What is Bremelanotide (PT-141)?
Bremelanotide
(formerly PT-141) is the generic term for a new medication for use in
treating sexual dysfunction in men (erectile dysfunction or impotence)
as well as sexual dysfunction in women (sexual arousal disorder). It is
a synthetic aphrodisiac. Unlike Viagra and other related medications,
it does not act upon the vascular system, but directly increases sexual
desire.
Originally, the peptide Melanotan II that
bremelanotide was developed from was tested as a sunless tanning agent.
In initial testing, Melanotan II did induce tanning but additionally
caused sexual arousal and spontaneous erections as unexpected side
effects in eight out of the ten original male volunteer test subjects.
In clinical studies, bremelanotide has been shown to be effective in
treating male sexual and erectile dysfunction as well as female sexual
dysfunction. It is currently being tested by Palatin Technologies.
Bremelanotide
is a cyclic hepta-peptide lactam analog of alpha-melanocyte-stimulating
hormone (alpha-MSH) that activates the melanocortin receptors MC3-R and
MC4-R in the central nervous system. It has the amino acid sequence
Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH or cyclo-[Nle4, Asp5,
D-Phe7, Lys10]alpha-MSH-(4-10). PT-141 is a metabolite of Melanotan II
that lacks the C-terminal amide function. Its molecular formula is
C50H68N14O10 with a molecular weight of 1025.2.
In the United States it is currently in a Phase III clinical trial.
Are these nasal? Oral, Injectable?
Currently
the nasal and oral routes have not been made efficient. PT-141 is a
sterile injectable made for sub-q injection, like insulin.
What's the dosing schedule...how much do I take?
.5mg-2mg is the range which people dose. Taking 2-4 hours before game time is ideal. The window of opportunity is very unique.
Say
you had a dinner and movie arranged. Taking before dinner may be the
best route, however during the climax of the movie may interfere with
one of your own…read between the lines there
Is there any reconstituting involved?
Yes
and bacteriostatic water is the recommended solvent here. To mix the
vial with bact water, take one syringe (BD Ultrafine II 1cc or 1/3 cc
are excellent and I recommend them) and grab your vial of
bacteriostatic water. If using a 1 cc syringe (100 units), use the
syringe to withdraw 1 full ml (1cc) and inject that into the vial of
PT-141 through the rubber. Be sure to aim the needle towards the
glass, so that it will trickle down and not harm the peptide. Swirl
the vial to thoroughly mix and let the peptide dissolve. The key here
is to be gentle. Say you had the vial of PT-141 stored in the freezer,
move the vial of PT-141 to fridge for an overnight stay. Then you are
ready the next day to reconstitute the same temperature refrigerated
bact water with the PT-141 in the most efficient manner. Just some
tricks of the trade here.
So now you have 100 units (1cc) of
bacteriostatic water mixed with 10 mg of PT-141 in your vial ready to
go. A 1mg dose would be 10 units or .1ml (.1cc). Make sense? Hope so.
How is it stored?
The
lyophilized powder (freeze dried state) can be stored in the freezer or
refrigerator. Once reconstituted (mixed with water) it will be good
for a month in the refrigerator before it begins to degrade.
Does this help give erections or just put you in the mood?
“With
PT-141, you feel good, not only sexually aroused,” reported anonymous
patient 007, a participant in a Phase 2 trial, “you feel younger and
more energetic.” Said another patient: “It helped the libido. So you
have the urge and the desire. . . . You get this humming feeling;
you’re ready to take your pants off and go.” And another: “Twice my
wife and I had sex twice in one night. I came in [to work] and I just
raved about it: ‘Jesus, guys . . . 58 years old and you don’t do that.’
” Tales of pharmaceutically induced sexual prowess among 58-year-olds
are common enough in the age of the Little Blue Pill, but they don’t
typically involve quite so urgent a repertoire of humming, throbbing,
tingling, and double-dipping. Or as patient 128 put it: “My wife knows.
She can tell the difference between Viagra and PT-141.”
The
precise mechanisms by which PT-141 does its job remain unclear, but the
rough idea is this: Where Viagra acts on the circulatory system,
helping blood flow into the penis, PT-141 goes straight to the brain
itself. And there it goes to work, switching on the same neural
circuitry that lights up when a person actually, you know, wants to.
Basically
this takes men back to middle school. You may find yourself in a
similar situation as you were in 8th grade science class with the
teacher bent over helping the student in front of you. It may be
necessary to do a “tuck up” if at the office…especially at the public
pool!
Women state that the sensation given from injecting
PT-141 is like being in heat! One colleague in particular stated that
she didn’t know what was going on…but she had wanted “it” all day long
after dosing the night before.