Bremelanotide (PT-141)




PT-141 (Bremelanotide) is the first of a new class of drugs called melanocortin agonists being developed to treat sexual dysfunction. The mechanism of action of PT-141 (Bremelanotide) may offer significant safety and efficacy benefits over currently available products because it acts on the pathway that controls sexual function without acting directly on the vascular system. Clinical data indicates that PT-141 (Bremelanotide) may be effective in treating a broad range of patients suffering from ED. The nasal formulation of PT-141 (Bremelanotide) being developed is as convenient as oral treatments, is more patient-friendly than invasive treatments for ED, such as injections and trans-urethral pellets, and appears to result in a rapid onset of action.

About PT-141

Bremelanotide (PT-141) was developed from Melanotan 2 (MT-II). PT-141 is a metabolite of MT-II that lacks the C-terminal amide function-stripping away tanning properties

PT-141 is the only synthetic aphrodisiac. Studies have shown Bremelanotide to be effective in treating sexual dysfunction in both men (erectile dysfunction or impotence) and women (sexual arousal disorder). Unlike Viagra and other related medications (PDE5s), PT-141 does not act upon the vascular system, but directly through the nervous system (hypothalamus) to increase desire. Viagra, Cials and Levitra are not considered aphrodisiacs as they do not have any direct effect on the libido. However, treatment with PDE5 inhibitors and PT-141 are known to have a synergistic effect.

Bremelanotide is a melanocortin peptide hormone. PT-141 binds to the melanocortin 4 receptor (MC4R) in particular in the brain. Nine out of ten volunteers experienced sexual arousal in trials. The aphrodisiac effects of Bremelanotide are in a class of its own.

Bremelanotide comes in 10mg and 2mg vial sizes. Peptides photographed at right are synthesized by the same laboratory, contain no filler and therefore the difference is visible. Freeze dried Melanotan peptides (PT-141) are very durable and stable. Most PT-141 comes in the industry standard 10mg size. The 2mg PT-141 is used more as a travel peptide or couples dose. As a lifestyle peptide, the 10mg product is a lot to consume and may offer up to 20 doses when dosing light. The PT-141 peptide reconstituted with bacteriostatic water remains potent in the fridge for months. Nasal sprays, pre-mixed PT-141, pills and loose powder are not legitimate. There are successful reports of snorting and nasal spray experiences…however they are few and far between.

Bremelanotide, injected (subcutaneously), has a unique window of opportunity lasting six to 72 hours. In lab trials female rats exposed to PT-141 began “flirting” with male rats for sex. Postures and movements left no doubt in the male rats minds that they were in the mood. The human PT-141 date is one where the dosage precedes the activity by at least a couple hours. When the stars align, hours after the injection, …this is your window of opportunity, enjoy.

Example- 1ml(cc) bacteriostatic water per 10mg PT-141 vial equates to a 1mg dose approximately each 10 units on a U100 insulin syringe.
Example- 1ml(cc) bacteriostatic water per 2mg PT-141 vial equates to a 1mg dose approximately every 50 units on a U100 insulin syringe.

Recommended strategy for mixing and dosing would be to reconstitute with the volume that yields a .1ml injection.

Example- 1ml(cc) bacteriostatic water per 10mg PT-141 vial equates to a 1mg dose approximately each 10 units on a U100 insulin syringe.
Example- .2ml(cc) bacteriostatic water per 2mg PT-141 vial equates to a 1mg dose approximately every 10 units on a U100 insulin syringe.

Dosing: Read as much as possible to gain clarity and align expectations. Gradually dosing increases likelihood for success without sides. A test dose of .25-.5mg on the first attempt is recommended. 1mg, give or take a quarter, is the efficacious dose which yields the most positive reports by users.

Nasal spray for women who are sniffy about sex

Robin McKie, science editor

It is the seducer’s ultimate dream: a potion that will turn a woman’s cold indifference into warm sexual interest. Sound improbable? Not any more. Scientists last week revealed they had successfully tested a nasal spray, PT-141, that sent ‘healthy, normal women’ into states of high sexual arousal.

‘The crucial point about PT-141 is that it directly targets the brain’s arousal centre,’ said Dr Carl Spana, president of Palatin Technologies, of New Jersey. Originally uncovered through tests on rats, the drug aroused female rodents ‘so quickly they started mounting males’, added Spana.

Now the company hopes to market PT-141 for humans in two or three years though Spana stressed Palatin’s main target was people with sexual problems: men with impotence and women with low arousal.

Given that more than 40 per cent of women suffer from ‘female sexual dysfunction’ – they are interested in sex but cannot reach climax – this still gives PT-141 a massive market while at the same time providing hope for a lot of unsatisfied men.

The drug could even prove to be more popular than Viagra which works by directly stimulating blood flow in sexual organs. But for many women, it is lack of libido – not physiological difficulties – that causes them problems. By contrast, PT-141 targets the brain’s arousal centre and looks more likely to defrost sexual interest, says Palatin.

This point was underlined last week when Professor Raymond Rosen of New Jersey’s University of Medicine and Dentistry revealed results of the first human trials of PT-141. Sixteen healthy women were given the drug and 16 were given a placebo. All were shown erotic videos, while detectors measured blood flow in their vaginas.

The women given placebos hardly reacted while those on PT-141 had pronounced increases in blood flow – results that demonstrate the drug has potential that goes well beyond its use only as a medical aid, though Spana counselled caution. ‘The drug can only be administered as a nasal spray – which isn’t good for seducers. You can’t put it in a drink and sticking it up a girl’s nose is hard to do surreptitiously, after all.

‘On the other hand, related compounds could easily be made into pills one day, though I still don’t think they will turn on a woman who was previously totally uninterested in a man or in having sex. She has to be halfway there already.’

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