Melanotan-1 Nasal Spray
Melanotan-1 nasal spray is a melanotocyte stimulating hormone analogue. It is used clinically in Europe to prevent sun-induced skin damage (phototoxicity) in erythropoietic protoporphyria patients. In addition, it has been discovered that Melanotan 1 has physiologic effects on the central nervous system, blood pressure, and feeding behaviour. Actinic keratosis (a type of sun-induced skin damage) and squamous cell carcinoma are being studied in phase 3 clinical trials.
What is Melanotan-1 nasal spray?
Melanotan 1 is a synthetic version of the natural alpha MSH, best known for its effect on melanocytes, the pigment-producing cells in the skin and hair. Strong binding to Melanocortin Receptor 1 mediates this function. MSH is a non-selective full agonist of MCR1, 3, 4, and 5.
MT 1 is a sunless tanning agent that differs from alpha-MSH by a single amino acid. Scientists quickly discovered that while Melanotan 1 caused pigmentation, it increased sexual arousal, appetite and altered baseline metabolism. Other melanocortin-binding proteins have also been studied, including Melanotan 1.
Molecular Formula: M78H111N21O19
Molecular Weight: 1646.874 g/mol
Sequence: Ser Tyr-Ser Nle-Glu His D Phe-Arg Trp-Gly Lys-Pro Val
Size: 15ml | 30ml
Melanotan-1 nasal spray sunless tanning formula clinical trials in humans exposed to UV radiation have looked at MT-1’s effect on tanning in phase 1. MT-1 users tanned 75% faster and sunburned 47% less. It took half as much UV light to achieve the same tanning effect as Melanotan-1 nasal spray on controls. They also lasted three weeks longer than those only exposed to UV light. Melanotan 1 may enhance tanning in high UV environments while protecting against sunburn and long-term UV skin damage, say scientists. Patients with fair skin may benefit from this (type I and type II by the Fitzpatrick scale) .
These people are less likely to tan than the average person. However, because Melanotan 1 improves tanning and melanin density, it can help safeguard people who don’t tan and need the most photoprotection . These people should use sunscreen sparingly and avoid direct sunlight to prevent skin cancer. With better UV protection, skin cancer rates could be significantly reduced.
Melanotan 1 may also be used to treat vitiligo. A small phase 1 trial found that using Melanotan 1 with UVB light therapy-induced both melanin production and melanocyte proliferation. Almost fifty per cent of treated patients had improved vitiligo pigmentation and faster repigmentation .
Combining Melanotan-1 with other vitiligo treatments has been shown to produce synergistic effects and more immediate aesthetic results . If Melanotan 1 effectively treats vitiligo, it may be used to treat hypopigmented scars, etc.
Actinic keratosis is a scabby/scaly skin growth caused by excessive UV exposure. If left untreated, it will progress to a type of skin cancer (squamous cell carcinoma). Every year, over 400,000 cases occur. A dermatologist or surgeon can remove visible lesions, but most are too small to see or feel. Melanotan-1 nasal spray is being studied as a possible first-line treatment for these undetectable lesions and for skin cancer prevention.
Melanotan-1 nasal spray targets the MC5 receptor. MC5R stimulation promotes muscle fatty acid oxidation and shifts fat cells from storage to burning . These findings in mice show that melanocortin stimulation causes fat burning via multiple receptors and physiologic pathways . For those who cannot exercise due to obesity, disability, or injury, the ability to boost baseline physiology without exercise is tantalizing.
Melanotan-1 nasal spray has been shown to protect against hypertension in hypertensive mice without affecting normal blood pressure. Existing medications for blood pressure can generate hypotension, which can cause loss of consciousness, heart attack, stroke, and other complications . Due to their labile physiology, the elderly are more prone to this side effect. Melanotan 1’s ability to control high blood pressure without causing significant lows makes it an ideal candidate for further drug development.
Melanotan-1 nasal spray and other melanocortins have reduced injury and improved circulatory parameters in heart attack rats. MT-1 administered during CPR, along with epinephrine, helps restore baseline arterial pressure and heart rate, reverse metabolic acidosis, reduce inflammatory markers, and improve cardiac gene expression. In addition, it increased survival by 80%, making it a likely candidate for emergency advanced cardiac life support .
According to research, the MC1 receptor produces pigmentation for skin and hair. Many believed that the receptor’s sole function was to bind. However, recent studies in mice suggest this receptor is involved in CNS inflammation. The loss of myelin on neurons causes neuron dysfunction and even death in multiple sclerosis. In mice studies, chemoprevention of neuronal damage by Melanotan-1 nasal spray helped restore myelin and restore neuron signalling .
Acute uveitis in mice causes pain and loss of vision. Scientists are constantly looking for new research in search of safer alternatives to steroids and immunosuppressive drugs. By mimicking the MC4 receptor, MT-1 inhibits T-cell function. Local MC4 receptor agonists are as effective as systemic MC4 receptor agonists when administered directly to the eyes. Bypassing systemic side effects, this route of administration .
Not only AD biomarkers benefit from MT-1 treatment. Treatment with nanomolar doses of Melanotan 2 reduces damage to the brain, including neuron death, and improves learning and memory recovery in gerbil stroke models. This effect is achieved even nine hours after a stroke .
MT-1 is thought to stimulate neuroplasticity and promote long-term functional recovery by rerouting memory and learning to healthier brain areas. The Zif268 gene appears to be the key here. Zif268 is overexpressed in Melanotan-1 nasal spray treated animals. The same gene is overexpressed in Alzheimer’s disease models that improve cognitive function.
Dementia and cognitive decline
Melanotan-1 nasal spray protects the brain from the damage that leads to cognitive impairment and Alzheimer’s disease in transgenic mice research. Even at low doses, Melanotan 1 reduces the amount of amyloid-beta plaques in the brain, safeguards neurons from death, improves clinical and laboratory measures of synaptic transmission, and enhances clinical actions of cognitive function. Also, blocking Melanotan 1 at the MC4 receptor reversed the peptide’s beneficial effects .
Other studies have looked into the advantage of Melanotan-1 nasal spray action on the MC4. MC4 receptor activation can enhance neurogenesis and improve cognition in AD mice. Some studies show a slowing of decline, but this one shows an improvement . Furthermore, all AD-related biomarkers are reduced by MT-1 once daily, indicating that it works through various pathophysiological pathways .
Astrocytes, which protect and nourish neurons, only express the MC4 receptor. Melanotan 1 appears to improve astrocyte function in rats by increasing BDNF levels. BDNF protects synapse stability and neurogenesis .
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