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#Post#: 1280--------------------------------------------------
Melanotan and Melanotan II (MT2) - (part 1)
By: PartyBoy Date: June 9, 2019, 5:13 am
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[center] Melanotan and Melanotan II (MT2)[/center]
Article by PartyBoy (MT Lives Administrator and former
MuscleTalk Moderator)
Pharmaceutical Names of Actual and Related Peptides:
PT-141, Clinuvel, Epitan, Bremelanotide, Afamelanotide
Common Brand/Trade/Slang Names:
MTII, MT-II, MT2, MT-2, Scenesse
Amino Acid Structure:
Melanotan
al-NH2
or [Nle4, D-Phe7]-alpha-MSH
Melanotan II
Bremelanotide
cyclo-[Nle4, Asp5, D-Phe7, Lys10]alpha-MSH-(4-10)
Molecular Formula and Molecular Weight:
Melanotan
Melanotan II
Bremelanotide
Peptide Hormone Base:
(α-MSH)
Delivery Method:
oral, nasal and implanted pellet form are forthcoming
Half Life:
Contents:
with bacteriostatic water to provide an injectable solution.
[center][URL=
HTML https://beta.photobucket.com/u/BritishDragon1/p/71053e6a-2d07-44cc-85ba-1c2b5e16def0][IMG]https://hosting.photobucket.com/images/f149/BritishDragon1/0/71053e6a-2d07-44cc-85ba-1c2b5e16def0-original.jpg?width=1920&height=1080&fit=bounds[/img][/URL][/center]
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:
•
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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.
An example of a good solution would be to mix 10mg of Melanotan
II powder with 4ml of bacteriostatic water. This now provides:
10mg/4ml or 1mg/0.4ml or 0.25mg/0.1ml
0.1ml can be accurately measured using a 0.5ml or 1ml syringe.
Obviously, as your dosages become higher, you may dilute
subsequent vials with lower amounts of water to reduce the
volume of each shot. I would recommend that when you are using a
dosage of 1mg, you reconstitute the vial with 1ml or 2ml of
water so that each shot will be 0.1ml or 0.2ml respectively.
The injection is given into the sub-cutaneous layer which
includes adipose tissue (fat), as in the figure below:
If you are using insulin syringes which have short needles, you
will need to enter the skin at 90°. to the skin, otherwise you
can inject as shown in the illustration above with a 29 or 30
gauge, 0.5″ needle.
I would suggest that you use standard 1ml syringes to which you
can interchange needles as required. By doing so, you are able
to attach any gauge/length you want to reconstitute and draw the
solution (I use a 25guage 1″ needle). Once done, simply
attach your suitable needle for the injection. Following the
injection, ensure that you pull back the plunger a little to
‘reclaim’ the solution that is contained within the needle
itself. The syringe/needle is then placed in the refridgerator
for storage until your next injection is due whereby you will
attach a brand new injection needle. This process is repeated
until you have administered all of the solution in that
particular syringe.
Alternatively, you may pre-load insulin syringes and refrigerate
until needed. However, because they have non-detachable needles,
this can be quite cumbersome as they require loading from the
rear.
Instability of the peptide is a much greater issue once
reconstituted so you don’t want it sitting in the fridge for
months on end. Ideally one 10mg vial of MT-II could be shared by
two people (each having their own syringe/needles) so even
during the maintenance phase of two injections per week of 1mg
each; the longest it will be reconstituted for is 2.5 weeks.
Example of How to Dose Melanotan II
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on the needle only – see diagram)
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Part 2
HTML https://mtlives.createaforum.com/testosterone-other-steroids-and-ped's/melanotan-and-melanotan-ii-(mt2)-(part-2)
#Post#: 1288--------------------------------------------------
Re: Melanotan and Melanotan II (MT2) - (part 1)
By: PartyBoy Date: June 9, 2019, 9:16 am
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