HOPE THIS INFO PROVIDES USEFUL
Robbie
Pharmaceutical Names of Actual and Related Peptides: CUV1647, PT-141, Clinuvel, Epitan, Bremelanotide
Common Brand/Trade/Slang Names: Melanotan, Melanotan II, MT, MTII, MT-II, MT2, MT-2
Amino Acid Structure:
Melanotan - Ac-Ser-Tyr-Ser-Nle-Glu-His-D-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH2 or [Nle4, D-Phe7]-alpha-MSH
Melanotan II - Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2
Bremelanotide - Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH or cyclo-[Nle4, Asp5, D-Phe7, Lys10]alpha-MSH-(4-10)
Molecular Formula and Molecular Weight:
Melanotan – C78H111N21O19 1646.85 Dalton
Melanotan II – C50H69N15O9 1024.18 Dalton
Bremelanotide – C50H68N14O10 1025.16 Dalton
Peptide Hormone Base: alpha-melanocyte stimulating hormone (α-MSH) Delivery Method: Injectable at this time though transdermal, oral, nasal and implanted pellet form are forthcoming Half Life: 30-60 minutes Typical Vial Contents: 10mg lyophilised white powder. Requires reconstitution with bacteriostatic water to provide an injectable solution.
Background
Melanotan (MT) and Melanotan II (MT-II) are both analogs of the alpha-melanocyte stimulating hormone (α-MSH) which is produced within the pituitary gland. Along with other melanocortins, they are responsible for various internal human functions including skin and hair pigmentation, appetite, libido and physical sexual arousal. Whilst these effects have been observed in both sexes, it is worth noting that increases in libido and sexual function are exclusive to MT-II. This article will primarily look at the tanning and pigmentation properties of the hormone, though it would be foolish to ignore the other effects which are discussed further in the Side Effects section.
Prompted by ultraviolet (UV) exposure, α-MSH release consequently stimulates production of melanin from the melanocytes within the skin. Melanin, as I'm sure you are aware, is a brown pigment and responsible for the tanning of the skin. Simply put, more α-MSH means more melanin, resulting in greater skin pigmentation. Since bodybuilding is such an aesthetic pursuit, and with darker skin that accentuates muscularity, it's little wonder that these drugs are in such high demand.
Currently, analogs based upon MT and MT-II are undergoing clinical trials, with a view to bringing medicinal products to market. These synthetic variants of α-MSH were developed at the University of Arizona during the 1980s. Australian based Clinuvel Pharmaceuticals Limited have marketing rights to MT (CUV1647), with their primary market being individuals with adverse reaction to UV exposure. This includes those with Polymorphous Light eruption (PLE/PMLE) and Actinic Keratosis (AKs or solar keratosis) where skin is intolerant to UV and characterised by severe sores, lumps, itching or burning sensations, or dry skin lesions/growths. You might think that this peptide would be an ideal treatment for pure albinos. However, these individuals are generally not deficient in α-MSH, but instead are have zero melanocyte receptor binding. Therefore, merely increasing circulatory levels of α-MSH or its analogs is futile. Palatin Technologies Inc. based in the United States, has instead focused on an analog of MT-II. Licensed as Bremelanotide (formerly PT-141), this is aimed squarely at the sexual dysfunction market, more specifically, erectile dysfunction (ED) in men. However, early (phase I & II) clinical trials have also been performed using female subjects with results being described by the company as 'encouraging'.
Both Melanotan and Melanotan II have been shown in the clinical setting to increase pigmentation without exposure to UV, a feature that is also confirmed anecdotally by users that report tanning in areas of the body that would seldom see the light of day! However, the process of tanning is greatly expedited by UV exposure. It is worth noting that tanning effects may not be uniform throughout the skin. This is in part due to the half life and distribution of the drug itself, but primarily in response to the concentration of melanocytes within certain areas of the skin. Most will notice the greatest tanning effect on the face, arms, abdominal region. Interestingly, the genitals have one of the highest concentrations of melanocytes enabling these particular areas to respond very well to the peptide in conjunction with UV exposure.
