Melanotan 1 Research Peptide

Melanotan 1 Research Peptide

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What is Melanotan 1?

What is melanotan 1?

The melanocortin system has an established regulatory role in homeostasis and there is sufficient information on melanotan 1’s involvement in nociception, memory and mood disorders. Melanocortin 4 receptor plays an integral role in changes in synaptic plasticity in diverse physiological systems. Melanocortin induced changes in synaptic vesicles are crucial because they control pain receptors, memory impairments and related conditions. Afamelanotide or melanotan 1 is a synthetic analog of alpha-melanocyte stimulating hormone and was first synthesized by the University of Arizona and later by Clinuvel Company. Melanotan 1 is essential in accentuating the production of melanogenesis or skin pigmentation. Currently, melanotan 1 is under review for the treatment of skin cancer or melanoma. Ultraviolet radiation is a major cause of melanoma in mice with low pigmentation and it resulted in erythropoietic protoporphyria (EPP). Melanotan 1 is essential in repigmentation or reintroduction of brown or black pigment in test subjects with vitiligo.


Melanotan 1 Mechanism of Action

Currently, there is research underway to determine the photo-protective effects of melanin and the use of melanotan 1 to induce its production. Test subjects with low EPP have showed an increase in pigmentation when the melanotan 1 peptide is administered. Findings showed that melanotan 1 is vital in the conversion of eumelanin to melanin in the epidermal layer of the skin. Hypothalamic neurocircuitry is essential in regulating energy homeostasis in adult rats. It is imperative to note that this neurocircuitry is not developed until the third week. In essence, fibers from the hypothalamic arcuate nucleus which include alpha-melanocyte stimulating hormone fibers and neuropeptides peptide Y do not indicate innervate downstream effect until the research mice are two weeks old. However, it is essential to note that the alpha-melanocyte stimulating hormone from melanocortin receptors and brainstems are present in the hypothalamus at birth. Research studies showed that administration of the melanotan 1 peptide caused a significant change in body weight, hypothalamic neuropeptide Y expression and energy expenditure. Expression of melanocortin receptors varies from one species to the another and using melanotan 1 peptide is an area of interest in modern science.

According to research done on mice, melanotan 1 was administered and then stomach weight and brown adipose uncoupling protein messenger ribonucleic acid were monitored. Moreover, central c-Fos was assessed after every two hours. Studies revealed that neuropeptide Y messenger RNA showed a reduction in body and stomach weight while uncoupling protein messenger ribonucleic acid increased. It is imperative to note that this indicated an increase in energy expenditure and a  decrease in food intake. However, it is imperative to note that melanotan 1 has no effect on the acid levels of the neuropeptide Y messenger ribonucleic in the hypothalamic region.

These studies showed that melanotan 1 can help to stimulate energy expenditure and inhibit food intake. This concept is under research because it will help reduce weight in obese test subjects. Moreover, hypothalamic neurocircuitry is enhanced and they do not affect changes in NPY expression. Research indicated that in adult rodents, the arcuate nucleus of the hypothalamic region plays a significant role in weight reduction. This happens by the induction of various signals in the peripheral and accentuating metabolic processes in a system. Peripheral signals responsible for metabolism such as leptin play a vital role in protein synthesis.


Melanotan 1 Research

Melanotan 1 Research

Melanotan 1 research

The effects of weight gain are mediated by two types of neurons: anorexigenic alpha-melanocyte stimulating hormone neurons and orexigenic neuropeptides Y or agouti-related protein neurons. These neurons play a crucial role in food intake and energy expenditure. The neurons include the paraventricular nucleus of the hypothalamus, perifornical region, dorsomedial nucleus and paraventricular nucleus of the hypothalamus and lateral hypothalamic area. The neurons in the brain’s hypothalamic region work by modifying various aspects of a biological system. Arcuate nucleus hypothalamic neurocircuitry is essential for regulating energy homeostasis. However, this part of the body is not fully yet developed in young mice. Arcuate nucleus hypothalamic neurons do not innervate downstream target until postnatal week two. Studies showed that ingestion is stimulated by dehydration of the test subject and the primary inhibitory signal is gastric distention. After nine weeks of research, mice began to show a reduction in caloric intake and stomach weight.

