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1kits（10Vials）
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▎Melanotan-2 Structure
Source: PubChem |
Sequence: Ac-Nle-cyclo(Asp-His-D-Phe-Arg-Trp-Lys)-NH₂ Molecular Formula: C50H69N15O9 Molecular Weight: 1024.2 g/mol CAS Number: 121062-08-6 PubChem CID: 92432 Synonyms: MT-II |
▎Melanotan-2 Research
What is the research background of Melanota ?
Melanota is a synthetic analogue. It is a synthetic analogue of α-melanocyte-stimulating hormone (α-MSH), which is prepared by chemical synthesis methods[1] . α-MSH is a naturally occurring hormone that has various physiological functions in the human body, including regulating skin pigmentation. Melanota was designed to mimic some of the effects of α-MSH but has stronger activity and specific application purposes. Melanota was initially developed as a substance to promote skin pigmentation, that is, a so-called tanning agent. With the increase in people's demand for tanning, some people began to seek to obtain a rapid skin darkening effect by injecting Melanota . The research in this regard mainly focuses on its mechanism and effect on skin pigmentation. For example, studies have found that Melanota can bind to specific receptors on melanocytes to stimulate the production of melanin, thereby darkening the skin [2, 3].
What is Melanota ?
Melanota is a synthetic analogue that is related to α-melanocyte-stimulating hormone (α-MSH). Its main function is to increase skin pigmentation and darken human skin. Melanota mainly exerts its effect by interacting with melanocortin receptors. Specifically, as a non-selective melanocortin receptor agonist, it can stimulate the production of melanin in the skin, thus achieving skin pigmentation, that is, the tanning effect. In addition, it can also produce spontaneous penile erection and sexual stimulation effects.
What is the specific mechanism of Melanota in tanning?
Melanota induces skin tanning by interacting with the melanocortin 1 receptor on melanocytes. It is believed that Melanota mimics the effect of the melanocortin α-melanocyte-stimulating hormone (α-MSH) on the MC1 receptor of melanocytes, resulting in an increase in the expression of agouti signaling protein. Melanota stimulates melanocytes to produce and secrete melanin, thereby increasing skin pigmentation[4]. It can promote the production of eumelanin in the skin to achieve skin pigmentation. Studies have shown that the α-melanocyte-stimulating hormone (α-MSH) analogue cyclic -[Ac-Nle(4), Asp(5), D-Phe(7), Lys(10)] alpha-MSH-(4 - 10) amide (Melanota ), a potent melanocortin receptor agonist, can stimulate the production of eumelanin to achieve skin pigmentation[5] .
What is the specific mechanism of Melanota in inducing penile erection and enhancing sexual stimulation?
Induction of erection:
In anesthetized rats, Melanota —a non-specific melanocortin receptor agonist—exhibited dose-dependent erectile induction when administered via intravenous injection (0.1–1 mg/kg) or hypothalamic paraventricular nucleus infusion (0.1–1 μg). This effect triggered penile erections and reduced the latency of first erectile events [6].Its effect may involve activating melanocortin receptors in the central nervous system, thereby regulating the neural pathways related to erection. When Melanota is intrathecally injected (0.2 μg) at the L6 - S1 level, the amplitude of erection events is higher. This indicates that the neural pathways at the spinal cord level may also be involved in the induction of erection by Melanota [6].
Promotion of erection:
After intravenous injection of Melanota (1 mg/kg), the erectile response induced by cavernous nerve stimulation is increased, thus playing a promoting role in erection[6] . After acute removal of the lumbar paravertebral sympathetic chain, the promoting effect of Melanota is abolished. This indicates that the promoting effect of Melanota on erection depends on the integrity of the lumbar paravertebral sympathetic chain. In contrast, Melanota injected into the corpus cavernosum (1 μg) did not show any promoter activity. Spinal cord transection or bilateral transection of the pelvic nerve or the dorsal nerve of the penis did not impair the promoting activity of intravenous Melanota (1 mg/kg), further indicating that the promoting effect of Melanota on erection is mainly through the sympathetic nerve pathway rather than the pelvic nerve or the dorsal nerve of the penis [6].
