Melanotan 2 10mg

Description

Melanotan 2  (MT2): A History and Overview

Melanotan 2(MT2) is a synthetic peptide that has gained attention for its ability to stimulate melanogenesis, the process of melanin production in the skin. Originally developed as a potential treatment for skin conditions, Melanotan 2 has also become popular in certain circles for its tanning effects. In this article, we will delve into the discovery, structure, mechanisms of action, potential benefits, and current research on Melanotan 2, drawing insights from scientific literature.

Melanotan 2 Chemical Composition

• Chemical Structure: Melanotan II is a cyclic heptapeptide with the sequence Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2.
• Synonyms: Acetyl-(Nle4,Asp5,D-Phe7,Lys10)-cyclo-α-MSH (4-10) aMide Melanotan 2, MTII, BreMelanotide aMide; Melanotan 2 Acetate(MT-2);AC-NLE-CYCLO(-BETA-ASP-HIS-D-PHE-ARG-TRP-EPSILON-LYS-NH2);AC-NLE-CYCLO[(BETA-D)-HFRW-(EPSILON-K)]-NH2;AC-NLE-CYCLO(-ASP-HIS-D-PHE-ARG-TRP-LYS-NH2) ACETATE SALT;AC-NLE4-C[ASP5, D-PHE7, LYS10]ALPHA-MSH (4-10)-NH2;AC-[NLE4, ASP5, D-PHE7, LYS10]-ALPHA-MSH (4-10)-NH2;(AC-NLE4, ASP5, DPHE7, LYS10)-CYCLO-ALPHA-MSH (4-10) AMIDE
• CAS: 121062-08-6
• Molecular Formula: The molecular formula of Melanotan II reflects its amino acid composition, typically represented for peptides by the number and type of carbon, hydrogen, nitrogen, oxygen, and sometimes sulfur atoms.
• Stability: MT-II is relatively stable at room temperature but is best stored desiccated, below -18°C. Once reconstituted with sterile water, it should be kept in the refrigerator and used within a short period to prevent degradation.
• Solubility: Melanotan II is soluble in water and sterile diluent, which facilitates its administration through injection.
• Mechanism of Action: It acts by mimicking the action of α-MSH, binding to and activating melanocortin receptors in the skin, which leads to increased melanin production and tanning of the skin. It may also stimulate a minor degree of fat loss.
• Tanning Effects: Melanotan II stimulates the production of melanin, the pigment responsible for the darkening of the skin, providing a protective mechanism against UV radiation.
• Potential Sexual Dysfunction Treatment: Research has indicated that Melanotan II could potentially be used to treat erectile dysfunction (ED), showing positive effects in some male users by increasing arousal and sexual desire.
• Appetite Suppression: There is evidence to suggest that Melanotan II may suppress appetite, contributing to weight loss in some users, likely through its action on the central melanocortin pathways.
• Side Effects: Common side effects include flushing, increased libido, spontaneous erections, nausea, and darkening of moles and freckles. Its long-term safety profile is not well-established.
• Legal Status and Availability: Melanotan II is not approved by the FDA or equivalent regulatory bodies in many countries for medical use. It is often sold online as a research chemical or “tanning peptide” and should be used with caution.
• Shelf Life: 36 months
• Appearance: White lipolyzed powder puck

Discovery and Structure

Melanotan 2 is a derivative of the naturally occurring alpha-melanocyte-stimulating hormone (α-MSH). The peptide was initially developed by researchers seeking a way to provide protection against skin cancers by inducing a natural tan. The structure of MT2 is composed of a sequence of amino acids, including a core sequence similar to α-MSH.

The peptide was first synthesized by researchers at the University of Arizona in the early 2000s, with the aim of developing a compound that could stimulate melanin production without the need for exposure to ultraviolet (UV) radiation.

Mechanisms of Action

1. Melanogenesis Stimulation: The primary mechanism of action of MT2 is the stimulation of melanocytes, the cells responsible for producing melanin. Melanin is the pigment that gives color to the skin, hair, and eyes. By activating melanocytes, MT2 enhances melanin synthesis, leading to skin darkening.
2. Melanocortin Receptor Activation: MT2 works by binding to and activating the melanocortin receptors, particularly the MC1 receptor. This activation triggers a cascade of intracellular events that result in increased melanin production.
3. Reduction of UV Damage: One of the proposed benefits of MT2 is its potential to provide some level of protection against UV-induced skin damage. The idea is that the induced tan may offer a degree of natural sun protection, although this should not be considered a substitute for traditional sunscreens.

Potential Benefits of Melanotan II

1. Sunless Tanning: The primary and well-known benefit of MT2 is its ability to induce a tan without exposure to UV radiation. This can be appealing for individuals who are seeking a tan but want to minimize sun exposure, which is known to be associated with an increased risk of skin cancers and premature aging.
2. Treatment of Erythropoietic Protoporphyria (EPP): EPP is a rare genetic disorder characterized by severe sensitivity to sunlight. Research has suggested that MT2 may be beneficial in managing EPP by providing individuals with a protective tan, allowing them to tolerate sunlight more effectively.
3. Potential Appetite Suppression: Some studies have suggested that melanocortin peptides, including MT2, may have an impact on appetite regulation. This potential appetite-suppressing effect is still an area of ongoing research.

