PT-141 (Bremelanotide)

PT-141 (Bremelanotide)

PT-141, also known as bremelanotide, is a peptide shown in clinical studies to enhance erectile function in men while increasing sexual desire and response in both men and women.

Quantity: 10mg per vial  |  Purity: Exceeds 99% (HPLC)

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Description
Description

Introduction

PT-141 is a melanocortinergic peptide with powerful erectogenic, sex drive, and libido enhancing properties. Also known as bremelanotide, it has been demonstrated in clinical study to promote increased sexual arousal and desire in male and female subjects alike. Critically, it has been shown to stimulate both mental and physical sexual arousal, with subjects reporting an increased desire for sex in addition to enhanced physical ability to engage in sexual intercourse. Although it is a metabolite of Melanotan 2, PT-141 does not have any tanning or skin pigmentation effects.




Mechanism of Action

PT-141 works in both sexes by binding to specific melanocortin receptors in the hypothalamus, specifically the MC3R and MC4R receptors. In men, it promotes erections by stimulating the production of nitric oxide in the corpora cavernosa, the erectile tissue in the penis. Nitric oxide is a critical initiator of vasodilation and blood flow vital to erectile function. Following administration, the increase in local nitric oxide production promotes engorgement of the penis and improved erection quality. Bremelanotide further promotes enhanced sexual function by facilitating the release of neurotransmitters key to motivating sexual desire, including oxytocin.

In women, PT-141 enhances sex drive by somewhat more complex mechanisms of action. When administered, the peptide stimulates specific regions of the brain governing sexual arousal and desire, promoting increased libido and enhanced physical arousal. Through its modulation of mesolimbic dopamine pathways, bremelanotide has been shown in studies to enhance female satisfaction with individual sexual motivation and response.

Properties

Properties

Structurally, PT-141 is a truncated cyclic lactam heptapeptide variant of α-MSH that has been altered to reduce enzymatic degradation (increase half-life) and enhance receptor binding (increase potency). The chemical name, Ac-cyclo[Nle4, Asp5,D-Phe7, Lys10]α-MSH4–10-OH, signifies that the PT-141 peptide is comprised of the 4-10 amino acid sequence of α-MSH, but with substitutions at the 4, 5, 7 and 10 positions and a lactam bridge connecting the amino acids at the 2 and 7 positions.

In essence, PT-141 is a shortened, circular analog of α-MSH consisting of seven amino acids.


Formal Name Bremelanotide
Synonyms PT-141; PT141
CAS Number 189691-06-3
Molecular Formula C50H68N14O10
Molar Mass 1025.2 Da (g/mol)
Amino Acid Sequence Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH
Peptide Structure
Physical Appearance Sterile filtered white lyophilized (freeze-dried) powder.
Dosage

Dosage Guidelines

For men:  suggested PT-141 dosages range from 0.5mg to 2mg per administration.
For women:  dosage amounts range from 0.25mg to 1mg per administration.

As with all melanocortinergic peptides, it is highly recommended to start with the lowest possible dose initially and increase only as necessary to attain the desired effects. Importantly, it is not recommended to exceed 2mg per dose (for men) or 1mg per dose (for women), as side effects at these higher levels may potentially become more pronounced. Ultimately, the appropriate dosage should be determined in consultation with an individual’s healthcare provider.

Individual reports indicate that the ideal time to administer PT-141 for men and women is around 4 hours before engaging in sexual activity. The effects of one dose typically last for around 24 hours in both sexes. There are incidences of effects lasting for a longer period of time, however, especially after a prior period of repeated daily dosing. Still, individuals will typically administer only one dose per 24 hour period, so as to avoid the occurrence of any negative side effects. This is likely an advisable practice.

Results

Positive Results in Men:

▪ Enhanced ability to achieve an erection
▪ Improved erection quality
▪ Enhanced ability to maintain an erection
▪ Increased libido and desire for sex

Unlike pharmaceuticals such as PDE5 inhibitors, which only affect physical erectile capability, PT-141 works both physically and mentally to stimulate sex drive. That is, the peptide not only improves an individual’s ability to achieve and maintain an erection, but it also enhances libido, increasing the desire for sex as well.

Physically, PT-141 improves erections by increasing nitric oxide levels in the erectile tissue of the penis. As nitric oxide is critical to blood flow and vasodilation, the increased levels promote enhanced blood flow to erectile tissue. This results in greatly improved erectile quality along with rapidly occurring, longer lasting erections.

Although the exact mechanisms of action by which bremelanotide enhances libido are still being revealed, research has shown that this effect may be linked to a facilitation of neurotransmitters key to sexual desire, such as oxytocin and dopamine. Studies have repeatedly demonstrated an increase in libido independent from physical arousal following the administration of PT-141.



Positive Results in Women:

▪ Increased libido and desire for sex
▪ Enhanced sexual response

While the purely physical effects of PT-141 in women may not be as pronounced as those in men, studies have repeatedly demonstrated its ability to enhance female sexual desire and satisfaction with sexual response when compared to a placebo. Bremelanotide has been shown to increase libido and enhance physical arousal in women by stimulating regions of the brain governing sexual arousal and desire. Further, the peptide has been revealed to modulate mesolimbic dopamine pathways involved in the response and motivation to engage in sexual activity. As a result, women in multiple studies have reported a greater desire for sex and an improved response following PT-141 administration lasting for around 24 hours after dosage.

Side Effects

Side Effects

PT-141 has been well tolerated in clinical studies. Typically, any side effects that do occur are often mild, if any, and pass quickly in a matter of minutes. Above recommended dosage levels, however, side effects may potentially increase to uncomfortable levels. This is why most individuals choose to start with a low dose initially and increase slowly and only if necessary.

Like all melanotan peptides, the most common side effects of PT-141 are flushing, dizziness, lightheadedness, and nausea. These effects are typically mild and clear up in minutes or seconds. Reports indicate that any side effects that do occur may tend to lessen over time as the body becomes used to bremelanotide administration.

Importantly, PT-141 does not have any skin tanning or pigmentation effects.

Again, at recommended dosage levels, PT-141 is generally well tolerated. However, at excessive amounts, harsher side effects may occur, including increased severity of dizziness or nausea as well as gastrointestinal discomfort. In men, administration of extreme levels of PT-141 may potentially lead to priapism, an erection that lasts longer than several hours. Needless to say, it is highly recommended to start with a small dose to assess individual tolerance to its effects before moving on to higher levels. Critically, PT-141 should only be used under professional medical supervision. Experts advise stopping use immediately and seeking medical attention if any abnormal reactions are suspected.

HPLC

PT-141 (Bremelanotide) HPLC


Mass Spec

PT-141 (Bremelanotide) Mass Spectrometry