Synonym |
(D-Arg2)-Kyotorphin |
Species |
Human |
Protein Accession |
P01581 |
Purity |
Greater than 98% as determined by HPLC and SDS-PAGE |
Endotoxin Level |
Less than 1 EU/µg |
Biological Activity |
Not determined |
Expression System |
E. coli |
Fusion Tag |
None |
Predicted Molecular Mass |
2576.9 Da |
Formulation |
Lyophilized from a 0.2 µm filtered solution of 20 mM HCl |
Reconstitution |
Centrifuge vial before opening. Add deionized water to a concentration of 0.1-1.0 mg/ml. Do not
vortex. Let the lyophilized pellet dissolve completely. |
Storage & Stability |
Store at -20°C. Store under desiccating conditions. |
FAQ
What is (D-Arg2)-Kyotorphin and how does it work?
(D-Arg2)-Kyotorphin is a synthetic analog of
kyotorphin, a neuropeptide first discovered in bovine brain tissue. Kyotorphin itself is a dipeptide
composed of tyrosine and arginine, known for its analgesic properties within the central nervous system.
(D-Arg2)-Kyotorphin is an enhanced version of this naturally occurring compound, optimized for increased
stability and efficacy. It functions primarily by modulating the body's pain perception pathways. The
mechanism involves the enhancement of endogenous opioid activity. Kyotorphin can activate met-enkephalin
release, a naturally occurring peptide with strong analgesic properties. Although kyotorphin does not
directly bind to opioid receptors, it stimulates the release of the endogenous opioids, thereby
producing analgesia indirectly. This makes it a unique compound in the sense that it bridges the gap
between traditional painkillers and non-opioid pain modulation. The (D-Arg2) modification confers
greater stability compared to the native version, as it increases the resistance to enzymatic
degradation within the body. This stability means higher bioavailability and longer duration of action.
While insights into exact pathways are ongoing, the compound stands out because it does not produce the
addictive properties associated with typical opioid therapies. Therefore, researchers are interested in
its potential application for chronic pain management without the side effects of traditional
opioids.
What are the potential benefits of using (D-Arg2)-Kyotorphin?
The potential
benefits of using (D-Arg2)-Kyotorphin primarily revolve around its pain management capabilities. Its
unique functionality sets it apart from traditional analgesics, offering a multifaceted approach to pain
relief. Unlike many pain relief methods that rely on direct opioid receptor activation, leading to
dependency and tolerance, (D-Arg2)-Kyotorphin works by promoting the release of naturally occurring
opioids like met-enkephalin. This mechanism minimizes the risk of addiction, making it a safer option
for long-term pain management when compared to conventional opioids. Additionally, the compound's
enhanced stability due to the D-Arg modification suggests it has a longer effective duration in the
human body, allowing for less frequent dosing and improved patient compliance. Patients who require
consistent pain management could potentially experience fewer side effects and a reduced burden of
managing their medication schedule. Furthermore, because of its indirect activation of opioid pathways,
(D-Arg2)-Kyotorphin has been shown in preliminary studies to cause fewer gastrointestinal side effects,
like constipation, which are commonly experienced with traditional opioids. This positions the compound
as a candidate for people who experience intolerable side effects from other pain management therapies.
It is also worth mentioning that the analgesic effect does not interfere significantly with cognitive or
motor functions, an important consideration for individuals who must maintain mental alertness. Thus,
its application becomes broad, potentially benefiting those with chronic pain conditions, postsurgical
pain, or neuropathic pain states, expanding the toolset clinicians have at their disposal for managing
pain.
How does (D-Arg2)-Kyotorphin compare to traditional painkillers?
When compared to
traditional painkillers, (D-Arg2)-Kyotorphin offers a unique alternative that targets pain through
different mechanisms. Traditonal painkillers often fall into categories such as NSAIDs, which reduce
inflammation, or opioids, which activate opioid receptors directly to produce analgesia. NSAIDs, while
effective for inflammatory pain, can cause gastrointestinal ulcers and cardiovascular complications with
prolonged use. Opioids, on the other hand, are associated with significant risks, including tolerance,
dependency, and addiction, largely due to their direct activation of opioid receptors in the brain.