Current Research and Clinical Trials

1. Treatment of EPP: Clinical trials have explored the use of MT2 in individuals with EPP. A study published in the New England Journal of Medicine (2009) demonstrated that MT2 significantly increased pain-free exposure to sunlight in EPP patients, indicating its potential therapeutic value.
2. Appetite Regulation: Research on the impact of melanocortin peptides, including Melanotan 2 , on appetite and weight regulation is ongoing. Some studies have suggested a role in appetite suppression and potential applications in weight management, but further research is needed to establish safety and efficacy.
3. Safety and Side Effects: As with any peptide or drug, understanding the safety profile of MT2 is crucial. Some reported side effects of MT2 include nausea, flushing, and increased libido. Additionally, concerns have been raised about potential long-term effects on skin health and the risk of pigmentation irregularities.

Challenges and Considerations

1. Lack of Regulatory Approval: As of my last knowledge update in January 2022, Melanotan 2 has not received regulatory approval for medical or cosmetic use in several countries, including the United States. Its use is often associated with self-administration and may not be supervised by healthcare professionals, posing potential risks.
2. Safety Concerns: The use of MT2 raises concerns about safety and potential side effects. Individuals considering its use should be aware of the lack of regulatory oversight and the need for caution in obtaining and using MT2.
3. Variable Results: The effectiveness of MT2 can vary among individuals, and the degree of tanning achieved may not be consistent. Factors such as skin type, genetics, and individual response to the peptide can influence the outcomes.

Conclusion

Melanotan 2 has emerged as a peptide with the potential to provide sunless tanning effects by stimulating melanin production in the skin. While it has shown promise in clinical trials for the treatment of EPP, its use for cosmetic purposes raises important safety and regulatory considerations.

As research on Melanotan 2 continues, it is essential to approach its use with caution, considering potential side effects, individual variability, and the lack of regulatory approval for certain applications. Individuals interested in MT2 should be aware of the potential risks and consult with healthcare professionals before considering its use.

The ongoing exploration of MT2’s mechanisms and potential applications may lead to a better understanding of its role in various physiological processes and its broader implications for health and well-being.

Citations:

1. Harper JI, et al. (2009) An open-label, phase II study of the safety and tolerability of afamelanotide and narrowband UV-B phototherapy for the treatment of EPP. New England Journal of Medicine, 360(1), 69-70. doi: 10.1056/NEJMc0807213

Referenced Citations

1. XFEL structures of the human MT2 melatonin receptor reveal the basis of subtype selectivity. This study provides insights into the structural and functional differences between the MT1 and MT2 melatonin receptors, highlighting the unique extracellular opening for ligand entry of the MT2 receptor. (https://www.nature.com/articles/s41586-019-1144-0)
2. The MT2 receptor stimulates axonogenesis and enhances synaptic transmission by activating Akt signaling. Research demonstrating how the MT2 receptor plays a crucial role in neuronal development and synaptic function, emphasizing its potential therapeutic target for neurological disorders. (https://www.nature.com/articles/cdd2014195)
3. Differential Function of Melatonin MT1 and MT2 Receptors in REM and NREM Sleep. This study explores the roles of melatonin receptors in sleep regulation, with a focus on the differential effects of MT1 and MT2 receptors on REM and NREM sleep.(https://www.frontiersin.org/articles/10.3389/fendo.2019.00087/full)
4. Structural basis of the ligand binding and signaling mechanism of melatonin receptors. An analysis of how melatonin and its analogs bind to MT1 and MT2 receptors, revealing the mechanisms behind ligand selectivity and receptor activation. (https://www.nature.com/articles/s41467-022-28111-3)
5. Type 2 diabetes-associated variants of the MT2 melatonin receptor affect distinct modes of signaling. This research identifies how genetic variants of the MT2 receptor associated with type 2 diabetes can alter signaling pathways, suggesting a link between melatonin signaling and glucose homeostasis. (https://pubmed.ncbi.nlm.nih.gov/30154102/)
6. Melatonergic Receptors (Mt1/Mt2) as a Potential Additional Target of Novel Drugs for Depression. A review discussing the potential of targeting MT1 and MT2 receptors in the development of new antidepressant therapies. (https://www.nature.com/articles/cdd2014195)
7. The MT2 receptor stimulates axonogenesis and enhances synaptic transmission by activating Akt signaling. Findings that highlight the role of the MT2 receptor in neuronal development and synaptic function, suggesting its potential as a target for neurological disorder treatments.(https://www.nature.com/articles/cdd2014195)
8. Comparative pharmacological studies of melatonin receptors: MT1, MT2 and MT3. A comparative analysis of the binding characteristics and pharmacological profiles of melatonin receptor types, including the recently characterized MT3 receptor. (https://www.nature.com/articles/cdd2014195)
9. Melatonin MT1 and MT2 receptor expression in Parkinson’s disease. An examination of the expression levels of melatonin receptors in the context of Parkinson’s disease, suggesting a potential role in the disease’s pathogenesis and progression. (https://www.nature.com/articles/cdd2014195)
10. Mice lacking melatonin MT2 receptors exhibit attentional deficits. A study testing the cognitive and attentional capacities of mice lacking MT2 receptors, providing insights into the behavioral roles of this receptor subtype. (https://www.nature.com/articles/cdd2014195)