Bremelanotide is being hailed by many as the first true aphrodisiac. Like many well known pharmaceuticals, it was discovered by accident. However, before describing in more detail I thought I'd share another story, one which led me to discover this substance.
Way back during the eighties when MDMA first appeared locally, I was talking to a friend about it. I'd only known the guy for a year or so, following his return from California with new wife and child. Apart from the odd beer I'd assumed he was straight and always had been. When I mentioned MDMA, he remarked that while in the states he knew a chemist who gave him and his girl a jar of the drug at a time before it became illegal. He then went on to talk about how the guy eventually got busted. My friend said that although they enjoyed their time with the drug, they had certainly had their fill of it.
Now, for some reason I've always remembered that story. Anyway, a few months ago while attending a party, I bumped into my friend again. It had been nearly 15 years since we'd last seen each other. During conversation I mentioned that story, and he said "Look up Leonard Pickard, he's the guy.... doing 2 life sentences atm..."
Leonard Pickard; now that name rang a bell, but I couldn't place it. We arrived home late from the party and crashed. I went to sleep with that name in my head, but some 3 hours later I awoke suddenly, remembering where I'd heard it. It was on a piece of video footage shot at the LSD symposium - to also celebrate Albert Hoffman 100th b/day - held earlier this year in Switzerland. I dug out the file and rewatched the piece. It had initially seemed quite confusing although I'd never followed it up.
Basically, the vid starts with an audience member - blotter-art historian Mark Mc Cloud - as he's interrupting Rick Doblin (from maps) while speaking. Mc Cloud gets quite loud, accussing one of Doblin's cohorts (John Halpern) of cooperating with the DEA to convict Leonard Pickard. The vid then switches to another scene, where surrounded by audience members, Mc Cloud lists the dates that Halpern appeared as witness, implying that Halpern is in part responsible for Pickard getting 2 life sentences for manufacturing LSD. The accusation was that Halpern had testified against Pickard for the DEA so as to gain government funding for MAPS work with MDMA. Pickard and associates had used an abandoned missile silo for manufacturing LSD and were caught with precursor chems and something like 400,000,000 x 100ug doses. So from what I can gather, Pickard was probably fucked anyway.
Halperngate footage (~32MB)
I cheked out Leonard Pickard further and was led to The William Leonard Pickard Website where among other very interesting things, the topic of Bremelanotide was addressed.
So what is this drug? Bremelanotide aka PT-141 was developed by Palatin Technologies. Early tests with Melanotan II, an artificial tanning compound, resulted in male rats developing erections. It was soon discovered the compound responsible was the metabolite of Melanotan II - PT-141, like Melanotan II, it's a cyclic petide. Reports also stated that female rats were so sexually stimulated, that they engaged in the rarely seen behavior where females would mount males.
It would appear Bremelanotide is fairly free of side effects and is now in stage 3 clinical trials. Depending upon the outcomes, bremelanotide could be available to the public sometime in the near future.
How does it work? Well, it doesn't work in any way like Viagra or Cialis. Those drugs work by inhibiting a specific phosphodiesterase enzyme which results in increased blood flow to the genitals. This is considered a purely physiological action. Bremelanotide however, seems to work at a much more basic level. It's been described as working on the same brain areas where cocaine and meth cause increased sexual desire. Bremelanotide apparently works in both men and women and is said to work on the same neural areas that are activated when someone gets horny naturally. So it's affects are claimed to be pyschological in essence, resulting in a "natural" state of arousal. However, apart from some claims of youthful euphoria and increased energy, unlike meth and coke, it doesn't result in a high or CNS stimulation.
The chemical structure of Bremelanotide is somewhat interesting in that it's a peptide containing 8 amino acid residues.
from Wikipedia: Bremelanotide
From my digging around I've discovered the drug is available online from chemical suppliers in India and China, although I haven't inquired as to price. Rumours say the Palatin product (their patent) will be very expensive, and that current OS sourced product is not cheap either. This then begs the question of whether the drug could, or will be made in a clandestine environment. Peptide synthesis is not all that difficult if the amino acids and other required chemicals are available (solid phase resins, protecting groups, deprotecting substances, linkers etc). I looked at this subject with great interest while studying drug discovery some years ago. While many of the techniques are different to those employed in most illicit drug syntheses, I do not believe clandestine production is outside the ability of educated chemists (as opposed to back yard cooks).
It's likely that hydrofluoric acid would be required as deprotecting agent, so if that is the case, clandestine manufacture would be limited to facilities that can protect against accidental exposure (10mg of HF spilt on the skin will kill everytime!)
Getting back to Pickard's page; Because of the mode of action of this drug, grave concerns have been expressed regarding the possibility of Bremelanotide being used as the next date rape drug. This is certainly a concern, as unlike other drugs used in this manner, Bremelanotide does not result in any noticeable state of intoxication. Also, the dose response window is very large, so many times the standard dose could be administered without apparent side effects. So, while it may be of great benefit to post-menopausal women and men suffering erectile dysfunction, the potential for abuse is certainly there, particularly in the area mentioned.
From Pickard's Site A Word of Caution Concerning Bremelanotide (PT-141)
15.) While recognizing that bremelanotide may be effective in ameliorating clearly-defined instances of FSD or ED and may be successfully employed as a marital adjuct, global distribution of an erotogenic drug that selectively induces sexual response may also result in signifiant societal problems, viz.:
a.) unanticipated social consequences from non-medical use.
b.) substantially heightened promiscuity across age groups and genders.
c.) surreptitious administration to unwitting individuals, resulting in drug-induced consensual sexual activity among individuals that would not consent in the absence of the drug.
d.) a increase in "date-rape" in conjuction with flunitrazepam or other drugs.
e.) an increase in the incidence of prostitution, including the drug's employment in human trafficking.
f.) an increase in sexual crimes, including rape, gang-rape, and child abuse.
g.) uncontrolled use among minors.
h.) abuse among users of crack cocaine, cocaine, or methamphetamine.
i.) abuse among populations that would not normally employ any unprescribed drug.
j.) overdose scenarios requiring medical intervention.
k.) medical complications from acute or chronic use.
l.) an increase in sexual aberrrations that are rarely seen by clinicians.
m.) increased incidence of AIDS and other sexually transmitted diseases.
n.) increased incidence of unwanted births, and among lower age cohorts.
o.) the advent of criminal organizations specializing in manufacture or distribution of this or related substances.
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