Melanotan 1 (10mg)

What is the Melanotan 1 peptide?

Melanotan 1 (MT-1) is a synthetic equivalent of alpha-melanocyte-stimulating hormone (alpha-MSH). The peptide has been exhaustively researched in clinical studies for patients suffering from erythropoietic protoporphyria to prevent phototoxicity or sun-related skin damage.^[1] It was initially formulated to act as a sunless tanning agent. It was also observed to have the potential to influence diverse physiological processes like feeding patterns, central nervous system operations, blood pressure, etc. The molecule’s clinical trials are currently in phase II stage for keratosis (a particular kind of skin damage induced by the sun). The more severe squamous cell carcinoma is in phase III stage to treat polymorphous light eruption.

Specifications

AKA: MT-1

Molecular Formula: C78H111N21O19

Molecular Weight: 1646.8 g/mol

Sequence: Ac-Ser-Tyr-Ser-Nle-Glu-His-D-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH2

PubChem: CID 16154396

CAS Number: 75921-69-6

Reconstitution: Required

How Does MT-1 Work?

Melanotan 1 is structurally and functionally similar to the physiological alpha-melanocyte-stimulating hormone (alpha-MSH). Alpha-MSH is primarily known to affect melanocytes, skin cells, and hair cells responsible for pigmentation. This hormone interacts strongly with melanocortin receptor 1, thus mediating its role. Alpha-MSH is a non-selective agonist of melanocortin receptors 1, 3, 4, and 5 and completely stimulates them. MT-1 varies from alpha-MSH by a single amino acid and was initially developed as a sunless tanning agent. It was soon studied for its role in inducing sexual arousal, appetite boosting, and baseline metabolism modifications, in addition to affecting skin pigmentation. Subsequent research on the peptide and other melanocortin-binding proteins helped scientists to explore the melanocortin signaling system better.

Research

Melanotan 1 and Sunless Tanning
MT-1 has been studied in phase I clinical trials for its tanning effect in humans exposed to ultraviolet radiation.^[2] The work observed that volunteers who were administered MT-1 showed 75% more tanning and about 47% less sunburn. Melanotan 1 appeared to induce similar tanning in subjects compared to controls even with 50% less ultraviolet light exposure. The tan persisted on these subjects for three weeks longer than those exposed only to UV light. Therefore, MT-1 may be researched for applicability in tanning skin under conditions of high UV exposure, thereby potentially protecting from skin damage as well as melanomas. This would thus be a possible therapy for individuals who possess skin types with poor tanning (referred to as type I and type II as per the Fitzpatrick scale). Variant MC1 receptors in individuals cause less skin tanning than an individual with wild-type MC1 receptors. In this genetic backdrop, the use of MT-1 may increase melanin density, induce substantial tanning, and mediate photoprotection. Sunscreen is of limited use for such individuals. Hence they require to reduce their sun exposure to a significant extent to prevent skin cancer. MT-1 is under scientific investigation a potential alternative for UV protection and decreasing the frequency of skin cancer. MT-1 is also studied to treat vitiligo. A small phase I trial noted that combinatorial use of the peptide with UVB light therapy appeared to promote both syntheses of melanin and proliferation of melanocytes. About 50 % of the MT-1 treated vitiligo patients showed rapid re-pigmentation and a decrease of vitiligo patches on the skin. MT-1 may have the ability to help hypopigmented scars based on the outcome of vitiligo trial study. Overexposure to UV light causes scaly and crusty skin growth known as actinic or solar keratosis. This precancerous lesion, if left unattended, can develop into squamous cell carcinoma. There are greater than 400,000 such cases every year. Unlike obvious lesions, which can be surgically corrected, the small and rather invisible ones may in the future be treated with MT-1 to possibly prevent the formation of skin cancer.

