Melanotan II acts as a non-selective agonist of the melanocortin receptors, MC1, MC3, MC4, MC5. To the extent that melanotan II produces melanogenesis, this is thought to be caused by activation of the MC1 receptor, whereas its clinically documented sexual effects are thought to be related to its ability to activate the MC4 receptor (though the MC3 is thought to possibly also be involved).
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Melanotan-2 (MT-2) is a cyclic hepapeptide analog of α-melanocyte-stimulating hormone (α-MSH), respectively. it is a synthetically produced variant of the α-MSH peptide hormone naturally found in the body. Alpha-Melanocyte Stimulating Hormone is a natural endogenous melanotanic peptide hormone of the melanocortin family. It considers the most important among melanocyte-stimulating hormones when taking into account the ability to stimulate melanogenesis. Stimulation of melanogenesis is the process responsible for pigmentation of the hair and skin of mammals. α-MSH is a non-selective melanocortin receptor agonist MC1, MC3, MC4 and MC5. It is through melanocortin receptors that the MT-2 peptide has a strong effect on fat metabolism, apethy, erection, and libido. Melanotan 2 activates the MC1 receptor, which is responsible for skin pigmentation effects.
The peptide further stimulates the MC4 receptor, which acts to improve erection and increase libido. Thanks to its melanogenic capabilities, MT-2 is also used as a protection against ultraviolet sunlight and its negative effects on human health. The origins of the production of the synthetic peptide Melanotan 2 are attributed to the University of Arizona. In the course of research to develop skin cancer protection, the emphasis has been put on creating a method that would naturally stimulate melanogenesis or natural melanin production in the skin without directly subjecting the subject to dangerous ultraviolet radiation from the sun. Initially, Arizona University researchers attempted to directly deliver the naturally-occurring a-MSH hormone to achieve the desired result, which yielded promising results.
However, it has been shown that natural a-MSH has an excessively short biological half-life to be used as a medicine. However, positive results from a-MSH administration have been triggered by further research that has led to the development of Melanotan 1 (MT-1) and Melanotan 2. Melanotan 2 has similar effects compared to the previous version (MT-1) but has a longer biological half-life and is therefore suitable for effective therapeutic use. Unlike the MT-1 precursor, the MT-2 peptide demonstrated aphrodisiac properties (a libido-promoting side effect). Laboratory mice also examined the effects of MT-2 on nutrition and intake of food. It was found that central melanocortin (MC) was activated and blocked immediately after application of the peptide to mice. Six-day treatment with Melanotan 2 confirmed that the peptide caused loss of body weight and adipose tissue in the internal organs of mice and suppressed the supply of calories to the body. This fact finds use in clinical therapy and provides a possible way to reduce carbohydrate or calorie intake, especially in overweight and obese patients. This study also demonstrated a sustained increase in the consumption of oxygen present in obese animals. The Melanotan 2 peptide has proven to reduce insulin levels, increase fat catabolism in the muscles, and even improve cholesterol metabolism. Further study results have shown that MT-2 reduces the expression level of acetylcholine A carboxylase and even provides prevention of the loss of carnitine mRNA and palmitol transferase I in muscle-type tissue by parenteral feeding of obese rats.
When investigating the effects of Melanotan 2 on human subjects, it has been confirmed that this peptide causes significant skin tanning together with side effects such as, spontaneous erections and increased libido also on humans. In the relevant study records, the effects of improved tanning were confirmed in all volunteers tested, and the effects of increasing libido and erection hardness were confirmed in nine of the ten male volunteers tested.
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