MIF-1

MIF-1 (Peptide) – Product Details

MIF-1, or Melanocyte-Inhibiting Factor-1, is a neuropeptide associated with the regulation of various physiological functions, including mood, stress responses, and pain perception. Derived from the precursor protein pro-opiomelanocortin (POMC), MIF-1 plays a role in modulating neurotransmitters like dopamine and serotonin. Ongoing research explores its potential implications in addressing mood disorders, stress-related conditions, and pain management, attracting interest in scientific and medical investigations.

• CAS Number: 478336-92-4
• Molar Mass: 284.35 g/mol
• Chemical Formula: C₁₅H₂₅F₃N₄O₅
• IUPAC Name: Pro-Leu-Gly-NH2

What is MIF-1?

Melanostatin, or MIF-1 (Melanocyte-inhibiting factor), is an endogenous peptide formed through the cleavage of oxytocin. Unlike its precursor, MIF-1 has diverse effects, acting as both an opioid receptor blocker and a positive allosteric modulator for dopamine receptors (specifically D2 and D4). It also inhibits the release of neuropeptides like alpha-MSH and enhances melatonin activity. This peptide demonstrates a multifaceted profile, offering antidepressant, nootropic, and anti-Parkinsonian effects.

Researchers explore related peptides like Tyr-MIF-1 and endomorphin-1 and -2, providing a broader understanding of their interconnected roles. In addition, Melanostatin, known for regulating melanocyte-stimulating hormone release, is identified as a specific tripeptide, L-prolyl-L-leucylglycinamide. Sharing similarities with the end part of oxytocin, Melanostatin enhances the effects of L-dopa and 5-hydroxytryptophan, counteracting induced tremors. These findings suggest a direct impact on brain function. [R] [R]

How Does MIF-1 Work?

In the central nervous system (CNS), melanostatin (MIF-1), a naturally occurring tripeptide (Pro-Leu-Gly-NH2), is an important positive allosteric modulator (PAM) of dopamine D2 receptors (D2R). By attaching to allosteric regions, this modulation causes conformational changes that improve the affinity with which orthosteric ligands bind to the receptor. Although MIF-1 is known to have potential uses in neurological conditions such as Parkinson’s disease (PD), it has drawbacks including low stability against enzymes produced by the central nervous system and low gastrointestinal absorption, which makes oral delivery in subjects difficult. [R]

Studies investigated a bioisosteric replacement of cyclic β-amino acids with the prolyl residue as a means of improving MIF-1’s pharmacokinetic profile without compromising its PAM activity in order to solve these problems. This alteration resulted in the design, synthesis, and pharmacological assessment of six new MIF-1 proline mimetics. During functional tests at D2R, one of these peptidomimetics outperformed MIF-1 neuropeptide at 1 nM in terms of performance (lower EC50). Crucially, in developed human neuronal SH-SY5Y cells, this drug did not show any cytotoxic effects at 100 µM. [R]

Studies are being conducted to evaluate this promising proline mimetic’s chemical stability and in vitro biological permeability. It now has more options to create alternative anti-Parkinson medicines because of the identification of a strong D2R PAM with a good safety profile. [R]

In the context of melanostatin’s effects, its ability to influence behavior and neurotransmitter levels underscores its potential interactions with the blood-brain barrier. Melanostatin’s capacity to modulate brain dopamine levels and its metabolite, homovanilic acid, suggests that it has the potential to interact with the brain’s neurotransmitter systems. This interaction could involve melanostatin crossing the BBB or affecting the BBB’s permeability to certain molecules. Although the precise mechanism by which melanostatin influences the BBB remains to be fully elucidated, its impact on neurotransmitter levels indicates that it interacts with the brain at a molecular level.  [R] 

MIF-1 Potential Applications

Below are other research-based potential benefits MIF-1 could bring:

MIF-1 on Brain Activity

Melanostatin (MIF-1), when administered into the brain’s ventricles, has been found to enhance electrical activity in various brain regions, including the neocortex, amygdala, hippocampus, and hypothalamus. This enhancement is seen in specific frequency ranges, such as the 3-7/sec high-voltage activity in multiple brain areas and the 7-12/sec activity in the neocortex. Interestingly, the effects of MIF-1 are influenced by morphine; morphine amplifies the impact of MIF-1, while pre-administration of MIF-1 can counteract the effects of low doses of morphine. Additionally, when the central nucleus of the amygdala is lesioned, the responsiveness of the nearby neocortex is diminished, but the responsiveness of the hippocampus remains intact. These findings contribute to our understanding of how MIF-1 influences brain activity, and they suggest potential interactions with opioid-related processes. This information is based on scientific research and is not intended for immediate application or use without further clinical investigation. [R] 

