Synonym |
Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se |
Species |
Human |
Protein Accession |
P20366 |
Purity |
≥ 95% |
Endotoxin Level |
< 1.0 EU per 1 μg of protein |
Biological Activity |
Not determined |
Expression System |
Chemical synthesis |
Fusion Tag |
Not applicable |
Predicted Molecular Mass |
818.96 Da |
Formulation |
Lyophilized from a 0.2 μm filtered solution in Acetonitrile and TFA |
Reconstitution |
Reconstitute in water to a concentration of 0.1-1.0 mg/ml |
Storage & Stability |
Store at -20°C upon receipt, stable for up to 3 months at -20°C |
FAQ
What is Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se and how does it work at a molecular
level?
Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se is a synthetic peptide derived from the
modification of Substance P, a neuropeptide known for its role in pain perception and modulation of
inflammatory processes. The derivative peptide specifically modifies the natural structure of Substance
P to potentially enhance or alter its biological activity. This modification is achieved through the
incorporation of specific amino acids and other molecular constituents, such as the succinyl group and
N-methylphenylalanine, which can change the binding efficiency and selectivity of the peptide to its
target receptors.
At the molecular level, Substance P typically exerts its effects by binding to
neurokinin receptors, which are part of the G-protein coupled receptor family, particularly the NK1
receptor. These receptors are distributed in various tissues, including the central nervous system and
peripheral tissues, playing a crucial role in transmitting pain signals and regulating inflammatory
responses. By altering the natural sequence of Substance P, Succinyl-(Asp6,N-Me-Phe8)-Substance P
(6-11), Se might display different binding affinities or potencies at these receptors, potentially
offering varied therapeutic benefits or research applications.
The modifications also mean that
the peptide may experience altered pharmacokinetics and metabolism in biological environments. This can
influence how the peptide is absorbed, distributed, metabolized, and excreted by the body, which is
crucial for determining its efficacy and side effect profile. Researchers utilize such modified peptides
to explore new therapeutic avenues, understand receptor-ligand interactions better, and develop
innovative treatments for conditions related to the modulation of Substance P activity, such as chronic
pain, depression, inflammation, and emesis. Understanding these interactions at a molecular level is
vital for translating these insights into clinical applications or further drug
development.
Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se also provides a valuable tool in
experimental pharmacology and neuroscience, allowing scientists to probe the principles of
peptide-receptor interactions and the downstream signaling pathways activated upon receptor binding. The
study of these pathways enables deeper insights into physiological and pathophysiological processes,
fostering the development of new strategies to manipulate pain pathways and treat related
disorders.
What potential applications does Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se have
in clinical research or therapy?
The potential applications of
Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se in clinical research or therapy are vast, primarily
revolving around its ability to provide insights into pain modulation, inflammatory responses, and
various neurological conditions. Given its foundation in the structure of Substance P, this modified
peptide serves as a vital tool for exploring new treatment paradigms and enhancing our understanding of
physiological and pathophysiological processes associated with the neuropeptide system.
One
significant application area is in pain management research, where Succinyl-(Asp6,N-Me-Phe8)-Substance P
(6-11), Se can be used to study its potential as a modulator of pain pathways. Chronic pain, an area
that often suffers from inadequate treatment options, can benefit from novel insights and therapies
derived from understanding how modifications to Substance P affect pain transmission and perception. By
potentially altering interaction dynamics with the NK1 receptor, researchers can identify pathways to
modulate the pain signal differently, leading to the development of new analgesics with potentially
fewer side effects than traditional opioid treatments.
In the realm of neuroinflammation, this
peptide offers research opportunities into conditions such as multiple sclerosis, a disease
characterized by the inflammation of the central nervous system. Studying the effects of
Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se may contribute to a better understanding of the
inflammatory processes mediated by Substance P, thus guiding the development of therapeutic
interventions that target neuroinflammatory signaling cascades more effectively.
Additionally,
the research into psychiatric disorders such as depression and anxiety can be advanced through studies
utilizing this peptide. Substance P and the NK1 receptor have been implicated in the pathophysiology of
these disorders, particularly concerning stress and emotional regulation. By examining how modified
peptides interact with these systems, novel therapeutic strategies could emerge that provide relief for
individuals for whom traditional antidepressants are ineffective.
