
patients will respond to certain treatments. This represents a move toward personalized medicine, where
understanding the role of neuropeptides like Substance P at a granular level enables tailoring treatment
to the individual patient's biological makeup.
In summary, the comprehensive exploration of
Substance P (4-11)'s function and potential modulation offers a fertile ground for innovative drug
development, making significant strides towards targeted, effective, and minimally invasive treatments.
The enduring impact of this research underscores the important interconnections between molecular
biology, pharmacology, and clinical therapy in addressing complex health challenges.