Synonym |
(D-Arg1,D-Phe5,D-Trp7,9,Leu11)-Substance P |
Species |
Human |
Protein Accession |
P20366 |
Purity |
≥95% |
Endotoxin Level |
<1.0 EU per 1 μg of the protein |
Biological Activity |
The ED50 is <2.5 nM |
Expression System |
Chemical Synthesis |
Fusion Tag |
None |
Predicted Molecular Mass |
1262.5 Da |
Formulation |
Lyophilized from a 0.2 μm filtered solution in Acetonitrile and TFA |
Reconstitution |
It is recommended to reconstitute the lyophilized product in 10 mM HCl at a concentration of 1
mg/ml, which can then be further diluted to other aqueous solutions |
Storage & Stability |
Store lyophilized protein at -20°C. Reconstituted protein can be stored at 4°C for a limited
period of time. Please avoid freeze-thaw cycles. |
FAQ
What is (D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P and what are its potential
benefits?
(D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P is a synthetic peptide analog of the
naturally occurring neuropeptide Substance P. This modified peptide has been developed to alter the
receptor binding characteristics and enhance the therapeutic potential of Substance P. As researchers
have advanced in the study of neuropeptides, Substance P has shown promise in a variety of areas
including pain management, inflammatory conditions, and mental health disorders. The modified version,
(D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P, is designed to improve the stability and efficacy of the
compound for potential therapeutic applications.
The substance operates primarily by interacting
with the neurokinin-1 (NK1) receptor, one of the key receptors in the transmission of pain signals, as
well as in various physiological processes such as stress and inflammation. By acting on this receptor,
(D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P possesses the ability to modulate these pathways, making it a
subject of interest for researchers focusing on chronic pain management or inflammatory
diseases.
The therapeutic potential of this peptide extends beyond just pain relief. Due to its
action on the central nervous system, it is being explored for anxiolytic effects, potentially offering
new hope for patients suffering from anxiety disorders. The relationship between Substance P and mood
regulation pathways also opens up avenues for its use in treating depression and stress-related
disorders.
Additionally, inflammation modulation is a significant aspect of what
(D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P brings to the table. Chronic inflammatory diseases, such as
arthritis and inflammatory bowel disease, might benefit from its ability to regulate immune responses
and decrease inflammatory markers. These anti-inflammatory actions could result in improved quality of
life for patients suffering from conditions characterized by chronic inflammation.
It is
important to note, however, that while the capabilities are promising,
(D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P is still under investigation in clinical settings. Successful
applications in animal models and initial human trials are encouraging but require more extensive
research to fully validate these benefits. Researchers are also exploring its potential in other areas
like cancer research, where its modulatory effects on cell growth and immune evasion are of particular
interest.
How is (D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P administered in research
settings?
In research settings, (D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P is typically
administered through various methods depending on the specific context of the study, the desired speed
of action, and the targeted site within the body. The administration route is a crucial consideration
because it impacts the bioavailability, the speed at which the compound begins to work, and the overall
efficacy of the effects being studied.
One of the common methods of administration is intravenous
injection, as it allows for direct entry into the bloodstream, which can provide quick onset of action.
This method is particularly useful in acute studies where immediate effects are necessary, such as in
pain management trials or studies examining the immediate physiological responses to the peptide. By
circumventing the digestive system, intravenous administration also prevents the degradation of the
compound, ensuring that the full dosage reaches the system.
Another method utilized, especially
in preclinical research, is intraperitoneal injection, where the peptide is introduced into the
peritoneal cavity. This route is often used in animal studies due to its simplicity and effectiveness in
allowing systemic absorption. The ease of administration in laboratory settings makes it a popular
choice for initial in vivo studies assessing a wide range of potential therapeutic actions of
(D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P.
In experimental scenarios focused on the central
nervous system, direct intracerebroventricular injection might be employed. This technique involves
administering the substance directly into the cerebrospinal fluid, which bathes the brain, allowing
direct interaction with central receptors like NK1. This method is particularly insightful for studies
targeting neuroinflammatory responses or central pain pathways, as it provides access to the brain with
minimal systemic interference.
