Synonym |
Neurotensin (1-11) |
Species |
Human |
Protein Accession |
P30990 |
Purity |
≥ 95% |
Endotoxin Level |
< 1.0 EU per µg |
Biological Activity |
N/A |
Expression System |
E. coli |
Fusion Tag |
None |
Predicted Molecular Mass |
1293 Da |
Formulation |
Lyophilized from a 0.2 μm filtered solution in Acetonitrile and TFA |
Reconstitution |
Reconstitute at 100 μg/mL in sterile 4 mM HCl containing at least 0.1% human or bovine serum
albumin. |
Storage & Stability |
Store at -20°C upon receipt, stable for up to 6 months at -20°C. |
FAQ
What is Neurotensin (1-11) and what are its primary functions in the body?
Neurotensin (1-11) is
a peptide fragment derived from the naturally occurring neuropeptide neurotensin. This peptide is known
for its wide range of biological activities and plays a crucial role in the central nervous system and
the peripheral organs. Neurotensin itself was first discovered in the 1970s. It consists of 13 amino
acids, and the 1-11 fragment represents the truncated form of this peptide, excluding the last two amino
acids. Despite being a fragment, Neurotensin (1-11) retains significant biological activity. The primary
functions of neurotensin in the body include modulating dopamine neurotransmission, influencing the
digestive system, and regulating the release of certain hormones. It interacts with specific receptors,
mainly the neurotensin receptors NTS1, NTS2, and NTS3, which are distributed widely throughout the brain
and in certain peripheral tissues.
In the central nervous system, Neurotensin (1-11) plays a
crucial role in modulating the release of dopamine, which is a vital neurotransmitter involved in
regulating mood, motivation, and reward pathways. This ability to influence dopamine release indicates
potential implications for neurotensin in managing psychiatric disorders such as schizophrenia, where
dopamine regulation is often disrupted. Additionally, neurotensin has been studied for its potential
effects on pain perception, as it is thought to be involved in descending pain inhibitory pathways,
which help modulate the body’s response to pain. In the peripheral system, neurotensin influences
intestinal motility and gastric secretions, making it relevant in digestion. It is secreted by the
N-cells in the intestine in response to the intake of fats, illustrating its role in digestive
processes.
Beyond its role in neurotransmission and digestion, neurotensin also influences
cardiovascular function, temperature regulation, and potentially has neuroprotective properties, making
it a peptide of interest in various areas of research. However, it should be noted that while the
effects of neurotensin are broad, Neurotensin (1-11) may exhibit slightly distinct pharmacological
profiles due to its truncated structure. Research into how this specific fragment interacts with
neurotensin receptors and exerts its effects is ongoing, as it provides a more selective approach to
studying the peptide’s role without engaging all the pathways activated by the full-length neurotensin
sequence. Scientists continue to explore the diverse functionalities offered by Neurotensin (1-11) to
provide insights into therapeutic applications that might suit the specific dynamics of this peptide
fragment.
How does Neurotensin (1-11) interact with its receptors, and why is this
significant?
The interaction of Neurotensin (1-11) with its receptors is a significant aspect of
its biological functionality, influencing multiple physiological processes. Neurotensin's primary
receptors are classified under the neurotensin receptor family, notably including NTS1, NTS2, and NTS3,
which are distinct in terms of their structure, distribution, and subsequent functionality. Neurotensin
(1-11) functions primarily through interacting with these G-protein coupled receptors (GPCRs), which are
known for their ability to translate extracellular signals into a range of intracellular effects, hence
influencing cellular responses across various types.
NTS1 and NTS2, the two major GPCRs in the
neurotensin receptor group specifically bind to bioactive neuropeptide fragments such as Neurotensin
(1-11). NTS1 is predominantly involved in the modulation of neurotransmitter systems in the central
nervous system, especially concerning dopamine pathways. Upon binding to NTS1, Neurotensin (1-11)
influences the activation of downstream effectors and second messenger systems, leading to changes in
neurotransmitter release, which can alter mood, cognition, and response to stress or pain. Meanwhile,
interaction with NTS2 is often associated with modulation resulting in analgesic effects, as this
receptor subtype is tied to antinociceptive pathways which counteract pain signaling in the central
nervous system. This makes neurotensin fragments especially interesting as potential therapeutic agents
for both neuropsychiatric and pain-related disorders.
The significance of Neurotensin (1-11)
receptor interaction extends to the peripheral functions. Both NTS1 and NTS2 have shown some degree of
distribution in peripheral tissues, where they affect gastrointestinal and endocrine systems. By binding
to these receptors in the peripheral areas, Neurotensin (1-11) can influence processes like intestinal
motility and gastric secretion. Additionally, NTS3, or the sortilin receptor, although not a GPCR, plays
a role in neurotensin's biological effects due to its involvement in sorting and trafficking cellular
proteins, thereby influencing the overall response induced by neurotensin peptides.
Such
receptor-mediated functions of Neurotensin (1-11) have marked implications for pharmacology and clinical
research, particularly in the design of drugs targeting these specific receptors to harness therapeutic
potentials. The specificity of Neurotensin (1-11) binding to these receptors can enable targeted
modulation of pathways, suggesting applications in disorders characterized by neurotransmitter
dysregulation such as schizophrenia, or where modulation of pain perception is beneficial. Thus, ongoing
research in understanding receptor interactions with Neurotensin (1-11) is crucial for realizing its
full pharmacological potential and for the development of clinical interventions leveraging its
interactions.
What research has been conducted on the effects of Neurotensin (1-11) on
psychiatric or neurological conditions?