Enhancement of female sexual arousal behavior:
Studies have found that Melanota also has an impact on female sexual behavior. In female rats, ovariectomized rats pretreated with estradiol benzoate (EB) and progesterone (P), intravenous injection of Melanota (1 and 3 mg/kg) increased the number of jumps, rushes, and ear wiggles, indicating that progesterone can interact with Melanota to increase female sexual arousal behavior [7].
Effect of MTII on tumorigenicity of melanoma cells.
Source:PubMed[1]
Melanota is a substance with multiple functions and research directions. The following will introduce other related research on Melanota .
Induction of erection:
In some studies, it was found that Melanota also has an impact on the reproductive system. For example, Melanota can cause abnormal penile erection. Some patients experienced painful erections after subcutaneous injection of Melanota , and also showed symptoms of sympathetic nerve excitation, such as increased heart rate, elevated blood pressure, restlessness, and excessive sweating[8] .This indicates that Melanota may affect the blood supply and neural regulation of the reproductive organs by acting on specific neurotransmitters and receptor systems, thus leading to changes in erectile function. In addition, in studies on rodents, melanocortin substances can cause a lordosis posture, which is interpreted as evidence of increased sexual arousal[8], further suggesting that the impact of Melanota on the reproductive system may be related to sexual arousal and the regulation of sexual behavior.
Promotion of melanin production:
As a synthetic melanocortin analogue, Melanota can bind to the melanocortin I receptor (MC1R) to promote melanin production [9].It mainly achieves this by promoting the proliferation of melanocytes and regulating the activity of tyrosinase. This effect of promoting melanin production gives Melanota potential application value in the field of skin, for example, it may play a role in the treatment and prevention of some skin diseases.
Research in anti-tumor aspects:
In the research on anti-tumor, studies using the B16-F10 melanoma model found that although Melanota has no effect on the proliferation of melanoma cells, it can effectively inhibit the migration, invasion, and colony formation ability of melanoma cells. Local application of Melanota can also significantly attenuate the tumor progression in mice with established melanoma. Its mechanism of action is to cause an upregulation of phosphatase and tensin homolog (PTEN) through the melanocortin 1 receptor (MC1R), thereby inhibiting the progression of melanoma by downregulating the cyclooxygenase II (COX-2)/prostaglandin E2 (PGE2) signaling pathway [1].
Therapeutic effect on autism:
Some studies used a maternal immune activation (MIA) mouse model of autism to evaluate the therapeutic potential of the melanocortin receptor 4 agonist M Melanota for autism-like characteristics in adult male mice[10].Male MIA mice showed autism-like characteristics, including impaired social behavior indicators, reduced vocal communication, and increased repetitive behaviors. Administration of Melanota to male MIA mice for seven consecutive days led to an improvement in social behavior indicators. There was no significant change in social behavior indicators in male C57 mice with a normal background after treatment with Melanota . In addition, in normal C57 mice, there were no changes in anxiety-like or repetitive behaviors after treatment with Melanota , but there was a significant decrease in body weight after subacute treatment. These data indicate that Melanota is an effective drug that can improve the autism-like behavioral deficits in the autism model of adult male MIA mice.
Reversal of memory impairment:
Studies have shown that a high-fat (HF) diet has been proven to increase the risk of nerve damage and neurodegenerative diseases. This study investigated the possible relationship between diet, Melanota targeting melanocortin receptors, and the behavior of zebrafish[11] . Surprisingly, even a short-term HF diet that lasted for about 1% of the zebrafish's life had a strong developmental impact. Compared with zebrafish fed a control diet, zebrafish fed an HF diet showed impaired recognition memory, increased anxiety levels, and reduced exploration tendency after only three weeks. And these abnormalities caused by the HF diet were reversed by Melanota . Animals fed an HF diet and treated with Melanota showed recognition memory, anxiety, and exploration behaviors similar to those of the control group. This study provides evidence that even a short-term HF diet can have an impact on memory and mood, and it is the first study to show that Melanota can reverse these changes.
