PT-141

What is PT-141 and How Does PT-141 Work?

PT-141 is a heavily modified derivative of a natural hormone called alpha-melanocyte stimulating hormone (α-MSH). In the most general sense, PT-141 works directly through the nervous system to increase sexual desire, arousal, and satisfaction. It does this by mimicking some, but not all, of the properties of α-MSH. To understand in more detail how does PT-141 work, it is necessary to understand the melanocortin system and the peptides that interact with it.

What Is a Melanocortin?

In the quest to understand how PT-141-works, it is necessary to understand how the melanocortin system works. All melanocortin’s are peptide hormones, which is to say proteins (made up of amino acids). The group gets its name from the parent molecule, proopiomelanocortin (POMC), that all other melanocortin’s are derived from. POMC is made in the pituitary gland, which is part of the brain and a critical center for controlling growth, the sleep/wake cycle, sexual desire, hunger, and more. Natural melanocortin’s made from POMC include melanocyte-stimulating hormone (MSH) and adrenocorticotropic hormone (ACTH). MSH has long been associated with sexual arousal and changes in appetite.

How Does UV Light Cause Tanning?

UV light causes tanning, which is to say and increase of the skin pigment melanin, by stimulating a cellular process mediated by the tumor-suppressor gene p53[1]. The whole point of this process is to protect skin cells against UV light, which can damage DNA and lead to problems like cancer, cell death, and the breakdown of extracellular matrix proteins (e.g., collagen) in the skin. This latter effect is what leads to observable skin aging in the form of wrinkles, lines, lost elasticity, and more.The pathway is activated when UV light damages DNA in the upper layers of the skin. The damage done to the DNA results in stabilization and activation of the p53 tumor suppressor protein. This, in turn, promotes activation of proopiomelanocortin (POMC). POMC is cleaved to product alpha-melanocyte stimulating hormone (α-MSH), which then binds to the melanocortin 1 receptor (MC1R). This causes melanocytes to both produce more melanin as well as divide and increase in number. Together, these effects cause an increase in melanin pigment leading to darkening of the skin. The melanin then absorbs the harmful UV light preventing further DNA damage[2].Note that tanning via UV light does not occur until after DNA damage has occurred. This means that the potential for cancer development is already present before tanning occurs because DNA damage has already occurred. Therefore doctors have warned against UV-based tanning for years. The only solution, until recently, has been to avoid UV light entirely by either staying out of the sun or by wearing sunscreen. Unfortunately, recent research shows that sunscreen has problems of its own such as damaging coral reefs and potentially causing hormone dysregulation[3]. The current research is focused on promoting melanin production without exposure to UV light, thus gaining the benefits of melanin protection without first inducing DNA damage.

The New Solution to Sunless Tanning

If scientists could stimulate tanning without the DNA damage that jumpstarts the natural process, then we could experience the benefits of tanning without any of the risks. Research into the tanning pathway has been of interest for several decades now, in part because of the discovery of melanotan and the melanocortin receptor system. Interestingly, melanotan was developed as a sunless tanning agent and then became of interest for an entirely different purpose. It’s ability to protect the skin against UV damage was almost completely forgotten as its ability to stimulate sexual arousal became the focus of melanotan research. Much later, research shifted again and melanotan became a front-runner in sunless tanning research. This peptide has since inspired the exploration and development of other peptides for sunless tanning research. Some of those peptides are discussed below along with other compounds associated with sunless tanning.

Primary Benefits of PT-141 in Summary According to Research

Enhanced Sexual Arousal: PT-141’s mechanism of action as a melanocortin receptor agonist may lead to increased sexual arousal and desire in individuals with FSAD. By targeting specific neural pathways involved in sexual behavior, PT-141 may help improve sexual sensitivity and responsiveness to sexual stimuli, leading to a heightened sense of arousal.

Improved Erectile Function: For men with ED, PT-141 has shown promise in clinical studies as a potential treatment for enhancing erectile function. By promoting vasodilation in the genital area, PT-141 can increase blood flow to the penis, potentially aiding in achieving and maintaining erections necessary for satisfactory sexual performance.

Localized Action: PT-141’s effects are primarily localized to the genital region, which helps minimize systemic side effects that might be associated with widespread vasodilation. This localized action makes PT-141 different from some other medications used to address sexual dysfunctions.Potential Alternative to Existing Treatments: For individuals who do not respond well to or cannot tolerate other treatments for sexual dysfunctions, PT-141 offers a potential alternative approach. Its unique mechanism of action makes it distinct from other medications like phosphodiesterase type 5 (PDE5) inhibitors commonly used for ED.

Psychological Benefits: By enhancing sexual desire and function, PT-141 may have positive psychological effects, boosting self-esteem and overall sexual satisfaction.

Mechanism of Action: PT-141 works by stimulating specific melanocortin receptors in the brain, particularly the melanocortin 4 receptor (MC4R), which plays a key role in regulating sexual function and behavior. Upon administration, PT-141 binds to MC4R, leading to the activation of downstream signaling pathways.