MIF-1 on Tremors

Melanostatin (MIF-1) is a peptide that influences the central nervous system. According to research, MIF-1 may lessen the symptoms of clinical Parkinsonism and counteract the effects of a cholinergic chemical linked to Parkinson’s disease in animals. An unusual dose-effect connection has been noted, wherein tremors are inhibited by MIF-1 and its equivalents up to a specific dose, at which point the impact becomes less pronounced. Additionally, the data raises the possibility that these peptides function via a common pathway. These results add to the understanding of the effects of MIF-1 and similar peptides on neuronal transmission, even though the precise mechanism is yet unknown. They may also have ramifications for future therapeutic uses. This information is based on scientific research and is not intended for immediate application or use in humans.  [R]

MIF-1 on Dopamine Release in the Brain of Subject

In a study, scientists investigated the impact of Melanostatin (MIF-1) and thyroliberin (TRH) on dopamine production and release in the brain. The findings suggest that MIF-1 and TRH do not influence dopamine production, but they do stimulate dopamine release from vesicular stores in a calcium-dependent manner. This means that these substances may play a role in regulating the release of dopamine, a neurotransmitter associated with mood and pleasure, through a mechanism involving calcium levels. Understanding these processes could have implications for mental health and neurological function. It is important to stress that these studies are being carried out for scientific purposes and are not meant for use by humans. [R]

MIF-1 on Potential for Emotional Responses

Animal research has shown that melanostatin (MIF-1) has an emotiotropic (emotion-modulating) influence on emotional reactivity. Although MIF-1 is not categorized as a conventional antidepressant, it functions similarly to that of other neurological medications. In experiments simulating depression, MIF-1 activates aggressive-defensive behavior in situations of reserpine-induced depression and reduces provoked aggressive behavior in haloperidol-induced depression. Reserpine counteracts hypothermia, improves muscular tone, and removes ptosis in animal models. Moreover, it reduces the catalepsy brought on by haloperidol. Significantly, it has been discovered that MIF-1 raises dopamine and homovanilic acid, a metabolite of dopamine, in the brain. These findings suggest potential modulatory effects of MIF-1 on emotional responses and neurotransmitter levels, but further research is needed before considering any practical applications. [R]

MIF-1 on Skincare Potential

Melanostatin, or MIF-1, is a peptide that belongs to the emerging class of cosmeceutical peptides. Its chemical properties make it a promising candidate for skincare applications. These peptides are essential for regulating a wide range of skin-related functions, including angiogenesis, melanogenesis, inflammation, migration of cells, and protein synthesis. MIF-1 belongs to the class of peptides that modulate neurotransmitters in the cosmeceutical domain. MIF-1 offers an interesting alternative for research, even though lysine-threonine-threonine-lysine-serine (KTTKS), which is found in type I procollagen, is a peptide that is frequently investigated in cosmetics. Because of its unique chemical makeup, it has the capacity to prevent melanin from forming in cells that produce melanin, which presents a promising treatment option for skin-darkening issues. Moreover, MIF-1 is a member of the group of peptides that have the capacity to control melanogenesis, a crucial mechanism controlling skin pigmentation.  [R]

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Conclusion

In conclusion, Melanostatin, or MIF-1 (Melanocyte-inhibiting factor), emerges as a fascinating endogenous peptide with a diverse range of potential effects. As a product of oxytocin cleavage, MIF-1 acts as both an opioid receptor blocker and a positive allosteric modulator for dopamine receptors, offering a unique profile with antidepressant, nootropic, and anti-Parkinsonian properties. Despite challenges with oral bioavailability in subjects, MIF-1 showcases remarkable resistance to metabolism and effective crossing of the blood-brain barrier, enhancing its therapeutic potential.

Ongoing research explores related peptides and investigates a bioisosteric replacement strategy to improve MIF-1’s pharmacokinetic profile. The identification of a potent D2R-positive allosteric modulator with a favorable safety profile opens new possibilities for developing alternative anti-Parkinson medicines.

Furthermore, studies on MIF-1’s impact on dopamine release, tremors, brain activity, emotional responses, and skincare applications reveal its multifaceted nature. MIF-1’s potential interactions with neurotransmitter systems and its modulation of various physiological processes suggest promising avenues for future therapeutic applications. However, it is essential to emphasize that these studies are conducted for scientific purposes, and further research is required before considering practical applications, especially in human subjects.

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Strength	5mg

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