Research into the effects of Neurotensin (1-11) on
psychiatric and neurological conditions has been fueled by its significant role in modulating
neurotransmitter systems, particularly dopamine. Schizophrenia and other psychotic disorders have been
at the forefront because dopamine dysregulation is a core feature of these conditions. Studies have
demonstrated that neurotensin may have antipsychotic properties due to its interaction with dopamine
pathways. While full-length neurotensin is a well-established modulator of dopaminergic activity, its
truncated fragment, Neurotensin (1-11), shows promise in offering similar benefits with a potentially
refined pharmacological profile.
Research indicates that Neurotensin (1-11), by binding to NTS1,
influences dopamine receptor modulation and neurotransmitter release in regions of the brain associated
with schizophrenia, such as the striatum and prefrontal cortex. These effects could mitigate
hyperdopaminergia typically observed in acute psychotic episodes. Furthermore, some studies suggest that
Neurotensin (1-11) might contribute to normalization of neurotransmitter dynamics, decreasing the
likelihood of exacerbated states resulting in psychotic symptoms. This highlights its intriguing
potential as an adjunctive treatment multifaceted to existing antipsychotic medications.
The
analgesic properties of neurotensin and its fragments have also attracted attention in neurological
research, particularly for conditions involving chronic pain or abnormal Nociception. Neurotensin
(1-11), through its activation of NTS2, has shown to participate in descending pain-control pathways.
Laboratory models have provided insights into its efficacy in pain management, suggesting Neurotensin
(1-11) can attenuate pain signals, potentially offering relief where conventional analgesics fail or
lead to side effects.
Recent explorations in mood disorders have also opened new pathways for
research, with initial studies hinting Neurotensin (1-11) could influence mood regulation through its
broad neurotransmitter activity modulation, though more evidence is needed to fully comprehend its scope
in mood disorders like depression and bipolar disorder. This lines up with neuropeptide-based mechanisms
being investigated for treatment-resistant depression, providing a molecular rationale to consider such
peptides in next-generation antidepressants.
Neuroprotection represents another exciting research
frontier, with several in vitro and in vivo studies suggesting neurotensin and its derivatives might
confer protective benefits against neurodegenerative processes. Neurotensin's influence on oxidative
stress pathways, neuroinflammation, and apoptotic processes has paved the way to explore its therapeutic
roles in conditions like Alzheimer's and Parkinson's disease, though Neurotensin (1-11) in particular
awaits further elucidation of such capacities.
In summary, while research on Neurotensin (1-11)
continues to evolve, the peptide represents a promising therapeutic candidate in psychiatric and
neurological disorders due to its receptor interactions and comprehensive modulation of neurotransmitter
systems. Continued investigations are expected to deepen our understanding of its potential clinical
applications and therapeutic efficacy, providing novel avenues for treating complex brain
disorders.
What are the potential therapeutic applications of Neurotensin (1-11) in pain
management?
Neurotensin (1-11) holds substantial promise in the domain of pain management due to
its unique interactions with neurotensin receptors and its resultant modulation of pain pathways. Pain
perception and the experience of pain are highly complex processes that involve central and peripheral
pathways, neurotransmitter systems, and various types of receptors. Neurotensin's involvement in these
processes positions its peptide fragments like Neurotensin (1-11) as intriguing candidates for
developing novel pain therapeutics.
The potential of Neurotensin (1-11) in pain management is
primarily tied to its interaction with its receptors, especially NTS2, in the brain and spinal cord
which are involved in descending inhibitory pain pathways. Activation of NTS2 has been associated with
producing analgesic effects without engaging the opioid system, hence suggesting a non-opioid-targeted
approach to pain relief. This non-reliance on opioid pathways is of particularly significant interest as
it opens the door to managing pain without the risk of dependency and tolerance commonly seen with
opioid analgesics.
Studies demonstrate that Neurotensin (1-11) has the ability to alleviate both
acute and chronic pain forms in preclinical trials, offering a potential therapeutic avenue for patients
who experience neuropathic pain where traditional analgesics have limited effect. When injected into
animal models, Neurotensin (1-11) elicited responses indicative of reduced nociceptive processing,
underscoring its analgesic potential. This suggests its relevance not just in modulating acute pain
situations but providing benefits in chronic conditions such as fibromyalgia or complex regional pain
syndrome.
Moreover, its potential extends into inflammatory pain management as well, a hypothesis
supported by its role in modulating neurogenic inflammation pathways. Neurotensin fragments, including
Neurotensin (1-11), have shown effects on reducing inflammation through cytokine interaction modulation
which often exacerbates pain states in inflammatory diseases.
Another interesting potential of
Neurotensin (1-11) in pain management lies in comorbidity conditions such as cancer-related pain. Given
Neurotensin (1-11)’s putative roles in modulating neurogenesis and neurotransmission in the central
nervous system, the peptide may contribute to ameliorating pain associated with oncological states while
also possibly interacting within pathways related to cancer biology itself. However, due to its varied
activities, careful modulation and dosage studies are imperative to ascertain therapeutic window and
efficacy without unpredicted systemic effects.
In summary, the therapeutic applications of
Neurotensin (1-11) in pain management are centered around its complex interplay with neurotensin
receptors within pain pathways, offering compelling non-opioid analgesic potential and expanding
treatment options beyond traditional pharmacotherapy. Further research into its mechanisms and receptor
interactions continues to be pivotal in translating its preclinical promise into clinical reality.
Understanding how these peptides can be utilized safely and effectively forms the cornerstone of ongoing
investigations into their potential to redefine pain management therapies.