Melanotan-2

Melanotan-2 is a synthetic analog of the naturally occurring peptide hormone melanocortin, which stimulates and intensifies skin tan through stimulation of melanin secretion.

Melanotan-2 was developed at the University of Arizona. Researchers claimed that administration of this synthetic peptide into the body could cause sunless tanning. Thus, with the help of this drug it is possible to get beautiful tanning and escape dangerous UV exposure, which can later lead to skin cancer (melanoma). On May 5, 2010 the Italian Medicines Agency (AIFA - Agenzia Italiana del Farmaco) became the first governmental health organization ever to authorize Melanotan-2 as a medicine for therapeutic use to reduce painful photosensitivity.

In addition to sunless tannin, Melantan-2 causes a fairly strong increase in Libido (sex drive) in both men and women.

The main effects of Melanotan-2 include tanning (without or with less frequent visiting of a tanning salon, without sunbathing), melanoma (skin cancer) prevention, increase in Libido (the drug is now being tested as a medicine for treatment of male impotency), and decrease of appetite.

dosage regimen:

2 mg every day until necessary tan color is obtained. The results appear gradually within 1-3 weeks. To accelerate pigmentation it is possible to visit a tanning salon (up to 3 times per week) or to sunbathe. When necessary tan color is obtained, the drug can be administered 1-2 times per week (to maintain an obtained result some people do not even need to have further injections; it is enough to visit a tanning salon or to sunbathe for them).

Melanotan II

Melanotan II belongs to a group of peptides called the melanotropin peptides. Other peptides belonging to this group are ACTH (adrenocortropic hormone) and the melanocyte-stimulating hormones (MSH).

Classification, Actions, Mechanisms:

The MSHs contribute to pigmentation and also play a role as a hypothalamic satiety signal [1]. Melanocortins also have been demonstrated to play a role in lipolysis of adipocytes, thermal control, sexual function, and cognition [1, 2]. Further, leptin exerts its action partly by activation of the melanocortin system in the brain [3]. Further, the MCR (melanocortin receptors), to which MTII binds, play a key role in eating behavior in humans [3]; Perboni et al write: MC4R activity affects meal size and meal choice but not meal frequency, with the type of diet affecting the efficacy of MC4R agonists to reduce food intake [3].

Dorr, et al, demonstrated in a pilot trial study using human subjects that significant change in pigmentation (specifically, darkening) occurred after just five applications of MTII (applied every other day via subcutaneous injection) as measured by visual perception as well as by quantitative reflection [5]. They also noted that penile erection consistently occurred concomitantly with "stretching and yawning" between one and five hours after application of MTII in males via subcutaneous injection [5]. Mild nausea was observed at most MTII dosage levels, although no treatment was required and all subjects opted to continue the trials for the duration of the two-week study [5].

Wessells et al concluded that "Melanotan-II is a potent initiator of erections in men with psychogenic erections in men with psychogenic erectile dysfunctions and has manageable side effects at a dose of 0.025mg/kg" based on the findings of their study that: In 8 of 10 men treated with Melanotan-II clinically apparent erections developed. Mean duration of tip rigidity greater than 80% was 38.0 minutes with Melanotan-II and 3.0 with placebo (p=0.0045). Transient side effects of nausea, stretching and yawning, and decreased appetite were reported more frequently after injections of Melanotan-II than placebo but none required treatment" [6].

The unique combination of effects, i.e. penile erection in addition to the hunger/satiety modulation properties, of Melanotan II as demonstrated in clinical trials renders it "complicate[d]" in applied treatment of obesity [3]. The CNS/MCR system plays a role in controlling adiposity through nutrient partitioning as well as cellular lipid metabolism independent of nutrient intake [3]. Pharmacologically inhibiting MCR in rats, and genetically disrupting MCR4 expression in mice, has resulted in lipid uptake, triglyceride synthesis, and fat accumulation in white adipose tissue "directly and potently." Conversely, increased CNS-MCR signalling increases lipid mobilization [3].

On the topic of MTII as a potential obesity treatment agent, Perboni et al write:

MC3R has been suggested to play a role in nutrient partitioning. Although agonists of the MC3R would not be expected to produce dramatic weight loss, they may favor a more beneficial partitioning of nutrients ... development of dual MC4 and MC3 receptor agonists has been addressed in order to reduce weight dramatically, as well as improve the metabolic co-morbidities of obesity significantly [3]. Melanotan II binds to both of these receptors.