Insulin levels reduced significantly with the introduction of melanotan 1 2-deoxygensase and there’s a decrease in insulin and food intake. Exogenous leptin does not cause any effect on food intake in the first three weeks. This indicated that the functional maturity of downstream of melanocortin receptors. Peripheral metabolic and caloric signals have minimal effect on food intake on developing rats. During the early postnatal period, the mice are growing fast and there is a high energy demand, suggesting an enhanced anorexigenic signals. Although orexigenic neurocircuitry projections have not been established, they are expressed in a number of cells in the hypothalamic region. During development, the administration of melanotan 1 is seen to activate the arcuate nucleus and this is an aspect in modern science that researchers are investigating. Transient neuropeptides Y expression increases two weeks after melanotan 1 administration and there is a likelihood of accentuating and expression of P30 neurons.

There is a sufficient evidence to show that melanocortin receptors and signaling molecules are increased when melanotan 1 is administered to the test subject. In addition, melanotan 1 is a non-selective agonist which increases alpha-melanocyte stimulating hormones released on somatotrophs. Melanocortin 4 receptor and other melanocortin receptors such as melanocortin receptor 1, melanocortin receptor 2, melanocortin receptor 3 and agonism of melanotan are vital in signal transduction. There is downstream innervation of arcuate melanocortinergic fibers and it is considered as an effective component in neuropeptide Y expression. Orexigenic dominates most of the conditions while anorexigenic are not present at the moment. Although anorexic features of melanotan 1 have not been fully established, there are studies underway to ascertain the mode of action of the melanotan 1 peptide.


Use of Melanotan 1 in Erythropoietic Porphyria (EPP)

The latest research findings in 2015 showed that melanotan 1 is effective in alleviating EPP. According to research, over 70% of research mice showed full recovery from EPP. Melanotan 1 is known to be a selective agonist that binds to specific melanocortin receptors on the hypothalamus region of the brain. The mice that were injected with melanotan 1 showed significant reduction in the effects of EPP.


Melanotan 1 and Tanning

Melanotan 1 polypeptide has shown to increase tanning effects

Melanotan 1 polypeptide has shown to increase tanning effects

According to a three-part series of trials on melanotan 1, the melanotan 1 peptide has a significant impact in ultraviolet B exposure. Tanning is a crucial process which protects the skin’s epidermal layers from unprecedented cellular multiplication. According to studies, administration of the melanotan 1 peptide enhanced conversion of eumelanin to melanin on the skin. Melanin is a photo-protective pigment that absorbs harmful ultraviolet rays that could cause skin cancer. During the first phase of research, melanotan 1 was administered and findings monitored 47% of test subjects showed an increased rate of melanogenesis. The second trial recorded 65% rate of melanogenesis and the skin on test mice changed significantly to prevent damage from ultraviolet B rays. It is imperative to understand that the melanotan 1 research has a control group that is treated similarly as the test subjects but without melanotan 1 injections. The melanotan 1 polypeptide has shown to increase tanning effects on epidermal layers of skin which results in extended tanning without exposure to the sun.


Melanotan 1 and Protein Translation

Apart from porphyria and tanning process, melanotan 1 has shown to have a host of other significant benefits in a biological system. Currently, studies are underway to ascertain how melanotan 1 works to accentuate protein translation. Protein translation is the main challenge in the pharmaceutical industry because any changes in protein conformation will affect its binding affinity. It is imperative to understand that a peptide must be presented in the right conformation and configuration to improve its efficacy and potency. Research showed that melanotan 1 has a therapeutic effect on test subjects.  According to studies conducted on mice, melanotan 1 is effective in increasing the translation of template messenger ribonucleic acid into amino acids. Amino acids then configure and join to form proteins. Challenges in modern science are degradation and enzymatic lysis in a biological system. It is imperative that in the modern production of polypeptides change, the structure of the peptide and its conformation is essential in increasing its half-life. Molecular characteristics play a crucial role in enhancing efficacy and potency of the melanotan 1 macromolecule.