Topical application is another method being explored, especially
for localized inflammatory conditions or skin-related studies. This route offers the advantage of
directly targeting the affected area, thereby minimizing systemic exposure and potential side effects.
Transdermal patches or creams containing the peptide are examples of how this method can be applied in a
controlled manner to study local effects.
Finally, oral administration is generally less common
due to potential degradation by the digestive enzymes and the possibility of reduced bioavailability.
However, advancements in formulation technology, such as encapsulation or liposomal delivery systems,
are being investigated to facilitate oral administration that circumvents these
limitations.
While these methods offer various advantages, it is important to align the
administration route with the research goals and the biological characteristics of
(D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P. Each method provides unique insights and enables researchers
to explore the diverse therapeutic potentials of this compound effectively in different
contexts.
What current research is being conducted on (D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance
P?
Current research on (D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P encompasses a broad array of
scientific inquiries aimed at elucidating its full therapeutic potential across various medical fields.
As a derivative of the naturally occurring neuropeptide Substance P, this analog has garnered
significant attention for its enhanced stability and efficacy in modulating the neurokinin-1 (NK1)
receptor, a key player in pain sensation, mood regulation, and inflammatory responses.
One of the
primary areas of research involves its application in pain management. Chronic pain conditions, such as
neuropathic pain and fibromyalgia, cause significant distress and are notoriously difficult to manage
with existing medications. Researchers are investigating the potential of
(D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P to provide effective relief by modulating pain pathways at
the central and peripheral levels. Through animal models and early-phase human trials, studies aim to
assess its efficacy in reducing pain intensity, frequency, and associated symptoms compared to
conventional treatments. Understanding how this peptide can effectively alter pain signaling without
severe side effects could revolutionize pain management strategies.
Another significant research
avenue is its role in mood and anxiety disorders. Given its interaction with central nervous system
pathways involving depression and anxiety, studies are exploring its anxiolytic and antidepressant
capabilities. Researchers are conducting preclinical and clinical trials to see if it can serve as a
standalone treatment or in conjunction with existing therapies to enhance efficacy and patient outcomes.
These studies look at not only symptomatic relief but also the potential for better treatment adherence
and improved quality of life for patients struggling with these disorders.
Inflammatory diseases
are another key focus area. The modulation of immune responses and the inhibition of specific
inflammatory markers by (D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P present promising implications for
conditions such as rheumatoid arthritis and inflammatory bowel disease. Research efforts aim to clarify
how this peptide can decrease chronic inflammation and prevent tissue damage. Trial results could lead
to novel treatments that present fewer complications than current anti-inflammatory drugs.
Beyond
these applications, exploratory research is examining its potential role in cancer therapy.
Investigators are interested in its effects on tumor growth regulation, immune evasion, and possibly
enhancing the efficacy of established cancer treatments. While these studies remain largely in the
experimental phase, they signify the peptide's versatile potential in tackling complex, multifaceted
diseases.
Finally, research is continuously expanding to include other potential applications,
such as neurodegenerative diseases like Alzheimer's and Parkinson's. The role of neuropeptides in neural
protection and repair provides an intriguing basis for these studies, aiming to uncover neuroprotective
strategies that could slow disease progression and enhance patients’ cognitive function and overall
quality of life.
What are the known side effects and safety considerations associated with
(D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P?
As with any therapeutic agent undergoing research and
development, it is crucial to thoroughly understand the potential side effects and safety considerations
associated with (D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P. While it offers promising therapeutic
benefits due to its interaction with the NK1 receptor system and its subsequent physiological effects,
comprehensive studies are needed to assess its safety profile.
During preclinical studies, some
common side effects have been observed in animal models, which researchers are monitoring closely as the
compound progresses through the pipeline of clinical trials. These side effects may include mild local
reactions at the injection site, which are typical of many compounds administered via injection and
generally resolve without intervention. Additionally, systemic reactions, such as minor changes in blood
pressure or heart rate, have been noted, emphasizing the need for continuous monitoring of
cardiovascular parameters, especially during early human trials.