(D-Arg2)-Kyotorphin, by contrast, operates by facilitating the release of the body's own opioid
peptides, like met-enkephalin, without directly binding to opioid receptors. This indirect method of
activating the body's pain-relief pathways means it does not carry the same risk of addiction or severe
side effects associated with opioids. As a result, it's an attractive option for long-term pain
management. It's important to recognize that while (D-Arg2)-Kyotorphin might not provide the immediate,
robust pain relief of a strong opioid, it supplements pain management regimens without significant risk
of dependency. Furthermore, early research indicates that because of its non-inflammatory pathway, it's
less likely to exacerbate gastrointestinal or cardiovascular issues, making it a versatile option for a
broader patient population. Understanding these differences is crucial for physicians considering
(D-Arg2)-Kyotorphin as part of a comprehensive pain management strategy, as it suggests a method that
maximizes safety and minimizes potential for abuse.
What are the known side effects of
(D-Arg2)-Kyotorphin?
As with any therapeutic compound, understanding the side effects of
(D-Arg2)-Kyotorphin is critical for assessing its suitability for patient care. Research into this
synthetic analog continues to grow to fully elucidate its safety profile. Presently, early studies are
promising and indicate that (D-Arg2)-Kyotorphin offers a more favorable side effect profile than many
traditional analgesics, particularly opioids. Given that (D-Arg2)-Kyotorphin does not bind directly to
opioid receptors, its side effects differ significantly from those typically associated with opioid
treatments. The indirect activation of the opioid pathway seems to result in less dependency and
tolerance compared to full opioid agonists. Furthermore, commonly observed side effects of opioids, such
as constipation, sedation, and nausea, appear to occur less frequently or with lower severity.
Additionally, because (D-Arg2)-Kyotorphin’s mechanism does not involve the cyclooxygenase pathways as
NSAIDs do, it is less likely to lead to issues like gastrointestinal distress or increased
cardiovascular risk, complications which are main concerns with prolonged NSAID use. However, as with
all therapeutic agents, individual responses can vary, and side effects may be experienced differently
throughout diverse patient populations. It's also crucial for clinicians and patients to report and
monitor any adverse effects to build a comprehensive safety profile as more people use the compound.
Although the current data suggests a promising profile, post-marketing surveillance and peer-reviewed
studies will further our understanding. This growing body of evidence will shape clinical practice and
maximize the therapeutic benefits while minimizing potential risks associated with (D-Arg2)-Kyotorphin.
Is (D-Arg2)-Kyotorphin suitable for all types of pain?
Understanding whether
(D-Arg2)-Kyotorphin is a suitable analgesic option hinges on identifying the specific type of pain it
may effectively address. Pain can be categorized into several types: acute, chronic, inflammatory,
neuropathic, and central pain, among others. Analyzing how (D-Arg2)-Kyotorphin interacts within these
categories is pivotal for deciding its application in treatment models. The analgesic properties of
(D-Arg2)-Kyotorphin are rooted in its ability to induce the release of met-enkephalin, thereby
influencing pain modulation in the central nervous system. Given this mechanism of action, it holds
particular promise for chronic pain management strategies that require prolonged alleviation without the
addiction risk of opioids. It may have particular benefits in cases where long-term treatment plans must
minimize the risk of side effects such as dependency or gastrointestinal distress. While its action
mechanism is distinctly beneficial, it's vital to acknowledge it may not be equally effective across all
pain types. For instance, while it shows potential in the treatment of neuropathic pain, due to its
central action, it might require adjunct therapies for inflammatory pain where local tissue damage and
inflammation are primary drivers. Additionally, due to its indirect mechanism, patients with acute
severe pain might require a compound offering immediate and robust relief, thus necessitating a
multifaceted pain management plan. Broadly, the suitability of (D-Arg2)-Kyotorphin will be determined by
ongoing research aimed at mapping its efficacy across different pain types and conditions, shaping
personalized analgesic strategies that fit individual patient profiles.