Melanotan 1 and Protein Translation

Melanotan 1 and protein translation

Mode of Delivery

There are many options of administering the melanotan 1 peptide. The primary means are intravenously, subcutaneously and intramuscularly. It is important to note that when administering the melanotan 1 peptide, you should change the areas where you have administered to avoid site inflammation. Moreover, the route of administration determines how efficient the peptide will be in a biological system. Research showed that melanotan 1 administration varies from species to species. However, you can start with 0.5 mg as you increase to 2 mg depending on the objectives of the study. You should monitor cytotoxicity, phototoxicity and other side effects that could occur when melanotan 1 is administered. Antibodies in a biological system have shown to affect the mode of action of melanotan 1.

Depending on the weight of test organism, you should adjust dosage to suit your objectives. It is vital to note that there is a certain concentration that even when melanotan 1 dosage is increased, the alpha-melanocyte stimulating hormone produced does not increase. Notably, development of antibodies in the test organism is known to reduce efficacy and potency of the research peptide. The half-life of melanotan 1 is usually eight hours to two days depending on internal factors in the organism. The endogenous alpha-melanocyte stimulating hormone plays an essential role in enhancing translational research and conversion of amino acids into proteins.


Melanotan 1 and Cardiac Research

Melanotan 1 and Cardiac Research

Melanotan 1 and cardiac research

In preliminary research studies, the effects of melanotan 1 have showed to have net positive effects in myocytes protection. Cardioprotective effect of melanotan 1 is under research. According to findings done on mice, it showed that the administration of the peptide enhanced production of myocytes. Mice with reperfusion injuries were used during the research and administration of the melanotan 1 peptide was done during transplantation to help prevent ischemic reperfusion.  Studies showed that phenotypic changes in the myocytes which were similar to those in an ischemic heart attack. Ischemic pre-conditioning is an essential method of protecting the heart against reperfusion injury leading to MI or myocardial infarction. Melanocortin 1 receptor-mediated effects coupled with potassium chloride were used to induce cardiac arrest.  Results showed that melanocortin improves return of spontaneous circulation of acidosis and this is vital in inhibiting oxidative stress. Moreover, an inflammatory cascade is altered and this is crucial in the accentuation of myocardial functionality. Translation mystique of melanotan 1 increased survival rate in rats. According to the study, 85% of mice were co-administered with cardiac preventive molecules.


Anti-Proliferative Effects of Melanotan 1

According to findings of a research done on mice, the melanotan 1 polypeptide has anti-inflammatory effects. Moreover, melanotan 1 has anti-oxidant properties which accentuate myoblastic activity. Antioxidant activities of melanotan 1 are mediated by transcription factor Nrf2. At various stages of the research, the melanotan 1 polypeptide has preventive measures on heart muscles. Preliminary results showed that melanotan 1 follows markers in the epidermal layer of the skin. Human melanoma cells are similar to those in mice. Researchers found that administration of the melanotan1 peptide on  test subjects increased tyrosinase activity in a biological system. Moreover, findings from this research showed that melanotan 1 reduced exposure of cells to degrading effects of tumorous cells.

Melanotan 1 has anti-proliferative effects on different cell lines with no effect on cell functionality and efficacy. There are promising potential benefits of melanotan 1 use in different areas of research such as cancer, cardiac functionality and protein formation. Melanotan 1 is supplied in freeze-dried or lyophilized vials and you should reconstitute it using bacteriostatic water or saline water. This is a vital part of any research as it reduces chances of contamination and bacterial transfer from the vial to test subjects.  Once you have reconstituted the vial, store it in a dark, cool dry place. It is imperative to note that all peptides supplied are for research purposes only and human consumption is not allowed.


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