Synonym |
Dyn A (1-10) amide |
Species |
Human |
Protein Accession |
P01261 |
Purity |
Greater than 95% |
Endotoxin Level |
Less than 1 EU/μg |
Biological Activity |
Not available |
Expression System |
Chemical Synthesis |
Fusion Tag |
None |
Predicted Molecular Mass |
1241.4 Da |
Formulation |
Supplied as a lyophilized powder |
Reconstitution |
Reconstitute in water to a concentration of 0.1-1.0 mg/ml |
Storage & Stability |
Store at -20°C. For long term storage, store at -80°C. Stable for up to 3 months when stored at
-20°C. |
FAQ
What is Dynorphin A (1-10) amide, and how does it function in the body?
Dynorphin A (1-10) amide
is a naturally occurring peptide fragment of the endogenous opioid peptide, dynorphin, derived from the
precursor protein prodynorphin. The sequence of this peptide consists of the first ten amino acids of
dynorphin A, with an additional modification at the C-terminal end known as amidation. This modification
increases the peptide's stability and affinity for opioid receptors, enhancing its physiological
effects. Dynorphin A (1-10) amide primarily interacts with the kappa-opioid receptor (KOR) but can also
have varying degrees of affinity towards delta and mu-opioid receptors, though these interactions are
typically weaker.
Dynorphins are vital in regulating numerous physiological processes, most
notably those associated with pain perception, stress response, mood regulation, and addiction. Upon
binding to the kappa-opioid receptors located in the central and peripheral nervous systems, dynorphin A
(1-10) amide can modulate neurotransmitter release, thereby influencing signal transmission in neuronal
pathways responsible for pain and reward. This modulation can result in analgesic effects, making it a
target for therapeutic applications aimed at treating different types of pain, particularly neuropathic
pain which is usually resistant to traditional analgesics.
Moreover, the activity of dynorphin A
(1-10) amide at kappa-opioid receptors is linked with stress-related behavioral responses. Activation of
these receptors has been associated with inducing dysphoric states, which contrasts with the often
euphoric effects exerted by mu-opioid receptor agonists. This property might be leveraged
therapeutically to help manage addiction. By mitigating the rewarding effects of addictive substances,
dynorphin A (1-10) amide potentially could be developed as part of treatment strategies aimed at
preventing relapse in individuals recovering from substance abuse disorders. Additionally, the peptide
also influences various neuroendocrine functions, contributing to its complex role in the body.
In summary, dynorphin A (1-10) amide, through its interaction with kappa-opioid receptors,
exerts significant effects on pain modulation, stress responses, mood, and addiction, highlighting its
potential in therapeutic applications such as analgesia and addiction management. Understanding its
mechanism and effects in more detail offers pathways to novel treatment modalities leveraging this
powerful peptide.
What are the potential therapeutic applications of Dynorphin A (1-10)
amide?
Dynorphin A (1-10) amide holds promising potential for numerous therapeutic applications,
particularly in managing pain, treating mood disorders, and addressing substance abuse. Its primary
function as a modulator of the kappa-opioid receptor (KOR) implies a range of physiological impacts
relevant to these medical areas. Indeed, one of the most studied aspects of dynorphins, underscored by
this amide fragment, is their analgesic properties making it a candidate for pain management, especially
neuropathic and chronic pain forms resistant to typical opioid treatments. Through the activation of
KORs, Dynorphin A (1-10) amide can reduce the perception of pain by influencing neuronal pathways
without the risk of addiction associated with mu-opioid receptor agonists.
Mood disorders such as
depression and anxiety may also benefit from interventions involving Dynorphin A (1-10) amide. The
peptide's ability to influence neurotransmitter release, particularly involving dopamine systems, means
it could modulate mood and anxiety levels. Research suggests that kappa-opioid receptor agonists, like
dynorphin, induce dysphoria and stress, with chronic exposure potentially triggering depressive states.
Counterbalancing this, however, understanding and modulating this response could provide a framework for
developing treatments aimed at mood regulation—essentially using the dynorphin pathway to recalibrate
neurochemical imbalances in affected individuals, though this requires substantial further research to
ensure therapeutic efficacy and safety.