In the central nervous system,
where (D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P exerts much of its action, potential side effects
include alterations in mood or behavior. Given its interaction with pathways related to anxiety and
depression, while these changes might benefit disorders of these kinds, there is a risk of exacerbating
symptoms in certain populations, which necessitates cautious dose titration and patient
evaluation.
Immunomodulatory effects bring about another set of considerations. While the
substance’s ability to modulate inflammatory responses holds potential therapeutic advantages, it could
inadvertently dampen necessary immune functions, increasing the risk of infections. Therefore,
individuals with compromised immune systems or those on immunosuppressive therapies must be carefully
assessed before being considered for treatments involving this peptide.
Long-term safety data is
still in development; hence, the potential for unforeseen side effects exists, supporting the need for
extended follow-up periods in clinical studies. Monitoring organ function, especially liver and kidneys,
is crucial as these organs are key to metabolizing substances and clearing them from the body. Extended
use or high doses might impose additional metabolic stress, which requires consideration in dosing
regimens and patient selection.
In clinical trials, special attention is given to
population-specific responses, including children, the elderly, and those with existing comorbidities,
to establish a comprehensive safety profile. This tailored approach aims to identify any unique risks
present within diverse demographic groups, enhancing the overall understanding of who might benefit most
from the therapy while minimizing potential harm.
Ultimately, while
(D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P shows significant therapeutic promise, continued commitment
to rigorous safety and efficacy assessment through well-designed clinical trials remains essential. With
advancement in research methodologies and commitment to patient safety, the comprehensive risk-benefit
profile for this promising compound can be better defined.
Are there any ongoing clinical trials
involving (D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P?
The landscape of clinical trials for
(D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P is dynamic, reflecting the broad interest in its therapeutic
potential across multiple medical disciplines. Currently, several ongoing trials are investigating its
application in various conditions, marking significant steps toward understanding its efficacy and
safety within human populations.
One area of active clinical research is chronic pain management.
Trials are underway exploring its utility in alleviating pain symptoms in patients with conditions such
as neuropathic pain, fibromyalgia, and arthritis. These studies are meticulously designed to evaluate
its pain-reducing capabilities compared to current treatments, assessing parameters such as pain
intensity reduction, improvement in function, and quality of life indicators. The studies often stratify
participants based on factors like pain duration, intensity, and previous treatment responses to tailor
therapeutic approaches more accurately.
Concurrently, researchers are investigating its potential
in treating mood disorders, including depression and anxiety. Clinical trials are focusing on its impact
on reducing anxiety symptoms, enhancing mood stability, and assessing its ability to complement existing
antidepressant therapies. This research is pivotal in understanding how
(D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P might modify or enhance neurotransmitter pathways associated
with mood regulation.
Trials in inflammatory diseases are examining its capacity to reduce
systemic and localized inflammation. These studies typically involve patients with rheumatoid arthritis
or inflammatory bowel disease, conditions notoriously difficult to manage with existing options. The
trials measure its effectiveness in reducing inflammatory biomarkers and alleviating clinical symptoms
while monitoring for any adverse immune responses.
In addition, exploratory trials are assessing
its role in oncology, particularly in managing cancer pain and potentially improving responses to
conventional therapies. These early-phase studies aim to establish initial safety and efficacy, as well
as determine the most suitable administration routes and dosages for tumor management and patient
comfort.
Neurodegenerative disease research is another frontier, with trials focusing on
conditions such as Alzheimer's and Parkinson’s disease. These studies are evaluating whether
(D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P can slow disease progression, improve cognitive function, or
enhance patient quality of life due to its neuroprotective mechanisms.
Overall, these diverse
clinical trials are critical in paving the way for potential regulatory approval and therapeutic use of
(D-Arg1,D-Phe5,D-Trp7–9,Leu11)-Substance P. By thoroughly assessing its benefits and risks across
various conditions, researchers aim to unlock its full potential, bringing forth new, innovative
treatment options that address the growing need for effective, targeted therapies in modern medicine.
These efforts represent a concerted push towards integrating this promising compound into therapeutic
regimens, driven by the need for enhanced patient outcomes and improved quality of life across multiple
diseases.