Taiy Chemical
(D-Trp11)-Neurotensin
Synonym D-Trp11-Neurotensin
Species Human
Protein Accession P30990
Purity Greater than 95% as determined by SEC-HPLC and reducing SDS-PAGE
Endotoxin Level Less than 1 EU/µg of protein as determined by LAL method
Biological Activity The ED50 for this effect is typically 0.1-0.3 μM
Expression System E. coli
Fusion Tag None
Predicted Molecular Mass 2.9 kDa
Formulation Lyophilized from a 0.2 μm filtered solution of 20% acetonitrile, 0.1% TFA
Reconstitution It is recommended to reconstitute the lyophilized D-Trp11-Neurotensin in sterile 18 MΩ-cm H2O not less than 100 µg/ml, which can then be further diluted to other aqueous solutions
Storage & Stability Store at -20°C. Upon reconstitution, store at 4°C for up to 3 days or freeze at -20°C for future use
FAQ
What is (D-Trp11)-Neurotensin and how does it work in the body?

(D-Trp11)-Neurotensin is a synthetic analog of the naturally occurring neuropeptide, neurotensin. Neurotensin is a tridecapeptide that plays a significant role in the central nervous system as well as in peripheral tissues. It is involved in various biological processes, such as the regulation of dopamine pathways, modulation of pain, and influencing body temperature control. The (D-Trp11) modification refers to the substitution of tryptophan at the 11th position with D-tryptophan in the peptide sequence, which can enhance stability and bioavailability, making it more effective for research and potential therapeutic applications.

In the CNS, neurotensin exerts its effects mainly through three known receptors: NTS1, NTS2, and NTS3. These receptors are G-protein coupled receptors (GPCRs), with NTS1 and NTS2 being most involved in mediating its central effects. The activation of neurotensin receptors can modulate neurotransmitter release, impacting several neurological pathways. For instance, neurotensin has been shown to influence the release of dopamine, a neurotransmitter critical for reward, motivation, and motor control, making (D-Trp11)-Neurotensin a molecule of interest in studying conditions like schizophrenia, Parkinson's disease, and substance abuse disorders.

In addition to its roles in the brain, neurotensin is involved in digestive tract regulation. It influences intestinal motility and increases the secretion of digestive enzymes, impacting nutrition absorption and gut function. The action of (D-Trp11)-Neurotensin, with its design to resist degradation, could offer insights into gut physiology and potential treatments for gastrointestinal disorders.

Furthermore, (D-Trp11)-Neurotensin may also be of research interest for its analgesic properties. By acting on the descending pain modulatory system, it can modify the perception of pain, offering a potential pathway for new analgesic drugs for managing acute and chronic pain conditions without the side effects associated with traditional opioids. Research is ongoing to explore the full scope of (D-Trp11)-Neurotensin and its analogs in therapeutic applications and their ability to modulate neurotensin pathways used in clinical applications.

What are the potential therapeutic applications of (D-Trp11)-Neurotensin?

(D-Trp11)-Neurotensin, given its origins from the neuropeptide neurotensin, presents a variety of potential therapeutic applications primarily due to its diverse physiological and neurological roles. One of the most promising areas is in the treatment of psychiatric disorders. Neurotensin’s interaction with dopamine pathways in the brain suggests this compound could be relevant in research targeting conditions like schizophrenia, which is characterized by dopaminergic dysregulation. By modulating dopamine pathways, (D-Trp11)-Neurotensin holds the potential to ameliorate symptoms or provide an adjunct to existing antipsychotic treatments.

Moreover, (D-Trp11)-Neurotensin’s involvement in the mechanism of pain perception presents another therapeutic avenue. Neurotensin exerts analgesic effects by modulating pathways in the central and peripheral nervous systems, offering an alternative to opioid-based treatments for pain management. This is particularly important as the medical community seeks non-opioid solutions to manage pain and counter the opioid epidemic. The analgesic property of (D-Trp11)-Neurotensin could contribute to developing new analgesics that offer effective pain relief with minimal risk of addiction and other serious side effects associated with traditional painkillers.

