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Melanotan and Melanotan II (MT2) - (part 2)
By: PartyBoy Date: June 9, 2019, 5:38 am
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[center] Melanotan and Melanotan II (MT2)[/center]Part 2
Major Differences between Melanotan and Melanotan II (MT2)
I’m guessing by now the question on most people’s mind would be
which of the two is better? The short answer is Melanotan for
the obvious reason that it facilitates tanning with limited side
effects. It is for this reason that this analogue is being
trialled with a view to bringing it to market by Clinuvel. They
would be faced with an almost impossible mission had they chosen
instead MT-II to develop and place before the regulatory
authorities for approval. This is due to the host of extra side
effects commonly encountered by users of this analogue, perhaps
also coupled with the fact that the side effects that are shared
with Melanotan appear more pronounced.
However, in terms of monetary cost, and perhaps also a desire to
experience and utilise the other side effects, most prospective
users will choose Melanotan II.
Melanotan’s peptide structure is very closely matched to that of
our endogenously produced alpha-melanocyte stimulating hormone
(α-MSH). It is a specific agonist of the melanocortin-1
receptor (MC-1R) which is primarily responsible for skin colour
and is found on melanocyte cells.
Melanotan II on the other hand has a much shorter sequence of
amino acids and because of this quite pronounced change in
length and structure, is an agonist of the range of melanocortin
receptors. Perhaps more importantly, binding at receptors other
than MC-1R is far greater than that of Melanotan. This ‘shotgun
effect’ agonism of the full spectrum of different melanocortin
receptors results in some effects that are only witnessed from
MT-II. Most notably, increases in sexual arousal are due to
MT-II’s activation of MC-3R and MC-4R.
Because the amino acid sequence is much shorter in the case of
MT-II, there is therefore a much greater density of peptide
chains than is present using MT within a given set weight.
Although the receptor binding affinity of MT-II may not be quite
as effective, there will be much more peptide chains than for MT
on a mg for mg basis so effectively you require much less in
terms of milligram weight of Melanotan II to achieve similar
results. This accounts for the wide difference in suggested
dosages for each peptide and of course, makes MT-II a much
cheaper proposition.
Effects / Side Effects
[table]
[tr][td] Melanotan [/td]
[td] Melanotan II[/td]
[/tr]
[tr][td] Skin pigmentation [/td]
[td] Skin pigmentation[/td]
[/tr]
[tr][td] Nausea [/td]
[td] Nausea[/td][/tr]
[tr][td] Flushing (esp. facial) [/td]
[td] Flushing (esp. facial)[/td]
[/tr]
[tr][td] Headache [/td]
[td] Headache[/td]
[/tr]
[tr][td] Lethargy [/td]
[td] Lethargy[/td]
[/tr]
[tr][td] Itching [/td]
[td] Itching[/td]
[/tr]
[tr][td] Dizziness [/td]
[td] Dizziness[/td]
[/tr]
[tr][td] New mole appearance or darkening [/td]
[td] New mole appearance or darkening[/td]
[/tr]
[tr][td] Hyperpigmentation [/td]
[td] Hyperpigmentation[/td]
[/tr]
[tr][td] White patches [/td]
[td] White patches[/td]
[/tr]
[tr][td] - [/td]
[td] Increased libido[/td]
[/tr]
[tr][td] - [/td]
[td] Physical sexual arousal[/td]
[/tr]
[tr][td] Anaphylactic shock [/td]
[td] Anaphylactic shock[/td]
[/tr]
[/table]
Of the above listed effects/side effects, it is worth bearing in
mind that the prevalence and severity are witnessed to a greater
degree from Melanotan II. Indeed, most will find Melanotan very
comfortable to use, typically only experiencing minor nausea,
appetite suppression and flushing.
Although side effects do become less troublesome with each
administration of MT or MT-II, most users will experience at
least some of the side effect to varying degrees, most commonly
nausea, appetite suppression, facial flushing and dull
headaches. These will typically become apparent within a few
minutes of administration but can last for many hours. In the
case of MT-II, increases in libido are often seen in conjunction
with outwardly physical signs of sexual arousal whereby the male
user experiences prolonged periods of increased blood flow to
the penis. This particular side effect does not diminish in
severity over time and instances of occurrence are to be
expected throughout the period of MT-II use. As I’m sure you can
appreciate, this aspect may prove embarrassing and perhaps quite
uncomfortable, so I must stress again the importance of building
dosage up gradually to assess personal tolerance and
susceptibility.
Some users will notice the new appearance of freckles as these
particular areas of skin have increased melanin. The good news
is that as the tan is developed, the visual appearance of them
will diminish, probably completely. Moles commonly become darker
too as these are actually highly concentrated clusters of
melanocytes. Both of these occurrences will reverse some time
after discontinuation of the peptide and suntanning is ceased.
In addition to freckles and mole changes, there are fairly rare
reports of a phenomenon called hyperpigmentation. This is
typified by blotches of darkened skin, normally much larger than
regular moles. Not all incidences of hyperpigmentation are
attributable to increased melanocyte activity even though their
appearance may only become apparent during melanocortin receptor
agonism by Melanotan I or II. This condition is specifically
referred to as diffuse hyperpigmentation, with many possible
underlying causes or disorders including Addison’s disease,
haemochromatosis, hyperthyroidism and certain medications which
may induce phototoxic reactions.
