Melanotan II Dosage

Melanotan II is a laboratory-synthesized analogue of α-melanocyte-stimulating hormone (α-MSH) whose main function is to stimulate the process of melanogenesis, resulting in efficient and accelerated skin tanning. This peptide is naturally synthesized in the pituitary gland and is always present in the body in certain amounts. Another effect is an increase in sexual arousal, especially in men when it causes an erection. This can potentially be used effectively in treating erectile dysfunction. Scientists assume this peptide could also be used as part of the therapy for certain skin conditions, such as rosacea or fibromyalgia. This amino acid sequence was developed to succeed afamelanotide ("Melanotan I"), a registered drug that works by a similar mechanism of action. This compound is most often used in the female population who want a tan, so abuse and overuse occur, which can often lead to serious side effects. Therefore, the responsible use of Melanotan II is always advised.

Dosage Chart

Timeline	1-12 weeks	12-24 week
Protocol for treating erectile dysfunction in men	0.025 mg/kg (one subcutaneous injection daily)	0.025 mg/kg Dosage can be tapered gradually (one subcutaneous injection daily)

About the Peptide

Melanotan II was synthesized in the laboratory to succeed afamelanotide ("Melanotan I"), which has a similar mechanism of action but is approved for use and is most often used to treat erythropoietic protoporphyria. This peptide is an analogue of α-melanocyte-stimulating hormone (α-MSH), which is naturally produced in the pituitary gland and regulates the work of skin cells that produce pigment. They function according to a negative feedback system, so when enough pigment is produced, a signal is sent that additional production is unnecessary.

Melanotan II leads to dysregulation, so the signals to stop additional secretion are significantly reduced, and melanogenesis is accelerated. As a result, a person tans much faster, which is its most common indication, when it serves as a supplement. But it is also responsible for various events in the body.

Another effect is a possible increased sexual desire, which occurs especially in men in the form of sudden and frequent erections. For a healthy man, this can be an unwanted effect and interfere with everyday life. Still, it can also represent a potential therapeutic tool in the treatment protocol of erectile dysfunction. Whether the cause of impotence is psychogenic or physical, various studies show an improved condition and the occurrence of spontaneous erections in men who received Melanotan II. Also, in all cases, the erection lasted an average period and ended with ejaculation, which speaks of the successful effect.

The mechanism of action is based on increased activation of the part of the central nervous system responsible for sexual stimulation. Skin diseases, such as rosacea or fibromyalgia, are another field of medicine where peptides’ potential could be used. Rosacea is a skin condition characterized by redness, dilated veins, swollen papules, and itching of the cheeks and nose. Symptoms can also be associated with excessive nasal discharge and minor vision problems. Scientists have discovered that melatonin levels are linked to genes that are responsible for the development of this disease. As Melanotan II leads to high production of that hormone, symptoms in patients in scientific studies have subsided over time. It is assumed that the mechanism of action is reflected in the modulation of inflammatory and vascular signaling pathways.

List of Peptide Uses

Sunless Tanning Effect

As an agonist of α-melanocyte-stimulating hormone, Melanotan II acts as a non-selective agonist of melanocortin receptors (including MC1, MC3, MC4, and MC5). By activating the first class of these receptors, the peptide stimulates melanogenesis and leads to increased production of the pigment melatonin, which is responsible for skin darkening.

The body has its mechanisms that regulate how much hormone is sufficient at what time of year and when it needs to stop secreting. This is done by using the Negative Feedback mechanism, where signals to stop further secretion are sent when enough hormone has already been produced. However, the peptide works by inhibiting these signals and thus disrupting the homeostasis of this hormone, which leads to excessive pigment production. The end effect is seen as a tan that is achieved quickly and effectively without sunbathing. This indication is most often limited to the female population, and often abuse can occur when higher doses are consumed for aesthetic reasons. In such situations, darkening of moles, the appearance of spots, and even an increased risk of developing skin melanoma are mentioned in certain studies. For this indication, subcutaneous administration or application as a nasal spray is most often used. However, none of the mentioned methods have been sufficiently studied.

Potential Effects in Treating Erectile Dysfunction

Erectile dysfunction is a condition characterized by difficulty achieving or maintaining an erection. There are various reasons why men develop it. Some of them are psychological, such as depression or anxiety, but there are also cases when there is a physical health problem that results in impotence. Some are heart problems, high blood pressure, high cholesterol, obesity, multiple sclerosis, Parkinson's disease, along with many others. Scientific studies have dealt with subjects with this condition, and the results suggest that Melanotan II acts on the part of the brain responsible for sexual desire, stimulating it. As such, a normal reaction to sensations in the form of an erection occurs. The tests showed spontaneous erections that lasted for a sufficient time and resulted in ejaculation. Such results show that the peptide could have potential for treating erectile dysfunction caused by various causes.