In addition, (D-Trp11)-Neurotensin is being researched for its role in managing neurodegenerative diseases such as Parkinson’s. Through its regulatory effects on dopamine, neurotensin analogs might help in offsetting the dopaminergic decline seen in Parkinson’s disease, providing symptomatic relief or potentially influencing disease progression. Improved motor control and neuroprotection are areas of interest where (D-Trp11)-Neurotensin could make significant contributions.

Besides neurological and psychiatric conditions, (D-Trp11)-Neurotensin has potential applications in gastrointestinal health. Its role in regulating gastrointestinal motility and secretion suggests therapeutic potentials for disorders such as irritable bowel syndrome (IBS) and other gastrointestinal motility disorders. By targeting neurotensin pathways, treatments could be developed that help normalize gut movement and secretion, improving quality of life for those affected by these conditions.

Overall, while clinical applications are still under exploration, the unique properties of (D-Trp11)-Neurotensin present a wide spectrum of potential therapeutic uses. Continued research into its mechanisms and effects will be crucial in the translation of this peptide into therapies that address some of the pressing health challenges in the modern world.

How does (D-Trp11)-Neurotensin interact with dopamine pathways, and what implications might this have for dopamine-related disorders?

(D-Trp11)-Neurotensin interacts with dopamine pathways primarily through neurotensin receptors, particularly NTS1, which are co-localized in dopaminergic regions of the brain such as the substantia nigra and the ventral tegmental area. These regions are critical in modulating motor activity, reward processing, and the pathophysiology of several psychiatric and neurological disorders. By binding to its receptors, (D-Trp11)-Neurotensin can modulate dopamine release, inhibit dopamine reuptake, and influence dopaminergic neuron activity.

In the context of dopamine-related disorders, such as schizophrenia and Parkinson's disease, the actions of (D-Trp11)-Neurotensin present significant clinical interest. In schizophrenia, an excess of dopamine activity, particularly in certain pathways, is thought to contribute to the positive symptoms such as delusions and hallucinations. (D-Trp11)-Neurotensin may help mediate these symptoms by influencing the dopaminergic signaling mechanism, providing a modulatory effect that could augment the efficacy of antipsychotic medications or offer alternative pathways for symptom management.

Conversely, in Parkinson’s disease, where there is a deficiency of dopamine due to the degeneration of dopaminergic neurons, modulating neurotensin pathways may offer symptomatic relief. Neurotensin’s interaction with dopamine pathways could lead to enhanced dopaminergic activity, helping to restore the balance and improve motor function and other symptoms in affected individuals. Furthermore, neurotensin analogs like (D-Trp11)-Neurotensin are being explored for their potential neuroprotective effects which could slow neuronal loss and alter disease progression.

Beyond these disorders, dopamine dysregulation is also implicated in substance use disorders. The reward pathways involved in addiction are heavily dopaminergic, and (D-Trp11)-Neurotensin could contribute to rebalancing neurotransmitter release and receptor sensitivity. By modifying dopamine signaling, there is potential for (D-Trp11)-Neurotensin to impact craving, withdrawal, and relapse rates, contributing to more effective addiction treatments.

In essence, the interaction of (D-Trp11)-Neurotensin with dopamine pathways holds profound implications for understanding and addressing a variety of dopamine-related disorders. By influencing the delicate balance of neurotransmitters, this peptide could inform and enhance therapeutic strategies for conditions characterized by both excesses and deficiencies in dopamine signaling. Continued research is crucial in elucidating the precise role and potential of (D-Trp11)-Neurotensin in these contexts, advancing both our understanding and treatment of complex neurochemical disorders.

What are the potential side effects or risks associated with (D-Trp11)-Neurotensin?

As with any compound that interacts with central nervous system pathways, (D-Trp11)-Neurotensin carries potential side effects and risks, though much research is still needed to fully understand them. Since (D-Trp11)-Neurotensin influences key neurotransmitter systems, unintended modulation could lead to various physiological and psychological reactions. One of the primary concerns in modulating neurotensin and dopamine pathways is the risk of affecting mood and cognition. These pathways are involved in regulating emotions, so disruptions could potentially lead to mood swings, anxiety, or cognitive disturbances. Individuals with a predisposition to mood disorders might experience exacerbations in their condition if neurotensin levels are altered inappropriately.