Of a study performed on rats, Banno summarizes:

...data showed that food intake and body weight were decreased by chronic administration of MTII and that insulin sensitivity as well as glucose tolerance was improved by MTII in those rats. The serum TG [triglyceride] levels were also decreased by MTII, and these effects persisted for at least 25 days. Thus, our data demonstrated that melanocortin agonists administered peripherally ameliorated obesity, insulin resistance and hypertriglyceridemia in OLETF rats [4].

Banno et al also refer to other data, and synthesize these data with their own to conclude, similarly to Perboni, that "melanocortin agonists [such as MTII] could well be a promising treatment for obesity in humans":

...[in a study on humans,] there was not full compensation in food intake, and body weight remained significantly lower for about a month in the present study. These data suggest that melanocortin agonists could well be a promising treatment for obesity in humans...administration of MSH/ACTH4-10, a MC4R agonist, was shown to decrease body weight and body fat in healthy and normal weight humans without apparent side effects [4].

Conclusion:

Trends in current research suggest that Melanotan II and other MSHs will likely be implemented in various capacities for treatment of obesity, metabolic syndrome, and comorbid disorders. While trials for various delivery systems are underway for MTII and similar peptides to be used for treatment of erectile dysfunction and for aesthetic purposes (harnessing the well-known pigmentation properties of the MSHs), FDA approval for treatment of more serious issues such as the abovementioned is more likely. The MSH are unique in their disparate and broad actions in the body.

references:

[1] Hruby VJ, Lu D, Sharma SD, Castrucci AL, Kesterson RA, al-Obeidi FA, et al. Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4–10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors. J Med Chem 1995;38(18):3454–61.

[2] Molinoff PB, Shadiack AM, Earle D, Diamond LE, Quon CY. PT- 141: a melanocortin agonist for the treatment of sexual dysfunction. Ann N Y Acad Sci 2003;994:96–102.

[3] PEPTIDES IN ENERGY BALANCE AND OBESITY (Book), Gema Frühbeck (ed.), CAB International 2009, Subsection: Anorexigenic Peptides, Perboni, S., Ueno, G., Mantovani, and Inui, A. pp. 45-47

[4]Banno R. The melanocortin agonist melanotan II increases insulin sensitivity in OLETF rats. Peptides Volume 25, Issue 8, August 2004, pp. 1279-1286

[5]Dorr R.T., Lines R, Levine N., Brooks C., Xiang L., Hruby V.J., Hadley M.E. Evaluation of melanotan-II, a superpotent cyclic melanotropic peptide in a pilot phase-I clinical study. Life Sci, 1996;58(20), pp.1777-84.

[6] Wessells H., Fuciarelli K., Hansen J., Hadley M.E., Hruby V.J., Dorr R., Levine N. Synthetic melanotropic peptide initiates erections in men with psychogenic erectile dysfunction: double-blind, placebo controlled crossover study. J Urol. 1998 Aug;160(2): pp. 389-93.

Melanotan II Guide

Melanotan 2 Dose:

Light: .5mg
Common: 1mg
Large: 1.5mg

Melanotan 2 (MT-II) is an analog of alpha-melanocyte stimulating hormone (a-MSH). Melanotan 2 comes in the form of a freeze dried (lyophilized) peptide in a sterile multi-use vial.
Melanotan 2 acts on melanocytes to stimulate melanin production. Melanin is the body's natural pigment responsible for your tan.


Melanocortins are a family of peptides beginning with the sequence: His-Phe-Arg-Trp. Melanotan peptides bind to and activate melanocortin receptors (MCRs) which influence pigmentation, inflammation, energy homeostasis, appetite and sexual function. MT-2 MCRs: MC1R, MC3R, MC4R and MC5R.

Melanotan 2 is a smaller and more potent than M-I (which targets MC1R) targeting more receptors. Melanotan 2 has a protective ring-like amino acid structure as compared to a linear peptide such as Melanotan One or Afamelanotide.



What does this mean? The fair skinned CAN achieve a natural tan with synthetic MSH, Melanotan 2. For people with sun allergies these discoveries are life changing. The best defense against skin cancer is a natural tan developed over time. MT-2 was designed to reduce skin cancer rates and be effective as a sunless tanner.