In the realm of addiction, Dynorphin A (1-10) amide’s
modulatory effect on reward pathways positions it as a candidate for disrupting addictive behavior
pathways. By affecting the release of dopamine in key brain areas associated with reward and pleasure,
it can diminish the rewarding effects of addictive substances such as opioids, alcohol, and
psychostimulants. This diminished effect could reduce craving and relapse incidence in individuals
undergoing recovery from substance abuse, making it a tool worth investigating within addiction
treatment frameworks.
Furthermore, research is expanding into other areas such as epilepsy,
Parkinson’s disease, and cognitive function where Dynorphin A (1-10) amide might offer benefits through
its broad-spectrum receptor interactions and regulatory roles. While significant efforts in basic and
clinical research are necessary to translate these potential applications into validated therapies, the
existing data underscores the promise held by this peptide. With ongoing advancements in peptide drug
design, stability, and delivery mechanisms, Dynorphin A (1-10) amide could emerge as a formidable
component in the new wave of therapeutics targeting complex neurological disorders and managing
intricate biopsychological processes.
How does Dynorphin A (1-10) amide differ from other opioid
receptor modulators?
Dynorphin A (1-10) amide, as a fragment of the larger dynorphin peptide, is
primarily distinguished from other opioid receptor modulators by its specific affinity and activity at
the kappa-opioid receptor (KOR), marking it as predominantly a kappa-selective agonist. In contrast,
many traditional opioids, such as morphine and codeine, are mu-opioid receptor (MOR) agonists, making
their interaction with opioid receptors markedly different from that of dynorphin derivatives. This
fundamental difference in receptor activity leads to varied physiological and pharmacological outcomes,
which further delineate their distinct therapeutic profiles and potential side effects.
The
emphasis on kappa-opioid receptor affinity results in dynorphin A (1-10) amide inducing physiological
effects that diverge from those typically associated with mu-opioid activation. While mu-opioid receptor
agonists generally produce analgesia accompanied by euphoric sensations—factors contributing to their
high abuse potential—dynorphin A (1-10) amide’s activation of KOR often leads to anti-reward effects,
such as dysphoria and anhedonia. This difference is pivotal in considering the role of such peptides in
addiction and managing pain without the pronounced risk of dependency and overdose inherent in many
mu-opioid receptor modulators. Consequently, these kappa-selective properties might be leveraged to
develop non-addictive analgesics or therapeutic agents aimed at treating addictive disorders by
mitigating the rewarding effects of drugs of abuse.
Moreover, Dynorphin A (1-10) amide can
modulate numerous other physiological processes that differentiate it from typical opioid analgesics.
Its involvement in stress response and modulation of hormonal release further demonstrates its broad
scope of influence. These distinct activities are underscored by the peptide's ability to induce complex
changes in neuronal circuitry beyond those observed with standard opioids, offering a nuanced approach
to disorders involving stress dysregulation, mood disorders, and neurodegenerative diseases.
In
addition, dynorphins exhibit a variation in their effects on neurotransmitter systems compared to
classic opioid therapies. While both types of compounds can influence the dopaminergic pathways within
the central nervous system, the outcomes diverge due to the opposing actions mediated by KOR and MOR
systems, providing nuanced opportunities for therapeutic manipulation. Considering their unique receptor
interactions and physiological impact, Dynorphin A (1-10) amide represents a distinct class of opioid
receptor modulators with potential advantages over traditional opioids, particularly in developing
non-addictive analgesics and complex neurological disorder therapeutics.
Are there any side
effects or risks associated with Dynorphin A (1-10) amide?
As with any bioactive peptide,
understanding the potential side effects and risks associated with Dynorphin A (1-10) amide is crucial,
particularly in light of its interactions with the kappa-opioid receptor (KOR) and the varied
physiological systems it influences. KOR agonists like Dynorphin A (1-10) amide are generally associated
with less risk of addiction compared to mu-opioid receptor agonists; however, they do present a unique
side effect profile that must be considered critically, especially in terms of mood and cognitive
effects.
One of the primary concerns with Dynorphin A (1-10) amide use is its propensity to
induce pronounced dysphoric and aversive effects. Unlike the euphoric states often associated with
mu-opioid receptor activation, kappa-opioid receptor engagement can result in feelings of dysphoria,
which, although contributing to its potential role in reducing addictive behaviors in substance abuse
treatment, might limit patient compliance and acceptance in broader therapeutic applications. These
dysphoric effects stem from the interaction of Dynorphin A (1-10) amide with central nervous system
pathways involved in mood regulation, highlighting a need for careful management and, possibly,
co-administration with mood-stabilizing agents to mitigate such adverse outcomes.