Previously unseen white spots or white patches of skin may also
become apparent as the tan deepens. Again, this is not thought
to occur as a direct result of using Melanotan, rather it merely
uncovers the underlying condition. There are a range of actual
causes. White spots (typically 2-5mm in size) may be the result
of Idiopathic guttate hypomelanosis where there are reductions
in the number of melanocytes and melanin in those particular
areas. Larger white areas of skin may be due to Tinea versicolor
which is a fungal infection caused by the yeast Malassezia
furfur which is found on the skin and is not normally
troublesome. Treatment would normally include an oral or topical
anti-fungal though it may take many weeks for the skin tone to
become consistent with surrounding areas.
It has been suggested that due to the greater difference of
MT-II to our own α-MSH, there is a greater chance of the
body to view the peptide as a ‘foreign body’ and produce an
allergic response. This could potentially trigger anaphylaxis, a
potentially life threatening situation whereby large amounts of
histamine are produced by the body which can lead to a host of
effects including severe bronchoconstriction and rapid drops in
blood pressure.
References
Hadley ME, Dorr RT
Peptides. 2006 Apr;27(4):921-30. Epub 2006 Jan 18
Melanocortin peptide therapeutics: historical milestones,
clinical studies and commercialization.
Hadley ME.
Peptides. 2005 Oct;26(10):1687-9
Discovery that a melanocortin regulates sexual functions in male
and female humans.
Zheng H, Patterson LM, Phifer CB, Berthoud HR
Am J Physiol Regul Integr Comp Physiol. 2005 Jul;289(1):R247-58.
Epub 2005 Mar 3
Brain stem melanocortinergic modulation of meal size and
identification of hypothalamic POMC projections
Grill HJ, Ginsberg AB, Seeley RJ, Kaplan JM
J Neurosci. 1998 Dec 1;18(23):10128-35
Brainstem application of melanocortin receptor ligands produces
long-lasting effects on feeding and body weight.
Shrestha YB, Wickwire K, Giraudo SQ
Neuroreport. 2004 Jun 7;15[8]:1365-7
Action of MT-II on ghrelin-induced feeding in the
paraventricular nucleus of the hypothalamus.
Trivedi P, Jiang M, Tamvakopoulos CC, Shen X, Yu H, Mock S,
Fenyk-Melody J, Van der Ploeg LH, Guan XM
Brain Res. 2003 Jul 11;977(2):221-30
Exploring the site of anorectic action of peripherally
administered synthetic melanocortin peptide MT-II in rats.
Dorr RT, Ertl G, Levine N, Brooks C, Bangert JL, Powell MB,
Humphrey S, Alberts DS.
Arch Dermatol. 2004 Jul;140(7):827-35
Effects of a superpotent melanotropic peptide in combination
with solar UV radiation on tanning of the skin in human
volunteers.
Dorr RT, Dvorakova K, Brooks C, Lines R, Levine N, Schram K,
Miketova P, Hruby V, Alberts DS.
Photochem Photobiol. 2000 Oct;72(4):526-32
Increased eumelanin expression and tanning is induced by a
superpotent melanotropin [Nle4-D-Phe7]-alpha-MSH in humans.
Barnetson RS, Ooi TK, Zhuang L, Halliday GM, Reid CM, Walker PC,
Humphrey SM, Klienig MJ
J Invest Dermatol. 2006 Aug;126[8]:1869-78. Epub 2006 Jun 8
[Nle4-D-Phe7]-alpha-melanocyte-stimulating hormone significantly
increased pigmentation and decreased UV damage in fair-skinned
Caucasian volunteers.
Dorr RT, Lines R, Levine N, Brooks C, Xiang L, Hruby VJ, Hadley
ME
Life Sci. 1996;58(20):1777-84
Evaluation of Melanotan-II, a superpotent cyclic melanotropic
peptide in a pilot phase-I clinical study
Diamond LE, Earle, DC, Heiman JR, Rosen RC, Perelman MA, Harning
R
J Sex Med. 2006 Jul;3(4):628-38.
An effect on the subjective sexual response in pre-menopausal
women with sexual arousal disorder by bremelanotide (PT-141), a
melanocortin receptor agonist.
Wessells H, Gralnek D, Dorr R, Hruby VJ, Hadley ME, Levine N
Urology. 2000 Oct 1;56(4):641-6.
Effect of an alpha-melanocyte stimulating hormone analog on
penile erection and sexual desire in men with organic erectile
dysfunction.
Wessells H, Fuciarelli K, Hansen J, Hadley ME, Hruby VJ, Hadley
ME, Levine N
J Urol. 1998 Aug;160(2):389-93
Synthetic melanotropic peptide initiates erections in men with
psychogenic erectile dysfunction: double-blind, placebo
controlled crossover study.
Molinoff PB, Shadiack AM, Earle D, Diamond LE, Quon CY
Ann N Y Acad Sci. 2003 Jun;994:96-102.
PT-141: a melanocortin agonist for the treatment of sexual
dysfunction.
Wessels H, Hruby VJ, Hackett J, Han G, Balse-Srinivasan P,
Vanderah TW
Ann N Y Acad Sci. 2003 Jun;994:90-5
MT-II induces penile erection via brain and spinal mechanisms.
Warning! Articles related to the use of performance enhancing
drugs are for information purposes only and are the sole
expressions of the individual authors opinion. We do not promote
the use of these substances and the information contained within
this publication is not intended to persuade or encourage the
use or possession of illegal substances. These substances should
be used only under the advice and supervision of a qualified,
licensed physician.
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