Synonym |
NTS |
Species |
Human |
Protein Accession |
P30990 |
Purity |
≥95% |
Endotoxin Level |
<1.0 EU per 1 μg of protein |
Biological Activity |
Fully biologically active when compared to standard. |
Expression System |
E. coli |
Fusion Tag |
None |
Predicted Molecular Mass |
Approximately 13.0 kDa |
Formulation |
Lyophilized from a 0.2 μm filtered solution of acetonitrile and TFA |
Reconstitution |
Centrifuge the tube briefly before opening. Reconstitute in water to a concentration of 0.1-1.0
mg/mL. Do not vortex. |
Storage & Stability |
Store at -20°C. Stable for 12 months from the date of receipt |
FAQ
What is Neurotensin and how does it work in the body?
Neurotensin is a 13-amino acid peptide
neurotransmitter found in the brain and gastrointestinal tract. It plays a vital role in modulating
several physiological processes, including hormone release, pain perception, and thermoregulation.
Discovered in the 1970s, Neurotensin has gained attention for its multifaceted roles in both the central
and peripheral nervous systems. In the brain, it functions as a neuromodulator and influences the
balance of neurotransmitters such as dopamine, serotonin, and norepinephrine, thus impacting mood and
emotional responses.
In the peripheral systems, Neurotensin contributes to gastrointestinal and
cardiovascular regulation. It is involved in processes such as gut motility, by stimulating or
inhibiting contractions of the intestinal muscles, and influences the secretion of digestive enzymes and
gastric acid. This peptide is also noted for its role in regulating blood pressure by modulating the
release and effects of other neurotransmitters and hormones within the cardiovascular system.
The
receptor system through which Neurotensin operates includes three main receptor subtypes - NTR1, NTR2,
and the low-affinity site, NTR3. The high-affinity binding of Neurotensin to NTR1 and NTR2 is primarily
responsible for its neuromodulatory effects, while NTR3 is involved in the intracellular signaling
pathways. Importantly, the neurotensinergic system's influence on dopamine has led to the exploration of
Neurotensin analogs and receptor modulators as potential therapies for schizophrenia and Parkinson’s
disease, as it can modulate dopamine signaling pathways profoundly.
Research into Neurotensin has
shown its promising role in protecting neural structures and preventing oxidative stress, which is
crucial in understanding degenerative diseases. Moreover, Neurotensin studies suggest potential
analgesic effects, as it modulates pain pathways centrally by influencing neurotransmitter release at
both spinal and supraspinal levels. This modulation can enhance or inhibit the transmission of pain
signals, offering an avenue for the development of new pain management therapies. However, despite its
therapeutic potential, a comprehensive understanding of its diverse biological functions and mechanisms
is essential to harness its full value safely and effectively.
How can Neurotensin be used in the
treatment of psychiatric disorders?
Neurotensin has been a focal point in psychiatric research
due to its profound effects on the dopaminergic system, which is critical in regulating mood and
emotion. A growing body of evidence suggests that Neurotensin and its receptor pathways could be
targeted for developing treatments for various psychiatric disorders, such as schizophrenia, anxiety,
and depression.
One of the most significant findings in psychiatric studies is the interaction of
Neurotensin with dopamine receptors. As an endogenous neuromodulator, Neurotensin can inhibit or excite
dopamine transmission, influencing symptoms associated with schizophrenia, such as hallucinations and
delusions. Neurotensin agonists and antagonists could potentially provide antipsychotic effects by
modulating these pathways. This offers a promising therapeutic strategy, especially for patients who are
resistant to traditional antipsychotic medications, which often target dopamine pathways but come with
severe side effects.
In cases of depression, Neurotensin could play a role in better
understanding and treating the disorder due to its interaction with serotonin, a neurotransmitter
intricately linked to mood regulation. Alterations in Neurotensin levels have been observed in
individuals suffering from depression, implying a potential pathway for therapeutic intervention. The
peptide's ability to upregulate serotonin might benefit those who do not respond adequately to selective
serotonin reuptake inhibitors (SSRIs), which are conventional antidepressants.
