Synonym |
Dab9-NT(8-13) |
Species |
Human |
Protein Accession |
P30990 |
Purity |
Greater than 95% as determined by HPLC |
Endotoxin Level |
Less than 1 EU/ug |
Biological Activity |
The ED50 as determined by its ability to inhibit cAMP production by CHO cells expressing
rat/human Neurotensin R1 is less than 1.0 ug/ml |
Expression System |
E. coli |
Fusion Tag |
GST-His |
Predicted Molecular Mass |
7810 Da |
Formulation |
Lyophilized from a 0.2 um filtered solution in Acetonitrile and TFA |
Reconstitution |
It is recommended to reconstitute the lyophilized Dab9-Neurotensin(8-13) in sterile 18MΩ-cm H2O
not less than 100 ug/ml, which can then be further diluted to other aqueous solutions. |
Storage & Stability |
Lyophilized Dab9-Neurotensin(8-13) although stable at room temperature for 3 weeks, should be
stored desiccated below -18°C. Upon reconstitution Dab9-Neurotensin(8-13) should be stored at
4°C between 2-7 days and for future use below -18°C. |
FAQ
What is (Dab9)-Neurotensin (8-13) and what makes it unique compared to other neuropeptides?
(Dab9)-Neurotensin (8-13) is a synthetic peptide derivative of the naturally occurring neuropeptide
neurotensin. Neurotensin, a tridecapeptide found in the central nervous system and gastrointestinal
tract, plays a critical role in affecting dopamine signaling, pain regulation, and body temperature
control, among other processes. The modification at the ninth position with a D-aminobutyrate (Dab)
residue enhances the peptide's resistance to enzymatic degradation, making it more stable and
longer-lasting in biological systems. This particular stability is significant because it allows
(Dab9)-Neurotensin (8-13) to be studied in various experimental settings with reduced risk of rapid
breakdown, which is common in other peptide formulations. Additionally, the unique structure of
(Dab9)-Neurotensin (8-13) increases its selectivity and affinity towards neurotensin receptors, making
it a more reliable candidate for neurological studies and offering promising therapeutic
potentials.
What are the potential therapeutic applications of (Dab9)-Neurotensin (8-13)?
(Dab9)-Neurotensin (8-13) holds considerable promise in several therapeutic areas due to its
interaction with the nervous system and associated physiological effects. The peptide's interaction with
neurotensin receptors gives it significant potential in managing pain, particularly neuropathic and
inflammatory pain. Its mechanism of action involves natural pathways that are believed to modulate
ascending pain signals in the central nervous system, potentially reducing the need for opioids, which
come with addiction and tolerance issues. Furthermore, its effects on dopamine pathways suggest possible
applications in treating psychiatric and neurological disorders, including schizophrenia and Parkinson’s
disease. For schizophrenia, it offers potential as an adjunct treatment by possibly improving symptoms
without the extensive side effects associated with current antipsychotics. Additionally, by influencing
dopamine transmission, (Dab9)-Neurotensin (8-13) might also be explored in addressing drug addiction and
withdrawal symptoms, offering a new avenue in addiction therapy. Emerging research has also hinted at
the peptide’s role in thermoregulation and metabolism, proposing it as a candidate for combating obesity
and related metabolic disorders. With its longer-lasting action and specificity, (Dab9)-Neurotensin
(8-13) may become a cornerstone in developing novel therapeutic strategies across these varied
fields.
What are the mechanisms of action for (Dab9)-Neurotensin (8-13) in the body?
The
intricate mechanisms of action for (Dab9)-Neurotensin (8-13) lie in its interaction with three primary
neurotensin receptors, namely NTS1, NTS2, and NTS3. The binding of (Dab9)-Neurotensin (8-13) to these
receptors initiates a cascade of intracellular responses pivotal in various physiological processes. The
NTS1 receptor, a G-protein coupled receptor, is primarily involved in the modulation of neurotransmitter
pathways, including dopamine, which is crucial for its potential use in treating diseases characterized
by dopamine dysregulation, such as schizophrenia and Parkinson’s disease. Additionally, NTS1 engagement
triggers pathways that can result in analgesic effects, presenting a non-opioid avenue for managing
pain. Meanwhile, activation of the NTS2 receptor further contributes to pain modulation, enhancing the
peptide's analgesic profile. It’s particularly noted for its role in anti-nociceptive effects, which are
beneficial in conditions like chronic pain. The receptor NTS3, though less understood, is implicated in
processes such as cell growth and survival, suggesting it may play a role in neuroprotection and
possibly cancer biology. Beyond receptor-mediated actions, (Dab9)-Neurotensin (8-13) also interacts with
other signaling molecules and pathways, modulating inflammatory responses and other neural functions.
Through these diverse interactions, (Dab9)-Neurotensin (8-13) demonstrates the multifaceted influences
essential for its therapeutic potential in neurological and psychiatric disorders, pain management, and
perhaps even in metabolic conditions.
How does (Dab9)-Neurotensin (8-13) compare with traditional
pain management treatments?