Regulation of social behavior:
In the field of neuroscience research, it was found that Melanotan-II can regulate social behavior by stimulating melanocortin receptors and then activating the central oxytocin system [12]. Specifically, after systemic administration of Melanota , intravenous injection rather than intranasal administration of Melanota can significantly induce Fos expression in the magnocellular neurons of the supraoptic nucleus (SON) and paraventricular nucleus (PVN) of the hypothalamus, and this response can be attenuated by pretreatment with the melanocortin antagonist SHU-9119. Electrophysiological recordings showed that intravenous injection of Melanota can increase the firing rate of oxytocin neurons in the SON. This indicates that Melanota has a regulatory effect on the oxytocin system related to social behavior in the nervous system, and its mechanism of action may be to regulate the activity and secretion of oxytocin neurons by activating specific receptors and signaling pathways.
Research on obesity and metabolic health:
In terms of obesity and metabolic health, some studies used a genetic model of pituitary adenylate cyclase-activating polypeptide (PACAP)-deficient mice and found that the melanocortin receptor agonist Melanota can partially rescue the impaired thermogenic capacity of PACAP-deficient mice during cold adaptation. This indicates that PACAP may play a role upstream of the melanocortin system, regulating the sympathetic nerve activity of brown adipose tissue in mice, thereby having an impact on obesity and metabolic health [13].
Regulation of metabolism and body temperature:
Melanota also has a significant impact on the endocrine system. For example, intraperitoneal administration of Melanota to mice can cause profound and transient hypometabolism/hypothermia[14] .Studies have shown that in mice lacking mast cells, the hypothermia caused by Melanota is eliminated, suggesting that the participation of mast cells is required. Melanota causes hypothermia in mice by activating mast cells and stimulating the histamine 1 receptor, and its mechanism of action involves the interaction of multiple endocrine factors and receptors.
In conclusion, as a synthetic substance that has attracted much attention, Melanota exhibits unique characteristics in multiple fields. In the field of skin, by binding to specific receptors on melanocytes, it can effectively promote the production of melanin, providing a non-traditional tanning method for those who desire a healthy bronze complexion. Compared with tanning by prolonged exposure to ultraviolet rays, Melanota can avoid the direct damage of ultraviolet rays to the skin and reduce the potential risks of sunburn, skin aging, and even skin cancer.
From the perspective of sexual function regulation, Melanota has a positive effect on stimulating spontaneous penile erection and enhancing sexual stimulation. This is a potential effective solution for some individuals with sexual dysfunction or those who hope to improve their sexual experience. It can achieve a positive impact on sexual function by activating specific neural pathways in the central and peripheral nervous systems and regulating related neurotransmitters and receptors, providing new possibilities for improving sexual health.
In the research on obesity and metabolic health, Melanota also shows potential advantages. It may be able to regulate energy metabolism and body temperature and has a certain improvement effect on the impaired function of adipose tissue in obesity. It provides a new research direction for the treatment of obesity and the management of metabolic health, which is helpful for the development of new treatment strategies and the improvement of the health status of obese patients.
About The Author
The above-mentioned materials are all researched, edited and compiled by Cocer Peptides.
Scientific Journal Author
Cousen, P is a researcher with a primary focus in the field of Dermatology Allergy. His work within this domain has been associated with several organizations, including South Tees Hosp NHS Fdn Trust, James Cook University Hospital, Royal Cornwall Hospital, University of Sheffield, and Chesterfield Royal Hosp. Beyond his core specialization in Dermatology Allergy, Cousen, P's research interests and activities likely extend to related areas such as immunology, given the inherent connection between allergic reactions and the immune system. This might involve studying the immune responses that lead to allergic skin conditions and exploring new therapeutic approaches to modulate these responses.
Additionally, his research could encompass clinical trials for new dermatological treatments, the study of skin barrier function and its role in allergy prevention, and the investigation of genetic factors that predispose individuals to skin allergies. Furthermore, considering the multidisciplinary nature of healthcare research, he might collaborate with experts from other fields like pharmacology, microbiology (studying skin microbiome's impact on allergies), and even psychology (examining the psychological impact of chronic skin allergies), thereby contributing to a comprehensive understanding and management of dermatological allergic conditions. Cousen, P is listed in the reference of citation [4].