Who uses Melanotan 2? Athletes and fitness enthusiasts choose MT-2 as a lifestyle product to increase tanning efficacy, the aphrodisiac and appetite suppression. MT-2 was dubbed the Barbie drug and has been highlighted in wired magazine. Synthetic melanocortin use helps to attain a tan with the least amount of exposure to harmful ultraviolet radiation (UVR).


Skin types I and II: Lower skin types on the Fitzpatrick scale are the best candidates for Melanotan 2.



Treatment: Melanotan stimulates melanin effectively, in particular those with low skin types.



Note: Melanotan is approximately 1,000 times more potent than natural a-MSH and MT-2 has a greater efficacy than M-I.

Disclaimer: Please pursue information regarding the usage of these products from your own research, academic journals, or the research of your in-house scientific team. Products are sold for research purposes are not for human consumption. Remember when you contact these types of stores/sponsors not to relate the questions or topics to human consumption or they tend not to answer. Always inquire in a research type question.

Melanotan 2 Peptide: Melanotan 2 peptides come in 5mg and 10mg sizes. Photograph at left shows a 5mg and 10mg MT-2 peptide as an example. Peptides within photograph were synthesized by the same laboratory, contain no filler and therefore volume reflects content. All peptides and freeze drying processes are not created equal. Current MT-2 industry standard is the 10mg, 2ml vial size. Trending towards lower doses, freshness, safety, travel and other factors are increasing demand for smaller quantities.

Reconstituted with bacteriostatic water (BW), MT-2 peptide remains potent and preserved. Reconstituting (mixing) your Melanotan 2 peptide is a necessity and will require proper due diligence for results. Nasal sprays, pre-mixed Melanotan 2, pills, oral and loose powder are not often legitimate. There are successful reports of nasal spray experiences, however, they are few and far between as the molecule is larger than the membrane will allow. Enzymes will render the peptide inactive if ingested.

Shipping and Handling: Melanotan peptides are durable and stable. Highlighted in study, the reconstituted MT-2 was shown to be stable at 37 degrees Celsius (98 degrees Fahrenheit) for at least 28 days. Shipping MT-2, even in summer months, is not a problem. Do not pay for cold shipping as it is not a premium. When receiving MT-2 it is recommended to store in the refrigerator.

Mixing: Add BW to the vial when you are ready to begin MT-2 research.

Remove plastic flip top from vial to expose rubber stopper. Needle will pierce the stopper making way inside the vial to turn the white powder into a clear liquid.

Calculator: Add 100 units (1ml) of water to the vial. 1ml/100 units will minimize the volume that you have to inject and will simplify the arithmetic in your MT-2 experiment. Dosing measurements are often mentioned in both milligram (mg) and microgram (mcg). Example: .5mg = 500mcg
http://peptidecalculator.com/

1ml syringe (U100), 1ml BW to reconstitute
Calculations for a desired 0.5mg dose:
Step 1= 1ml
Step 2= 10mg MT-II
Step 3= 1ml bact water
Step 4= 500mcg dose
2-3 ticks on your insulin pin (approximately 1/20th of a U100 syringe)



Some prefer to add more dilutent which works fine, take note of the volume increase.

Needles: 29-31 gauge X 1/2", 1 CC (100 unit). That is a typical insulin needle used to mix as well as inject. Use needles one time only. Once your technique perfected, injections are almost painless.

Starting dose: Your first injection should be a very small dose, for example .25mg (250mcg). See how you react. Goal should be to feel nothing. Dose after dinner, before bed. Any dosing chart stating that you should take a high dose (according to your weight) is outdated and potentially dangerous.

Loading dose: Load with 0.5-1mg once a day. People who have used doses in this range generally report getting excellent results. Don’t worry if you miss occasional days. It will not make much difference, focus on the cumulative effects.

Maintenance dose: Maintenance is taking doses less frequently than daily to avoid becoming darker than you want. Yes, that will happen. With enough UVR, you will get much darker than you have even been before. A maintenance dose can help prolong super-physiological photo-protection MT-2 delivers.

UV Radiation: Melanotan is a poor sunless tanner. UV (from sun or a tanning bed) light is necessary to develop a tan. Without it, almost nothing happens. In other words, NO UV = NO TAN. Well, user will pigment depending on skin type.... If you have loaded for a full month and then start UV exposure, you (and your friends) will be astounded by how fast you tan and how dark you get. Moreover, it is advisable to keep areas of your skin that ordinarily get exposure covered up with a towel and/or zinc oxide (nose/lips/face) and let less exposed areas develop pigmentation first. Areas of skin that are typically sun-exposed in your day to day life will respond more readily to the effects of the melanotan peptides.