(Dab9)-Neurotensin (8-13) presents a promising alternative to
traditional pain management strategies, primarily due to its unique mechanism of action and reduced risk
of side effects. Traditional pain management often relies on nonsteroidal anti-inflammatory drugs
(NSAIDs), opioids, and acetaminophen. While effective, each of these treatments comes with significant
limitations. NSAIDs, for instance, are associated with gastrointestinal disturbances and increased
cardiovascular risk with long-term use. Opioids, which are highly effective for acute pain, pose
significant risks related to addiction, tolerance, and respiratory depression. Acetaminophen, though
generally safer, carries the risk of liver toxicity, especially when used in higher doses. In contrast,
(Dab9)-Neurotensin (8-13) exerts its analgesic effects primarily through modulation of central nervous
system pathways that inhibit pain signal transmission. This central modulation occurs with a lower risk
of addiction since it does not engage opioid receptors. Furthermore, the target-specific action of
(Dab9)-Neurotensin (8-13) offers pain relief similar to that of opioids, but without the associated
adverse effects like euphoria-induced dependency. Additionally, its enhanced stability and resistance to
degradation afford a potentially longer duration of action, which could allow for less frequent dosing
compared to traditional treatments. This profile positions (Dab9)-Neurotensin (8-13) not just as a
powerful analgesic, but also as a safer long-term alternative for chronic pain patients, an area where
traditional pain medications often fall short.
Can (Dab9)-Neurotensin (8-13) have any adverse
effects with long-term administration?
While (Dab9)-Neurotensin (8-13) provides many promising
therapeutic benefits, it is essential to consider potential adverse effects that may arise from
long-term administration. Current understanding suggests that, compared to traditional medications,
(Dab9)-Neurotensin (8-13) may have a favorable safety profile due to its specific mechanism of action
and reduced interaction with non-target receptors. However, as with any therapeutic peptide or compound,
unforeseen risks could emerge as more extensive clinical trials are conducted. Potential adverse effects
may include issues related to neurotensin receptor desensitization or down-regulation with prolonged
use, which could potentially reduce efficacy over time or require adjustments in dosing. Furthermore,
since neurotensin and its analogs are involved in a broad range of physiological processes, there is
always the potential for off-target effects that may impact gastrointestinal function or
thermoregulation. Researchers must thoroughly explore the peptide's impact across various biological
systems to ensure comprehensive safety evaluations. Additionally, although (Dab9)-Neurotensin (8-13) is
designed to resist rapid degradation, its stability may also contribute to an extended duration in the
body, which could lead to cumulative effects or interactions with other treatments. Continuous
monitoring and detailed studies will be critical to uncover any long-term consequences of using
(Dab9)-Neurotensin (8-13), ensuring that the benefits experienced by patients are maximized while
minimizing potential risks.
How does (Dab9)-Neurotensin (8-13) affect neural pathways associated
with psychiatric disorders?
(Dab9)-Neurotensin (8-13) has piqued the interest of researchers in its
potential application for psychiatric disorders due to its interaction with neural pathways often
implicated in these conditions. Many psychiatric disorders, including schizophrenia, bipolar disorder,
and depression, involve the dysregulation of neurotransmitter systems like dopamine, serotonin, and
glutamate. Neurotensin, and by extension its analogs such as (Dab9)-Neurotensin (8-13), modulate these
pathways by acting primarily on neurotensin receptors, which have a direct and indirect influence on
dopaminergic systems. In schizophrenia, characterized by an imbalance between dopamine pathways,
(Dab9)-Neurotensin (8-13) may help to modulate dopamine signaling, potentially reducing symptoms like
hallucinations and delusions without resorting to typical antipsychotics, which can have significant
side effects. Additionally, its mood-regulating effects could potentially impact serotonin pathways,
offering benefits in treating depressive symptoms and mood stabilization. Moreover, its neuroprotective
properties, as evidenced through NTS3 interactions, suggest potential benefits in preventing or reducing
neural damage associated with psychiatric conditions. Through these multifaceted effects,
(Dab9)-Neurotensin (8-13) may offer a novel mechanism of therapeutic action for psychiatric disorders,
augmenting or providing alternatives to existing treatments.
What research is currently being
conducted on (Dab9)-Neurotensin (8-13)?
Currently, research on (Dab9)-Neurotensin (8-13) is quite
active, with various studies aiming to explore its broad therapeutic potential and underlying mechanisms
in detail. Much of the research is focused on its analgesic properties, given the growing need for new
pain management solutions that do not involve opioids. These studies are looking at both its efficacy in
reducing pain and its safety profile, particularly in chronic pain conditions that require long-term
treatment. In addition to pain management, there is considerable interest in the peptide’s potential
applications in neurodegenerative diseases and psychiatric disorders, due to its modulatory effects on
neurotransmission and receptor activity. Research is delving into the peptide's neuroprotective
capabilities, exploring how it might be able to mitigate neural damage or dysfunction characteristic of
diseases like Alzheimer’s or Parkinson’s. Additionally, its potential for modifying dopaminergic and
serotonergic pathways is being scrutinized in the context of psychiatric disorders like schizophrenia
and depression. Beyond this, animal model studies are progressing to determine its effects on metabolic
processes and thermoregulation, adding the prospect of treating obesity or metabolic syndrome to its
portfolio. Overall, these efforts are paving the way for establishing (Dab9)-Neurotensin (8-13) as a key
player in future medicinal therapies.