Having a suntan is fashionable in today’s society and is associated with an image of health and wellbeing. One only has to look at advertising billboards or popular television series to see the ideal suntanned physique associated with health and fame. This was not always the case, however; a tanned complexion is a fashion trend of the latter two-thirds of the 20th century.
In the 19th century, tanned skin was associated with field laborers and the working classes; the middle classes and the nobility had pale skin, in keeping with their socioeconomic status and social activity. In the 20th century, this situation was turned on its head and people without a suntan were those who could not afford holidays. The darker your skin and the longer you had a tan, the better. Gossip magazines showed the influential people of the moment with bronzed complexions enjoying long holidays on idyllic beaches. This was naturally reflected in the general population and there was an increase in tourism to sunny destinations.
Over the years, scientific progress has shown how harmful this fashion can be, as it has led to photoaging and an increase in different types of skin cancer. As a result, various sectors of the population who are unwilling to give up the coveted suntan have sought alternative methods of achieving it.In this article, I will focus on the drug melanotan.
WHAT IS MELANOTAN?
Melanotan is a lab-made chemical. Melanotan is a synthetic analog of alpha-melanocyte-stimulating hormone (α-MSH), a hormone belonging to the melanocortin group of peptide hormones, which have different functions in the body. It is similar to a hormone found in the body. It was originally made as a drug to help treat certain skin conditions. It is also sold over the internet as a supplement.
There are 2 synthetic melanotan molecules1–6:
Melanotan I ([Nle4-D-Phe7]-α-MSH) is a 13 amino acid linear peptide in which the fourth amino acid, methionine, is replaced with norleucine and the seventh amino acid, L-phenylalanine, is replaced with D-phenylalanine. This molecule is more resistant to breakdown than its natural analog, which means that the stimulus received by its receptor (principally MC1R) is more potent.
Melanotan II (Ac-Nle-[Asp-His-D-Phe-Arg-Trp-Lys]- α-MSH-NH2) is a shorter variant with a lactam ring. Like melanotan I, this analog is also more potent than natural α-MSH, but it also has more side effects because it is less receptor-specific. In addition to stimulating increased melanin production, this molecule also decreases appetite and increases libido.
Melanotan is commonly used for skin tanning. It is also used to produce erections in men with erectile dysfunction (ED), for rosacea, for fibromyalgia, and other conditions, but there is no good scientific evidence to support most of these uses. There is also concern that melanotan might not be safe when used as a shot under the skin.
Be careful not to confuse melanotan with melatonin.
How does it work ?
Melanotan is similar to a substance in our bodies, called “melanocyte-stimulating hormone.” This hormone increases the production of skin-darkening pigments. Melanotan might also work in the brain to stimulate erections of the penis.
Melanotan is similar to a substance in our bodies, called “melanocyte-stimulating hormone.” This hormone increases the production of skin-darkening pigments. Melanotan might also work in the brain to stimulate erections of the penis.
Melanotan Effect
Melanotan is a synthetic analog of alpha-melanocyte-stimulating hormone (α-MSH), a hormone belonging to the melanocortin group of peptide hormones, which have different functions in the body.1 α-MSH binds to different melanocortin receptors to produce different effects, including the following:
- Increases melanin production by binding to the melanocortin 1 receptor (MC1R), thereby stimulating production of different enzymes, including tyrosinase. It also appears to stimulate melanocyte proliferation.
- Produces erections and increases libido by binding to MC3R in the central nervous system. Unlike sildenafil, a phosphodiesterase-5 inhibitor that produces erections by means of a peripheral effect, it does not require sexual stimulation and its effect is longer-lasting.
- Decreased appetite. The anorexigenic effect is caused by the hormone binding centrally to the MC4R and peripherally to the MC2R; it also appears that it may affect lipolysis by binding to the MC5R.
- Immunomodulating effects. It appears to diminish the body’s inflammatory and immune responses.
- Vasopressor effects on the cardiovascular system that increase blood pressure.
- Changes in behavior. The effects in this regard are highly variable and may affect learning, attention, and motor coordination, in addition to modifying sexual and eating behaviors.
There are 2 synthetic melanotan molecules1–6:
Melanotan I ([Nle4-D-Phe7]-α-MSH) is a 13 amino acid linear peptide in which the fourth amino acid, methionine, is replaced with norleucine and the seventh amino acid, L-phenylalanine, is replaced with D-phenylalanine. This molecule is more resistant to breakdown than its natural analog, which means that the stimulus received by its receptor (principally MC1R) is more potent.