Fat Loss: The melanocortin (MC) system is a signaling pathway for leptin and insulin. The MC system is important for control of food intake and body weight. MT-2 treatment results in adipocyte lipolysis. MT-2 increases fatty acid oxidation(FAO) in which the MC5R plays a significant role. MT-2 improves insulin sensitivity through stimulating FAO in skeletal muscle tissue. Reduced food intake from the anorectic response of MT-2 is primarily responsible for weight loss.

Watch yourself: Your tan can sneak up on you. A tan generally sets in 3 days after UV rays. Dose and expose yourself gradually to UVR when tanning. Love your skin.

Avoid burning: You are protected from burning mostly by your tan, not the MT-2 peptide. Therefore, don’t overdo the rays at first. Start with only as much UV that you could tolerate without burring before you began Melanotan. It should not take many weeks before you can tolerate hours of strong sun without burning. Truly incredible for those who have never experienced freedom to enjoy the sun.

Continue your regular dosing protocol until you have reached your desired tan and do not want to become darker. Cut injection frequency to once every 2, 3, 4, or even 7 days. Experiment to find the frequency that gives the tan you want.

Storage: Store freeze dried and reconstituted peptides in the refrigerator.

Do you have to inject MT-II?
Yes. The best, most efficient method of administering Melanotan peptides are subcutaneous (subq) injections. Nasal sprays are inconsistent and inefficient. No detectable levels were observed following oral dosing - pills do not work.



Note: There are many things you will need to consider before experimenting with this peptide. Cyclic analogues (MT-II) have a wide range of peripheral effects and systemic control is always going to pose an issue in clinical use. Needless to say, MT-II is not an approved or regulated product. MT-II is legal to buy, possess, etc. Variables such as skin type and individual goals need assessment. Ask for critiques, plans and create a user log during use. Seasoned users are generally more than happy to offer tricks of the trade.

When you start supplementing a-MSH to tan keep in mind that tanning is literally a side effect. The tanning response is, in reality, a physiological repair mechanism to instant UV damage of the skin cells (epidermis/dermis). Melanocyte stimulating hormone is not going to color your skin, it is going to make your own skin create its own tan and that in turn creates protection. If you are looking to be some bronzed beach God with perfectly uniform and specific color then you are better off to going to mystic tan. Redheads, for example, naturally produce a variant form of melanin that is yellowish-red (pheomelanin). Do not expect a brown tan on a ginger body right away.

Know your skin type: Knowing your skin type is just one detail which will help create a public user log. There are 10s of thousands of melanotan users worldwide who share the experience. Raise awareness and help others who want to hear success stories, complications and failures.

Am I a good candidate for MT-II?
Melanotan is best suited for the folks with skin types I & II. Prior sun damage, scars, tattoos, freckles, moles, hair color, etc are deciding factors prospective MT-2 users consider.

How should I dose MT-II?
Start out small and build up. A typical starting dose is around .25mg and max dose reaching 1mg.

Things to consider: There is no magic pill or formula. Few dermatologists are familiar with Melanotan. The skin is a large, unpredictable organ. Feel comfortable and confident with MT-II before use. Check out as many before and after photos and user logs as you can. A skin type I individual may have to commit months of dedication before dialing in their desired results, be patient.

How much MT-II should I buy and how long will it last?
Skin type I: 30-50mg
Skin type II: 20-30mg
Skin type III: 10mg
Should last entire summer or season

How soon will I begin to see results?
You should notice a change in your skin tone after three weeks. If you have freckles, expect them to get darker before your actual skin color changes.

How long will tan last?
A tan developed using Melanotan 2 lasts much longer than an ordinary tan. A well-tanned person returning from a beach holiday will lose most of the tan in a month if they stop getting sun. But if they had been using Melanotan 2 and continued on maintenance after returning, they would still have most of their tan 3 months later.

Melanotan 2 Report 2007:
YouTube - Melanotan II report on Campbell Live of TV3, New Zealand - Sept. 2007

Side effects of MT-II?
Possible short-term side effects you should know about, including: nausea, appetite loss, facial flushing and increased libido. These may be noticeable during the first few days of treatment but should taper off.

Dosing an anti-histamine, such as Claritin (Loratadine), works to eliminate sides such as nausea after injecting.