Synonym |
Tyr8-Substance P |
Species |
Human |
Protein Accession |
P20366 |
Purity |
≥ 95% |
Endotoxin Level |
< 1 EU/μg |
Biological Activity |
Measured by its ability to induce calcium flux in HEK293 human embryonic kidney cells
co-transfected with the rat NK1 receptor. The ED50 for this effect is typically 3-15 nM. |
Expression System |
E. coli |
Fusion Tag |
None |
Predicted Molecular Mass |
1241.4 Da |
Formulation |
Lyophilized from a 0.2 μm filtered solution in Acetonitrile and TFA |
Reconstitution |
Centrifuge the vial prior to opening. Reconstitute in water to a concentration of 0.1-1.0 mg/ml.
|
Storage & Stability |
Store at -20°C. After reconstitution, store at -80°C. Stable for 3 months from the date of
receipt when stored at -20°C to -80°C. |
FAQ
What is (Tyr8)-Substance P and how does it work in the body?
(Tyr8)-Substance P is a modified
peptide that serves as an antagonist to the naturally occurring neuropeptide known as Substance P.
Substance P is part of the tachykinin neuropeptide family and plays a crucial role in transmitting pain
and other sensory signals within the central nervous system and peripheral nervous systems.
Specifically, it binds to the neurokinin 1 (NK1) receptor, which leads to various physiological
responses, including the transmission of pain signals. It is also involved in the inflammatory process
and can influence mood, anxiety, the vomiting reflex, and vasodilation. By acting as an antagonist,
(Tyr8)-Substance P inhibits the action of Substance P, thereby blocking its ability to bind to the NK1
receptor. This blocking action can mitigate pain transmission and reduce inflammatory responses.
For people who experience chronic pain conditions, the use of NK1 receptor antagonists like
(Tyr8)-Substance P can be a significant development. They can potentially alleviate pain symptoms by
preventing the pain signal transmission that Substance P facilitates. Additionally, in the context of
mood disorders and anxiety, since Substance P is known to influence emotional responses,
(Tyr8)-Substance P might hold promise for therapeutic action by modulating the same pathways.
Furthermore, beyond its applications in pain and mood regulation, there is growing interest in
researching its effects on emesis and other physiological responses, which could open avenues for
managing chemotherapy-induced nausea or other conditions related to the dysregulation of Substance P
activity.
What are the potential uses of (Tyr8)-Substance P in medical
treatments?
(Tyr8)-Substance P has garnered interest for its potential therapeutic uses across a
range of medical conditions, primarily due to its ability to antagonize the actions of Substance P. Some
of the most researched areas include pain management, particularly for chronic pain conditions such as
fibromyalgia, neuropathic pain, and osteoarthritis. Since these conditions are characterized by
prolonged pain signals that could potentially be mitigated via the inhibition of Substance P,
(Tyr8)-Substance P might offer a new mode of treatment. Patients suffering from chronic pain often face
significant challenges with existing treatments such as opioids, which can lead to dependency and other
side effects. In this context, (Tyr8)-Substance P represents a potentially safer and non-addictive
alternative.
In addition to pain management, (Tyr8)-Substance P is being examined for its
usefulness in treating mood disorders and anxiety. It is known that Substance P is implicated in the
modulation of stress and anxiety due to its presence in areas of the brain that regulate emotions, like
the amygdala and the hypothalamus. Therefore, by inhibiting the effects of Substance P, (Tyr8)-Substance
P could have anxiolytic or even antidepressant effects, offering a novel approach to managing these
conditions without the drawbacks associated with conventional medications.
Further potential uses
include its application in anti-emetic therapies. During chemotherapy, patients often suffer from severe
nausea and vomiting, a condition understood to be partly mediated by Substance P. By blocking its
action, (Tyr8)-Substance P could play a significant role in improving the quality of life for these
patients. Moreover, there is ongoing research to explore its effectiveness in other inflammatory
disorders, given its ability to modulate inflammatory processes. As research progresses, it is
anticipated that (Tyr8)-Substance P will be explored for additional therapeutic potentials, potentially
addressing unmet needs in various medical fields.
How does (Tyr8)-Substance P differ from other
pain management treatments?
(Tyr8)-Substance P offers several distinguishing features compared to
conventional pain management treatments, which generally include nonsteroidal anti-inflammatory drugs
(NSAIDs), acetaminophen, corticosteroids, and opioids. One of the primary differences is its mechanism
of action. Unlike NSAIDs and acetaminophen, which primarily focus on reducing inflammation and blocking
peripheral pain signals, and unlike opioids, which affect the central nervous system by stimulating
opioid receptors, (Tyr8)-Substance P works by specifically antagonizing the NK1 receptor that Substance
P binds to. This targeted action reduces the transmission of pain signals at a more foundational neural
level, potentially minimizing the sensation of pain without the broader impacts seen with other
medications.