Anxiety disorders
may also be addressed through Neurotensin-based treatment strategies. The peptide's dual role in the
central nervous system impacts neural circuits related to fear and anxiety. Research indicates that
neurotensinergic signals can influence the amygdala, a brain region critically involved in anxiety
regulation. Thus, neurotensin analogs might serve as anxiolytics, offering relief by modulating these
pathways.
It's important to consider that while these therapeutic prospects highlight
Neurotensin's significant potential in treating psychiatric disorders, the path from discovery to
application is complex and requires extensive clinical research and trials. The intricate nature of
psychiatric disorders, along with the variability in Neurotensin receptor expression in individuals,
poses challenges. Personalized medicine approaches, focusing on genetic and phenotypic predispositions,
alongside Neurotensin pathways, might offer a more effective and tailored method for psychiatric
treatment in the future.
What are the potential therapeutic applications of Neurotensin in pain
management?
Neurotensin holds significant promise in the landscape of pain management due to its
diverse and complex interaction with pain modulation pathways within the central nervous system. Pain
management, a crucial aspect of medical care, often relies on medications that can have significant side
effects or limited efficacy. Thus, the exploration of new pathways and molecules like Neurotensin is
invaluable in developing innovative pain relief strategies.
The ability of Neurotensin to
influence both spinal and supraspinal mechanisms of pain control points to its potential as a novel
analgesic. Pain is typically transmitted from peripheral nerves to the central nervous system through
several pathways. In this complex process, Neurotensin can exert modulatory effects by its action on
neurotransmitter release, such as serotonin and nitric oxide, which play essential roles in transmitting
pain signals.
Research suggests that when Neurotensin is administered centrally, it has an
inhibitory action on acute pain by diminishing the excitability of nociceptive pathways, which are the
nerve pathways that transmit pain. Moreover, Neurotensin can interact with opioid receptors, suggesting
that it could enhance the effects of opioids, commonly used pain relief agents, thereby allowing for
lower doses and reducing the risk of addiction and other opioid-associated side effects.
In
chronic pain management, such as in neuropathic pain conditions, Neurotensin's role can be particularly
beneficial. Neuropathic pain, which results from nervous system dysfunction, often presents challenges
in treatment and is resistant to traditional analgesics. Neurotensin’s neuromodulatory effects on
calcium channels and various neurotransmitter systems could potentially alleviate chronic pain by
modulating the neural plasticity associated with prolonged pain states.
Additionally, the use of
Neurotensin analogs in research indicates promising outcomes in both pain reduction and protective nerve
health. These analogs may offer enhanced stability and bioavailability over the natural peptide, making
them more effective for clinical use. However, transitioning these findings into clinical practice
requires rigorous trials to ensure their safety and efficacy.
Incorporating Neurotensin-based
treatments into pain management protocols could revolutionize how clinicians address pain, offering
patients more options for relief. However, more studies are needed to fully unravel Neurotensin's
mechanisms in pain modulation. The aim is to bridge laboratory findings with patient care, ensuring that
such advances in pain management are clinically viable and accessible to the broader patient
population.
How does Neurotensin affect the gastrointestinal system?
Neurotensin plays a
multifaceted role within the gastrointestinal (GI) system, impacting various processes from motility to
hormone secretion, thus maintaining digestive health. Its presence in the GI tract positions it
strategically to influence numerous physiologic pathways critical for digestion and nutrient absorption.
One of the primary actions of Neurotensin in the digestive system is its impact on intestinal motility.
It exert both excitatory and inhibitory effects on GI smooth muscle activity, depending upon the
specific type of intestinal muscle and receptor involved. This balance is crucial for maintaining proper
peristalsis, the involuntary contractions that move food through the digestive tract.