Additionally,
kappa-opioid receptor activation can influence cognition and perception, sometimes manifesting as
impaired cognitive and motor abilities. While these effects vary depending on dosage and administration
routes, they necessitate vigilance when considering this peptide for therapeutic purposes, particularly
in populations where cognitive function is already compromised, or in concurrent usage with other
central nervous system modulating therapies.
Moreover, physical side effects like sedation and
nausea can accompany kappa-opioid receptor engagement. While generally of lesser concern than
complications arising from mu-opioid receptor agonist use, these issues still represent practical
considerations in therapeutic contexts, requiring tailored dosage strategies and potentially
necessitating supportive treatment to enhance tolerability and maintain patient
adherence.
Importantly, like with any pharmacological agents, individual variability in response
to Dynorphin A (1-10) amide should be anticipated. Genetic, environmental, and existing health status
factors can significantly influence both the efficacy and the side effect profile, emphasizing the
importance of personalized medical approaches and robust clinical trials to delineate these variables
more precisely. Ultimately, while Dynorphin A (1-10) amide holds enticing therapeutic promise across
several challenging medical domains, careful consideration of its side effects and patient-specific
factors remains imperative to harness its full potential safely and effectively.
What are the
research advancements concerning Dynorphin A (1-10) amide?
Research on Dynorphin A (1-10) amide
continues to advance, opening new windows into its potential therapeutic capabilities and physiological
roles. Recent studies have delved deeply into its molecular interactions, neuronal pathway impacts, and
potential clinical applications, with ongoing interest in leveraging its kappa-opioid receptor activity
to address pain, addiction, and mood disorders.
Significant strides have been made in
understanding the complex mechanisms underpinning Dynorphin A (1-10) amide’s action at the kappa-opioid
receptor level and beyond. Scientists utilize advanced molecular biology and neuroimaging techniques to
map the precise effects of its receptor engagement across various neuronal circuits. This growing
understanding has illuminated its nuanced role in modulating neurotransmitter systems, particularly
concerning dopamine pathways related to reward, reinforcement, and pain. These insights are critical as
they help clarify how Dynorphin A (1-10) amide potentially modulates addictive behaviors and equips
researchers with valuable knowledge to develop addiction therapeutics focused on mitigating cravings and
relapse.
In the realm of pain management, researchers are increasingly interested in Dynorphin A
(1-10) amide’s analgesic capabilities, especially for neuropathic and chronic pain forms that resist
traditional opioid therapy. Innovative studies employ animal models and advanced imaging to ascertain
effective, safe dosing parameters and better understand its long-term impacts compared to existing
opioid options. This research direction presents the prospect of novel therapeutics providing effective
pain relief without the addictive potential associated with current treatments, addressing a severe
healthcare challenge amid ongoing opioid crises.
Further noteworthy advancements include
examining Dynorphin A (1-10) amide’s potential for addressing mood disorders such as depression and
anxiety. By exploring its complex modulation of emotional pathways and its kappa-induced dysphoric
effects, scientists aim to develop complementary treatments that balance these aspects to offer
therapeutic relief for individuals with mood dysregulation. Such exploration is imperative as mood
disorders remain a critical unmet need globally, necessitating the pursuit of innovative pharmacological
strategies.
Research continues to progress into optimizing Dynorphin A (1-10) amide’s molecular
stability and bioavailability, vital steps for transitioning from lab-based findings to viable clinical
applications. Bioengineering and medicinal chemistry advancements are pivotal, with fresh approaches to
peptide modification enhancing its therapeutic profile by improving receptor selectivity, minimizing
side effects, and achieving targeted delivery in the body.
In conclusion, research advancements
concerning Dynorphin A (1-10) amide illustrate the robust potential of this peptide to offer innovative
solutions across pain management, addiction treatment, and mood disorder interventions. Combining
cutting-edge scientific techniques and interdisciplinary collaboration, researchers move closer to
translating laboratory discoveries into tangible medical advancements, highlighting a promising future
for Dynorphin A (1-10) amide in clinical practice.