Another significant difference lies in the side effect profiles. NSAIDs can lead to
gastrointestinal distress and cardiovascular issues with long-term use, while opioids are well-known for
their addictive properties and potential for abuse. Opioid addiction has become a significant public
health crisis, leading to heightened interest in alternative pain management options that bypass these
risks. (Tyr8)-Substance P, due to its non-opioid nature, avoids these addiction issues while still
providing an avenue for effective pain relief. It potentially offers a more favorable side effect
profile, which could improve patient compliance and broaden its applicability to individuals who are
unable to tolerate existing medications due to pre-existing conditions or the risk of adverse
reactions.
Moreover, while corticosteroids are effective for reducing inflammation, their
long-term use can result in immune suppression, thinning of the skin, and other systemic side effects.
In contrast, (Tyr8)-Substance P, by targeting specific neurotransmission pathways, could circumvent such
issues while providing relief from symptoms associated with chronic pain and inflammation. Its
specificity allows for highly targeted therapy, reducing the risk of ancillary effects and promoting
better management of chronic conditions that are otherwise treated with broader-spectrum
pharmaceuticals. Consequently, (Tyr8)-Substance P not only expands the current armamentarium for pain
management but does so with a promise for safer, more sustainable treatment regimens.
What
research has been conducted on (Tyr8)-Substance P, and what were the findings?
The research
surrounding (Tyr8)-Substance P has been quite vibrant, particularly concerning its potential
applications in pain management, mood disorders, and nausea control. A variety of preclinical studies
have been conducted, with animal models providing critical insights into its efficacy and safety
profile. These studies commonly demonstrate that (Tyr8)-Substance P significantly inhibits the NK1
receptor, an effect that results in the reduced perception of pain. Such outcomes underscore the
compound's potential utility in various chronic pain conditions, shifting the focus away from
traditional pain relief mechanisms that rely heavily on inflammatory mediators or opioids.
Beyond
preclinical studies involving pain, research also indicates that (Tyr8)-Substance P may be valuable for
mental health applications. Several experiments have delved into the anxiety-modulating effects of the
compound, leveraging its capacity to inhibit pathways associated with emotional regulation in the brain.
By targeting pathways that link Substance P to anxiety and stress responses, these studies suggest that
it could serve as a novel anxiolytic agent with a reduced risk of side effects compared to current
treatments, like benzodiazepines and selective serotonin reuptake inhibitors (SSRIs).
In
addition, research has indicated its potential efficacy in managing nausea and vomiting, particularly in
chemotherapy patients—a side effect often attributed to increased Substance P activity. Studies have
shown a reduction in chemotherapy-induced emesis in mouse models, bolstering the hypothesis that
(Tyr8)-Substance P could offer auxiliary support in cancer patient care, enhancing life quality and
treatment adherence by mitigating these debilitating side effects.
Human clinical trials, when
approached, will aim to build upon these promising results, establishing dosage efficacy and safety in
diverse settings and patient populations. These initiatives are integral for translating the promising
preclinical findings into practical medical therapies, albeit acknowledging the distinct biological
systems in human bodies compared to animal models. Overall, the body of research around (Tyr8)-Substance
P is expanding, generating optimism about its potential role in clinical practice within the coming
years. Collectively, these findings bolster the prospect of (Tyr8)-Substance P as a multifaceted
therapeutic tool, suitable for addressing a wide range of medical needs.
Are there any known side
effects or risks associated with (Tyr8)-Substance P?
As with any novel therapeutic agent,
understanding the side effects and risks associated with (Tyr8)-Substance P is critical for its safe
application in clinical settings. While detailed data on side effects must be thoroughly gathered
through ongoing and future clinical trials, preclinical studies provide some insights into its safety
profile. Generally, (Tyr8)-Substance P is considered to have a favorable safety profile compared to
traditional pain relief medications such as opioids and NSAIDs. By specifically targeting the NK1
receptor, it minimizes the broad systemic effects that more generalized pain medications can have,
potentially reducing the incidence of severe side effects.
However, the precise side effects can
vary depending on individual factors such as the dosage, method of administration, and patient health
conditions. Typical risks of using receptor antagonists are receptor desensitization or downregulation,
though these depend significantly on the receptor systems involved and the specific mechanism of the
antagonist. As (Tyr8)-Substance P specifically targets Substance P pathways, it carries a lower risk of
addiction or dependency, which is notable when compared to opioid-based therapies.
Nonetheless,
any pharmacological agent can cause individual adverse reactions, including allergic responses. These
reactions can range from mild skin irritation to more severe systemic reactions, though current studies
suggest that these outcomes are relatively rare with (Tyr8)-Substance P. Human trials are pivotal in
establishing the full side effect profile and understanding how often these occur in broader
populations.
Therefore, while (Tyr8)-Substance P shows promise in terms of a reduced risk
profile, healthcare professionals must observe a cautious approach as they consider it for comprehensive
treatment plans upon its clinical approval. Such caution ensures that it compliments existing safety
standards and effectively manages any unforeseen adverse reactions. As research expands, there will be a
clearer understanding of long-term risks and benefits, thereby helping to optimize dosing regimes and
further minimize risks associated with this promising treatment option.