Research
indicates Neurotensin's critical involvement in modulating gastric acid and enzyme secretion. When
triggered, Neurotensin can prompt the secretion of these digestive components, thereby aiding in the
breakdown of food into absorbable nutrients. This action complements its activity within the
enteroendocrine system, where it interacts with other hormones like cholecystokinin and gastrin, which
are involved in digestion and satiety signaling.
Additionally, Neurotensin impacts gut
inflammation and repair mechanisms. Studies demonstrate that Neurotensin can exert anti-inflammatory
effects within the gut, potentially making it significant for conditions like inflammatory bowel disease
(IBD) and irritable bowel syndrome (IBS). This anti-inflammatory role is potentially mediated through
modulation of cytokine profiles and immune cell activity within the gut mucosa, seeking to balance local
inflammatory responses and gastrointestinal health.
The neurotrophic effects of Neurotensin in
the GI tract imply that it may aid in tissue repair processes following injury or inflammation by
promoting cell proliferation and migration. This suggests a protective role for Neurotensin against
intestinal damage, which could be instrumental in recovery from gut injuries or surgical
procedures.
Furthermore, Neurotensin levels have been found to be altered in various
gastrointestinal disorders, signaling its integral role and potential as a therapeutic marker or target.
However, while the broad scope of Neurotensin's influence on the GI system highlights its therapeutic
potential, translating these functions into treatments requires robust clinical research to optimize
dosing, delivery methods, and identify any long-term effects of modulating Neurotensin
pathways.
Are there any safety concerns associated with Neurotensin-based
therapies?
Despite the promising applications of Neurotensin-based therapies, addressing
potential safety concerns is paramount for developing effective and secure treatment protocols. As with
any therapeutic agent targeting neurotransmitter systems, understanding the multifaceted interactions
and systemic implications of Neurotensin is vital to avoiding adverse effects and ensuring patient
safety.
A significant concern in Neurotensin-based therapies is receptor specificity. Neurotensin
operates through multiple receptors, each implicated in different physiological pathways across the
central and peripheral systems. Nontarget effects can arise from the broad distribution and diversity of
these receptor subtypes. Hence, ensuring that therapies selectively target specific pathways without
unintended activation of others is crucial in minimizing side effects. Receptor cross-activity could
potentially result in unwanted alterations in neurotransmitter balance, affecting mood, cognition, or
other physiological processes.
Another safety consideration is the potential for neurological and
psychological side effects. Since Neurotensin extensively interacts with dopamine pathways, therapies
could inadvertently mimic or interfere with dopaminergic drugs, affecting conditions like schizophrenia
or Parkinson's disease. Unbalanced activity could exacerbate psychiatric symptoms or result in new
neuromodulation-driven effects, such as mood swings or altered stress responses.
Furthermore,
systemic delivery of Neurotensin or its analogs might pose issues like peptide degradation or immune
responses. Peptides administered exogenously face rapid breakdown by enzymes and potential antigenicity,
where the immune system might recognize them as foreign, leading to adverse immune reactions. Therefore,
delivery methods require optimization for stability and bioavailability while ensuring minimal
immunogenicity.
Understanding the role of Neurotensin in cardiovascular regulation raises
concerns related to blood pressure modulation. The influence of Neurotensin on vasodilation suggests
that improper dosing or unexpected systemic effects could lead to hypotensive episodes, especially in
susceptible individuals or those with pre-existing cardiovascular conditions.
Long-term usage
implications are another aspect requiring attention. Chronic modulation of neurotransmitter and receptor
systems holds the potential for developing tolerance, desensitization, or compensatory adaptations,
where the body adjusts to the presence of the drug, potentially diminishing its efficacy or
necessitating dose increases.
Consequently, the development of Neurotensin-based therapies
mandates rigorous preclinical and clinical evaluation, with comprehensive monitoring for any adverse
effects, pharmacokinetic profiling, and specific targeting mechanisms. Through meticulous research and
careful design, these therapies could safely capitalize on Neurotensin’s multifaceted physiological
interactions for clinical benefit, offering novel treatments with reduced risks compared to existing
options.