Furthermore, in the field of
oncology, there is an emerging interest in understanding how Substance P and its receptors may
contribute to cancer proliferation and metastasis. Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se
could thus be pivotal in uncovering mechanisms by which cancer cells leverage Substance P signaling
pathways to promote tumor growth and survival. This research could pave the way for discovery of
targeted therapies that disrupt these processes and improve outcomes for cancer patients.
In
conclusion, Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se holds promise across multiple domains in
clinical research and therapeutic development, serving as a platform for advancing our understanding and
treatment of several complex medical conditions. Through continued exploration and study of this
peptide, significant strides could be made in designing innovative interventions that address unmet
medical needs across various therapeutic areas.
How does Succinyl-(Asp6,N-Me-Phe8)-Substance P
(6-11), Se differ from natural Substance P, and what are the benefits of these
differences?
Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se is distinctly different from
natural Substance P due to its modified peptide structure, which leads to distinct pharmacological
properties and potential effects. Natural Substance P is an undecapeptide that plays a role in the
regulation of pain and inflammation, functioning primarily through its interaction with the NK1
receptor, a G-protein coupled receptor. In contrast, Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se
introduces modifications designed to alter these interactions strategically.
One of the critical
differentiators is the incorporation of the succinyl group and N-methylphenylalanine (N-Me-Phe) into the
peptide chain. These modifications can significantly influence the peptide's binding affinity and
selectivity for the NK1 receptor. For example, substituting N-Me-Phe can enhance steric interactions
with the binding pocket of the receptor, potentially increasing selectivity and reducing off-target
interactions that could lead to adverse effects.
Beyond receptor affinity, these structural
changes can impact the stability and metabolism of the peptide in biological systems. The natural
degradation of peptides by endogenous enzymes often limits the therapeutic utility of peptides derived
from natural sources. However, the introduction of non-natural amino acids, such as N-Me-Phe, can
increase the resistance of Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se to enzymatic degradation,
thereby prolonging its half-life and bioavailability in vivo. This increased stability is beneficial for
therapeutic applications, where sustained activity is desired to achieve optimal
outcomes.
Furthermore, the modification can alter the peptide's intrinsic activity, potentially
leading to agonistic or antagonistic effects on the NK1 receptor, depending on the nature of the
structural changes. Such alterations can be leveraged in therapeutic contexts where modulation of
receptor activity is required. For instance, if the peptide acts as an antagonist, it can be used in
settings where the inhibition of NK1 receptor signaling is desired, such as in treating nausea and
vomiting associated with chemotherapy.
Another advantage of these differences is the potential
for reduced immunogenicity compared to natural peptides. Peptide therapeutics can sometimes elicit
immune responses, leading to diminished efficacy over time or adverse reactions. Structural
modifications can mitigate this risk by altering epitopes that provoke immune
recognition.
Overall, the differences between Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se
and natural Substance P confer several benefits, including enhanced receptor selectivity, increased
stability, prolonged in vivo activity, and adjustable intrinsic activity. These advantages broaden the
peptide's potential applications in clinical research and therapeutic development, positioning it as a
versatile tool for exploring new avenues in treating pain, inflammation, and related
disorders.
What kind of research has been conducted on Succinyl-(Asp6,N-Me-Phe8)-Substance P
(6-11), Se, and what are the key findings?
Research on Succinyl-(Asp6,N-Me-Phe8)-Substance P
(6-11), Se encompasses various studies aimed at exploring its pharmacological properties, therapeutic
potential, and underlying mechanisms of action. This research has predominantly been conducted in
experimental settings, utilizing both in vitro and in vivo models to evaluate the peptide's effects and
applications.
One line of research has focused on elucidating the peptide's interaction with the
NK1 receptor, a critical target in the neuropeptide system. Studies have demonstrated that modifications
in Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se enhance its binding affinity and selectivity toward
the NK1 receptor. Such findings suggest that the peptide could efficiently modulate receptor activation,
leading to potential applications as an antagonist or agonist in various therapeutic contexts. These
studies have also revealed insights into the structural determinants of receptor-ligand interactions,
offering valuable information for designing new therapeutic agents targeting the NK1 receptor.