Association Between Melanotan II and Rosacea

Rosacea is a relatively common skin condition characterized by redness, swollen papules (mainly in the cheeks and nose), dilated veins, and sometimes even itching. Scientists have long established that there are certain genes that, if present, have a much greater chance of developing the disease. Then, a potential connection was observed between the level of the hormone melatonin and the expression of these genes.

Since Melanotan II stimulates the release of this hormone in the aforementioned ways, it is assumed that this peptide may have something to do with the withdrawal of rosacea symptoms. The mechanism of action could be based primarily on the modulation of inflammatory and vascular signaling pathways. There are numerous studies where these statements have been confirmed in subjects whose skin lesions have regressed and the condition has improved, after the application of Melanotan II. Suppression of the migration of certain cells and a decrease in the secretion of pro-inflammatory cytokines led to a reduced production of keratinocytes and an extremely favorable effect on this skin disease.

Dosage Calculator

The adequate dose and method of administration of this peptide have been studied for years. After certain research, scientists have determined a dose of 0.025mg/kg as optimal. In the case of treating various forms of psychogenic and physical erectile dysfunction, Melanotan II may be part of the therapy if used in the form of subcutaneous injection in the dose above, once a day for the first 12 weeks. Later, under the supervision of a doctor, the dose may be reduced, and the method of administration remains the same, until 24 weeks, when therapy should be discontinued. This peptide is still being studied, and work is being done to eliminate the possibility of serious side effects such as the development of melanoma, pigment spots, skin redness, and others. It is advised to use it exclusively under the supervision of a doctor, according to indications and in an adequate dose.

Dosage Calculator

The adequate dose and method of administration of this peptide have been studied for years. After certain research, scientists have determined a dose of 0.025mg/kg as optimal. In the case of treating various forms of psychogenic and physical erectile dysfunction, Melanotan II may be part of the therapy if used in the form of subcutaneous injection in the dose above, once a day for the first 12 weeks. Later, under the supervision of a doctor, the dose may be reduced, and the method of administration remains the same, until 24 weeks, when therapy should be discontinued. This peptide is still being studied, and work is being done to eliminate the possibility of serious side effects such as the development of melanoma, pigment spots, skin redness, and others. It is advised to use it exclusively under the supervision of a doctor, according to indications and in an adequate dose.

Conclusion

Melanotan II is a synthetic peptide with many potential positive effects. Some of those described are its possible role in the treatment of various forms of erectile dysfunction and various skin conditions such as rosacea or fibromyalgia, if used in an optimal dose of 0.025mg/kg body weight. In addition, women in particular use it to quickly get a tan without sun. Although research has shown it to be potentially useful so far, further studies are needed to avoid extensive side effects.

References:

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2. Guo F, Bakal K, Minokoshi Y, Hollenberg AN. Leptin signaling targets the thyrotropin-releasing hormone gene promoter in vivo. Endocrinology. 2004 May;145(5):2221-7. doi: 10.1210/en.2003-1312. Epub 2004 Feb 5. PMID: 14764630.
3. Toda C, Shiuchi T, Lee S, Yamato-Esaki M, Fujino Y, Suzuki A, Okamoto S, Minokoshi Y. Distinct effects of leptin and a melanocortin receptor agonist injected into medial hypothalamic nuclei on glucose uptake in peripheral tissues. Diabetes. 2009 Dec;58(12):2757-65. doi: 10.2337/db09-0638. Epub 2009 Sep 14. PMID: 19752162; PMCID: PMC2780865.
4. Lau JKY, Tian M, Shen Y, Lau SF, Fu WY, Fu AKY, Ip NY. Melanocortin receptor activation alleviates amyloid pathology and glial reactivity in an Alzheimer's disease transgenic mouse model. Sci Rep. 2021 Feb 23;11(1):4359. doi: 10.1038/s41598-021-83932-4. PMID: 33623128; PMCID: PMC7902646.
5. King, Stephen H et al. “Melanocortin receptors, melanotropic peptides and penile erection.” Current topics in medicinal chemistry vol. 7,11 (2007): 1098-1106. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2694735/
6. Peters, Björn, et al. “Melanotan II: a possible cause of renal infarction: review of the literature and case report.” CEN case reports vol. 9,2 (2020): 159-161. doi:10.1007/s13730-020-00447-z. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7148395/
7. Wessells, H et al. “Melanocortin receptor agonists, penile erection, and sexual motivation: human studies with Melanotan II.” International journal of impotence research vol. 12 Suppl 4 (2000): S74-9. doi:10.1038/sj.ijir.3900582. https://pubmed.ncbi.nlm.nih.gov/11035391/