Melanotan 1 and Cognitive Decline, Alzheimer’s Disease
MT-1 administration appeared to protect transgenic mice brains from cognitive decline and the onset of Alzheimer’s disease (AD).^[3] he researchers note that the melanocortin receptor activation by MT-1 “restores the impaired homeostatic processes and microglial reactivity in the hippocampus in APP/PS1 mice.” Even minute amounts of the peptide were observed in an experimental study to decrease amyloid-beta plaques and neuronal apoptosis in the brains of mice suffering from moderate AD. This may enhance clinically defined cognitive function and synaptic transmission in the MT-1 treated animals. In the same study, inhibiting the effects of MT-1 at the MC4 receptor appeared to prevent all of the peptide’s favorable effects. MC4 receptor stimulation leads to neurogenesis and cognitive function recovery in murine AD models. All AD-linked biomarkers appeared to decrease significantly even with a once-daily dose of the peptide. The MC4 receptor is the sole melanocortin receptor to be expressed on astrocytes, the feeder cells that help to protect and provide nutrition to neurons. MT-1 is under study for its potential to enhance the production of brain-derived neurotrophic factor (BDNF) and thus stimulates astrocyte functioning. BDNF is also crucial to maintaining the stability of synapses and general neurogenesis.

Melanotan 1 and Blood Pressure
MT-1 appears to selectively help control hypertension in murine models without affecting animals with normal blood pressure.^[4] This role of MT-1 possibly may hold value as existing medication often leads to hypotension, heart attack, stroke, and other serious manifestations. The blood pressure medicines cause more harm in elderly patients due to their age-related frail physiology. MT-1’s possible ability to control hypertension without triggering critically low blood pressure could make it a suitable candidate for new medicine development.

Melanotan 1 and Stroke Recovery
MT-1 appears in research to alleviate adverse conditions of stroke as well. Studies on the gerbil model have shown that when the peptide is used even 9 hours after a stroke, it may help in controlling brain damage, neuronal death, and improve learning and memory.^[5] MT-1 appears to assist the brain to reroute learning and memory to the healthier parts. Thus it has the potential to help repair synaptic plasticity and long-term functional recovery of the brain. The most important mediator in this process is the expression of the Zif268 gene. Zif268 is reported to be over-expressed in animals administered with Melanotan-1. It is appears to be overexpressed in models of AD which exhibits improvement in cognitive abilities.

Melanotan 1 and Neuroinflammatory Disease
MC1 receptor was recently observed to induce inflammation in the central nervous system in mice. T helper cells attack the myelin sheath in neurons leading to neuronal dysfunction and even death in multiple sclerosis. The damage was apparently reversed in research studies through the use of MT-1. In fact, the administration of MT-1 to these mice appeared to augment myelin recovery and promoted neuron signaling.^[6] Uveitis is another inflammatory disorder of the eye which causes pain and leads to vision loss. Melanotan 1 has the potential to serve as an alternative to the existing steroids and other immunosuppressive medicines used to treat the condition. The peptide has been reported to mimic alpha-MSH’s role, which suppresses T-cell function through MC4 receptors. Local administration of the MC4 agonists directly to the eye has also appeared effective and helps avoid the adverse effects of systemic application.^[7]

Melanotan 1 and Heart, Circulation functions
Studies in rats have suggested the efficacy of using MT-1 and other melanocortins in reducing cardiac injury and improving circulatory parameters. The use of MT-1 during CPR and in combination with epinephrine appeared to reinstate baseline arterial pressure and cardiac rate, reversing metabolic acidosis, suppressing inflammatory markers, and promoting the expression of genes associated with cardiac function. Overall, the therapy appeared to help increase the survival rate by 81%, suggesting the efficacy of using Melanotan-1 or a similar melanocortin in a cardiac emergency.

Melanotan 1, Investigated in Fat Loss Trials
MT-1 appears to work directly on the MC5 receptor, like several melanocortin receptors. This interaction appears to stimulate MC5R into lipid metabolism by muscle cells and shifts the dynamics from fat storage to fat burning. These studies in murine models put forth the theory that lipid metabolism is a complex physiological process and involves various pathways.^[8] Research in mice reveal that “treatment leads to weight loss that affects both the visceral and subcutaneous fat compartments.” MT-1 may act as a experimental molecule to study fatty acid metabolism and the means to alter the baseline physiology without the need for exercise.

References