Another possible risk of (D-Trp11)-Neurotensin use is motor function impairment. Given its interaction with the dopaminergic system, which plays a crucial role in motor control, there is a potential for motor disturbances. These could manifest as tremors, rigidity, or involuntary movements, similar to what is observed in conditions with dopaminergic dysregulation such as Parkinson's disease. Such motor side effects would need careful management, particularly in clinical scenarios.

Autonomic side effects might also occur, as neurotensin is involved in regulating many autonomic functions including temperature regulation and appetite. Alterations in these pathways could lead to hyperthermia or hypothermia, changes in appetite, or gastrointestinal discomfort. Such effects highlight the importance of finely-tuned dosing and administration to minimize risks.

Furthermore, manipulating the neurotensin system could impact pain perception. While (D-Trp11)-Neurotensin is being explored for pain management, inappropriate use could paradoxically alter pain sensitivity, possibly leading to hyperalgesia or reduced pain tolerance, particularly if receptor downregulation occurs with long-term use.

Lastly, receptor-specific effects also pose potential risks. Depending on the preferential activation of NTS1, NTS2, or NTS3 receptors, diverse biological responses can be elicited, some of which could be undesirable. The use of (D-Trp11)-Neurotensin could lead to unintended receptor interactions, emphasizing the need for precise targeting and understanding of receptor pharmacodynamics and pharmacokinetics in therapeutic contexts.

Overall, while (D-Trp11)-Neurotensin holds therapeutic promise, these potential side effects underscore the need for extensive research and cautious advancement through clinical trials to ensure safety and efficacy. Determining optimal dosing, delivery methods, and patient populations is critical, emphasizing personalized medicine approaches to minimize risks while maximizing therapeutic benefits.

How is (D-Trp11)-Neurotensin expected to impact future research or treatment in the medical field?

(D-Trp11)-Neurotensin represents a promising molecule that could significantly impact future research and treatment paradigms across several medical fields, owing to its multifaceted biological roles. This peptide analog is poised to enhance our understanding and management of neurological, psychiatric, and gastrointestinal disorders, among others, bringing new insights that could translate into innovative therapies.

In neuroscience, (D-Trp11)-Neurotensin is expected to drive forward research in understanding neurotransmitter dynamics, particularly those involving dopamine and neuropeptide interactions. It offers unique opportunities to explore how neurotensin modulates central nervous system activity and behavior. This can deepen insights into disorders characterized by dopaminergic dysregulation, such as schizophrenia and Parkinson’s disease, potentially resulting in novel targeted therapies or adjunct treatments that provide more nuanced control over neurotransmitter systems.

For psychiatric conditions, (D-Trp11)-Neurotensin could pave the way for advancements in the treatment of mood and psychotic disorders. By elucidating its role in emotion regulation and stress, researchers could develop new therapeutic strategies that integrate neurotensin-based interventions with existing treatments, potentially improving outcomes for patients with depression, anxiety, or bipolar disorder. Furthermore, these insights might contribute to the development of biomarker-driven approaches, allowing for more personalized and effective mental health care.

The field of pain management could also see substantial advancements with (D-Trp11)-Neurotensin. As researchers continue to characterize its analgesic properties, it could lead to the development of novel pain relief medications that avoid the pitfalls of opioid use. This is particularly crucial in the context of the ongoing opioid crisis, highlighting the need for effective alternatives that mitigate pain with a lower risk of addiction and side effects.

In gastroenterology, this neuropeptide analog may offer new therapeutic options for digestive system disorders. Its role in modulating gut motility and secretion is an area rich with potential for developing treatments for conditions like irritable bowel syndrome and inflammatory bowel diseases. By targeting neurotensin pathways, researchers may discover ways to fine-tune gut function, enhancing patient outcomes and quality of life.

Moreover, (D-Trp11)-Neurotensin could impact the broader field of personalized medicine. As we learn more about individual variability in neurotensin receptor expression and function, there is potential to tailor treatments to individual neurobiological profiles, optimizing therapeutic efficacy and minimizing adverse effects.

Overall, (D-Trp11)-Neurotensin is likely to be an influential tool in both research and clinical settings, spurring new lines of inquiry while also offering tangible benefits for patient care. Ongoing studies and clinical trials will be pivotal in unlocking its full therapeutic potential, heralding an era of more targeted and effective interventions across a range of challenging medical conditions.
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