Melanotan II (Ac-Nle-[Asp-His-D-Phe-Arg-Trp-Lys]- α-MSH-NH2) is a shorter variant with a lactam ring. Like melanotan I, this analog is also more potent than natural α-MSH, but it also has more side effects because it is less receptor-specific. In addition to stimulating increased melanin production, this molecule also decreases
Possibly Effective for
Erectile dysfunction (ED). Most early research suggests that giving melanotan as a shot under the skin helps men with erectile dysfunction achieve and keep an erection. However, side effects like nausea mean that this is not the best product to use. Also, melanotan is now only available as an unregulated product over the internet.
Insufficient Evidence for
- Tanning of the skin.
- Preventing skin cancers due to sun exposure, when given as a shot under the skin.
- Rosacea.
- Fibromyalgia.
- Other conditions.
More evidence is needed to rate the effectiveness of melanotan for these uses.
What Are the Real or Potential Medical Uses of Melanotan?
The melanotan I and melanotan II molecules were originally developed to investigate their effects on melanin production with a view to achieving an increase in the natural photoprotective effect provided by this hormone. Both molecules proved to effectively increase melanin when injected and, furthermore, the type of melanin produced was eumelanin (which provides greater protection to cells than pheomelanin).1–3 However, as a side effect, melanotan II also produced penile erection. This led to research on Melanotan II as a photoprotector being abandoned and attention was focused on melanotan I, which is more selective of melanin production. Nevertheless, melanotan II did not disappear, but moved to another area of research: erectile dysfunction.1 Thus, we find that these two molecules have advanced in different areas:
Melanotan I (SCENESSE, Clinuvel Pharmaceuticals Ltd) is being studied in phase 2 and phase 3 clinical trials as a photoprotective drug for protection against nonmelanoma skin cancer and in other photoinduced skin diseases, such as erythropoietic protoporphyria, solar dermatitis, and polymorphic light eruption. The results of these trials appear to be promising.
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Melanotan II was replaced by a nasally administered molecule (PT-141, Palatin Technologies), which was studied in erectile dysfunction. It was found to produce erections by means of a central mechanism, unlike sildenafil, and to produce a lasting erection independent of sexual stimulation in 80% of patients who did not respond to sildenafil. Although promising, the molecule was never brought to market due to several patients presenting with high blood pressure. The same company is currently studying its use in hemorrhagic shock.
It should be noted that, while some studies contend that these molecules do not increase the risk of melanoma, their long-term effects are still not fully understood and concerns have been raised about secondary effects, such as the increased proliferation of melanocytes and reduced inflammatory and immune response.
Melanotan Side Effects
When given as a shot: Melanotan is POSSIBLY UNSAFE when given as a shot. It can causes nausea, stomachcramps, decreased appetite, flushing, tiredness, yawning, darkened skin, spontaneous erections of the penis, and other side effects. In some people, especially those with light skin, a change in the shape of moles, new moles, and skin cancer, have all occurred in people using melanotan.
When sprayed in the nose: There isn’t enough reliable information to know if melanotan is safe or what the side effects might be.
Special Precautions and Warnings
When given as a shot: Melanotan is POSSIBLY UNSAFE when given as a shot. It can causes nausea, stomachcramps, decreased appetite, flushing, tiredness, yawning, darkened skin, spontaneous erections of the penis, and other side effects. In some people, especially those with light skin, a change in the shape of moles, new moles, and skin cancer, have all occurred in people using melanotan.
When sprayed in the nose: There isn’t enough reliable information to know if melanotan is safe or what the side effects might be. Pregnancy and breast-feeding: There isn’t enough reliable information to know if melanotan is safe to use when pregnant or breast-feeding. Stay on the safe side and avoid use.
Pregnancy and breast-feeding：Not enough is known about the use of melanotan-II during pregnancy and breast-feeding.
Stay on the safe side and avoid use.
Interactions
POSSIBLY EFFECTIVE FOR
- Producing erections in men with ED (erectile dysfunction), when given as a shot under the skin.
- Tanning of the skin, when given as a shot under the skin.
ARE THERE SAFETY CONCERNS?
Melanotan-II is POSSIBLY SAFE when used under medical supervision for treating ED (erectile dysfunction).
It may cause nausea, stomach cramps, decreased appetite, flushing, tiredness, yawning, darkened skin, spontaneous erections of the penis, and other side effects.
There isn’t enough information to know whether melanotan-II is safe for other uses.
BY INJECTION UNDER THE SKIN
- For causing an erection in men with ED: the typical dosage of melanotan-II is 0.025 mg/kg
- For tanning skin: the typical dosage of melanotan-II is 0.025 mg/kg
Melanotan Store
Lyophilized Melanotan-II although stable at room temperature for 3 weeks, should be stored desiccated below -18°C. Upon reconstitution MT-II should be stored at 4°C between 2-7 days and for future use below -18°C.For long term storage it is recommended to add a carrier protein (0.1% HSA or BSA).Please prevent freeze-thaw cycles.