As I'm sure you can appreciate, the development of these peptides has not gone unnoticed by the general population and as a result, there has been an explosion of suppliers looking to exploit such demand, with the peptides being formulated and originating largely from China. Although not classed as controlled substances in the UK, they are viewed as medicinal substances by the MHRA (Medicines and Healthcare products Regulatory Agency). While this means that you can legally possess them for personal use, sale or supply is dependant upon whether the product holds a Marketing Authorisation (product licence) valid for the UK. Since I cannot find any evidence of this, nor would I expect to at this juncture of development, suppliers plying their trade within the UK are doing so illegally.
Suggested Cycles/Uses
If you look hard enough out there, you will find some weird and wonderful dosaging schedules whereby the user calculates their daily dosage by multiplying their bodyweight by a cofactor. Perhaps this approach has been adopted since this has been the method employed in the ongoing clinical studies. Typically, this type of formula would suggest a dose of 1mg of MT-II per day for someone weighing in at a mere 110lb (50kg). The cynical among us might be forgiven for thinking that these formulae are constructed by those with a personal interest in the sale of the product as I believe this to be more than necessary to achieve a great result. Indeed, there are many instances whereby users feel they have become too dark. While I have no problem with a bodyweight dosage scale in principle, I can't help thinking that it's not only unnecessary (particularly for the mathematically challenged), but also avoids the ability to gradually increase dosages from a relatively low level; something which I would advocate to assess individual tolerance levels to side effects, especially in the case of MT-II.
Clinical trials to determine efficacy of the drugs have typically used dosages up to 0.21mg/kg daily for Melanotan (16mg for a 75kg (165lb) individual), and up to 0.03mg/kg daily for Melanotan II (2.25mg for a 75kg (165lb) individual). More typically however, trials have used the dosages of 0.16mg/kg (12mg) and 0.025mg/kg (1.875mg) respectively. At this level of dosage, one such study involving Melanotan indicated the following incidences of side effects from subjects:
* Nausea 85%
* Facial Flushing 75%
* Fatigue 44%
* Vomiting 26%
* Injection site reactions 13%
* Zero incidence of erections
* No change in vital signs or haematological parameters, blood biochemistry (liver and renal function)
As is the case with any drug use, the user is ideally looking to minimise unwanted side effects, whilst still achieving an acceptable outcome. With this in mind, I would suggest that a tapering up of dosages is used in order to assess the individual's personal tolerance to the side effects.
Both MT and MT II can be used for extended periods, whereby there is an initial daily administration of perhaps 2-3 weeks or until desired level of pigmentation has been achieved, followed by a maintenance phase of two injections per week.
Melanotan:
Start with a dose of 1mg daily for the first two or three days and, if level of side effects permit, look to increase dosage by 0.25mg every day over the next several days until you reach a daily dosage of 2-3mg. This level should be adequate for most users, though some may wish to increase yet further, perhaps as high as 5mg daily in order to achieve a very deep tan. A maintenance phase as described above is then used.
Melanotan II:
Start with a dose of 0.25mg. If side effects (primarily nausea) are not proving troublesome, attempt to increase daily dosage by 0.25mg where possible, until you reach 1-1.5mg daily. Most have found that this level will yield a very pleasing result and I can't see much point in increasing too much further unless a very deep tan was desired. As with Melanotan, once the desired level of tanning is reached, a maintenance phase is used.
Administration
Both MT and MT II are currently supplied as white lyophilised powder contained in a sealed multi-use vial. The peptide is susceptible to temperature degradation and should be shipped preferably with an ice pack though contrary to popular belief, the rate of degradation is very slow (weeks) in its powder form, so there's no need to be alarmed if yours wasn't shipped in this manner or you are unable to collect your package from a depot for a day or two. Once delivered, the powder is best stored in a freezer, or refrigerated if this is not possible.
To prepare for injection, it must be reconstituted with bacteriostatic water. You may use anything between 1ml and 5ml of water for your vial. Dependant upon the amount of water used will determine the concentration of your solution. For example, a 10mg vial of Melanotan II mixed with 1ml of water will provide a solution of 10mg per 1ml (10mg/ml). This means that a 1mg dose will require a shot of 0.1ml. Bearing in mind that the recommended starting dose is 0.25mg, using the example above, the actual volume of the shot would be 0.025ml (¼ of 1 tenth of a ml). This is a very small volume and very difficult to accurately dose even with a 0.5ml insulin syringe. Therefore, at least until your dosages have increased, it is suggested that you use more water for your vial.