In
the context of pain management, research has explored the peptide's ability to influence pain
transmission pathways. Various animal models of pain have been used to investigate its analgesic
properties, with findings indicating that Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se can modulate
nociceptive signaling pathways, potentially reducing pain perception. This highlights its promise as a
candidate for developing new analgesics that offer an alternative to opioids, with potentially fewer
side effects and a lower risk of dependency.
Moreover, preclinical investigations have delved
into the peptide's role in modulating inflammatory responses. Studies have shown that
Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se can influence the expression of pro-inflammatory
cytokines and other mediators involved in inflammation, suggesting potential therapeutic implications in
conditions characterized by excessive inflammation, such as arthritis and other autoimmune
disorders.
Research has also extended to examining the peptide's effects on emotional and
psychiatric disorders, given the known involvement of Substance P and the NK1 receptor in conditions
like depression and anxiety. Preliminary studies indicate that modifying Substance P can influence
emotional regulation pathways, providing a basis for further exploration into its potential as an
adjunctive treatment for mood disorders.
Finally, efforts have been made to investigate the
peptide's role in cancer biology, particularly related to tumor growth and metastasis. Early findings
suggest that Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se could modulate pathways involved in cancer
cell proliferation, offering insights that could lead to the development of novel anticancer
strategies.
In summary, research on Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se has yielded
significant findings across several domains, highlighting its potential as a multifunctional agent in
therapeutic development. By advancing our understanding of its pharmacological properties and mechanism
of action, these studies pave the way for future investigations aimed at translating these insights into
clinical applications for managing pain, inflammation, psychiatric disorders, and cancer.
Are
there any known limitations or side effects associated with Succinyl-(Asp6,N-Me-Phe8)-Substance P
(6-11), Se?
While Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se offers promising therapeutic
potential, it is important to recognize and understand the limitations and potential side effects
associated with its use. As with any pharmacological agent, careful consideration of these factors is
critical to ensuring safe and effective application.
One of the primary limitations lies in the
early stage of research and development of this peptide. Although preclinical studies have demonstrated
promising results, further rigorous studies, including clinical trials, are necessary to fully evaluate
its efficacy and safety in humans. This limited clinical data means that any conclusions regarding its
therapeutic use must be made with caution until more comprehensive research is available.
In
terms of potential side effects, modified peptides like Succinyl-(Asp6,N-Me-Phe8)-Substance P (6-11), Se
may present challenges typical of peptide-based therapeutics. Despite structural modifications aimed at
increasing stability and reducing degradation, peptides can still be susceptible to enzymatic breakdown
in vivo. This degradation can lead to the rapid clearance of the peptide, potentially necessitating
frequent dosing to maintain therapeutic levels, which may not be feasible in all treatment
contexts.
Immune responses are another consideration, as the body's immune system can recognize
and respond to exogenous peptides, possibly triggering hypersensitivity reactions. Although
modifications can reduce immunogenicity, the risk of immune-related side effects remains and warrants
careful monitoring.
Off-target effects present another challenge. While structural enhancements
aim to increase selectivity for the NK1 receptor, there is a possibility of interactions with other
receptor systems or unintended biological pathways, leading to unwanted side effects. These interactions
could manifest as disruptions in physiological processes regulated by similar receptor families,
underscoring the importance of thorough selectivity profiling during preclinical
development.
Pharmacokinetic properties, such as absorption, distribution, metabolism, and
excretion, also present potential limitations. Peptides like Succinyl-(Asp6,N-Me-Phe8)-Substance P
(6-11), Se might face challenges related to bioavailability, particularly if intended for oral
administration, as the gastrointestinal tract's acidic environment can degrade peptide bonds.
Alternative routes of administration, such as intravenous or subcutaneous injections, might be
considered; however, these routes can impact patient compliance and convenience.
Lastly, cost and
manufacturing complexities are worth mentioning as potential hindrances. Peptide synthesis requires
advanced technologies, and large-scale production can be expensive, possibly affecting the accessibility
of therapies derived from such peptides.
In conclusion, while Succinyl-(Asp6,N-Me-Phe8)-Substance
P (6-11), Se holds considerable promise as a therapeutic agent, several limitations and potential side
effects must be carefully considered and addressed in future research and development phases. By
systematically overcoming these challenges, the therapeutic potential of this modified peptide can be
maximized for diverse applications, thereby contributing to the advancement of medical treatments across
various domains.