Exploring the PT-141 Peptide

Erectile dysfunction (ED) and female sexual arousal disorder (FSAD) are considered to be influenced by various biological factors. FSAD is characterized by reduced sexual arousal, and erectile dysfunction (ED) is defined as a persistent lack of erection strength.

PT-141 Peptide: What is it?

A synthetic peptide called PT-141, also called Bremelanotide, is made from the naturally occurring alpha-melanocyte-stimulating hormone (α-MSH). Studies suggest that its primary function may be stimulating the central nervous system’s melanocortin 4 receptor (MC4R), a member of the family of melanocortin receptor agonists. C50H68N14O10 is its chemical formula, and 1025.2 g/mol is its molecular weight.

PT-141 Peptide History

Erectile dysfunction (ED) and female sexual arousal disorder (FSAD) have been increasingly studied. The hypothesis that melanocortin receptors, and MC4R in particular, may significantly influence sexual behavior and arousal underpinned many of the studies.

Research suggests that by interacting with MC4R and perhaps modulating neuronal pathways and neurotransmitter systems involved in sexual behavior, the synthetic peptide PT-141 aims to target the central nervous system and thereby induce improved function.

Several studies were conducted on PT-141 to determine its potential activity in the context of erectile dysfunction. The scientific community has maintained an interest in PT-141, leading to further investigations into its action mechanisms and other potential impacts outside of ED and FSAD.

PT-141 Peptide Potential

Investigations purport that the melanocortin receptor agonist potential of PT-141 may have the potential to rebalance in the context of FSAD. The arousal-inducing potential of PT-141 may be due to its capacity to increase sexual sensitivity and responsiveness by acting on certain brain regions associated with sexual behavior.

Experimental tests on PT-141 have suggested that it may be useful in the context of erectile dysfunction by increasing blood flow to the penis via vasodilation in the genital region. Because findings imply that PT-141 may reduce the risk of systemic negative effects that may occur from broad vasodilation. One way in which PT-141 has been theorized to differ from other substances is by its speculated local activity.

A crucial player in controlling sexual function and behavior is the melanocortin 4 receptor (MC4R), and PT-141 seems to regulate this receptor and others like it in the brain. When given to animal research models, PT-141 may activate signaling pathways further down the signal transduction cascade by binding to MC4R. Although the precise ways in which PT-141 might improve libido remain a mystery, it is hypothesized to have many theoretical properties:

• PT-141 has been hypothesized to increase vasodilation, which means more blood to the genital area, leading to growth and increased sensitivity
• Increased blood flow may result from several actions that make up the mechanism of action. PT-141 may promote vasodilation or the widening and relaxing of blood vessels, especially in the genital region. Second, it is thought that PT-141 might cause the smooth muscle cells that line the blood arteries to emit more nitric oxide (NO). 
• PT-141 may have the potential to affect the brain’s release of neurotransmitters, including dopamine, a crucial neurotransmitter. Dopamine is considered to be important in brain pleasure and reward circuits. A higher level of arousal and desire for sexual activity may result from PT-141’s potential to stimulate dopamine release via interactions with MC4R in specific areas of the brain.
• Following the presentation, PT-141 has been hypothesized to attach to certain brain melanocortin receptors, most notably the melanocortin 4 receptor (MC4R). This binding theorizes several neurotransmitters’ downstream signaling pathways to be activated. It is speculated that PT-141 may affect the production and activity of certain neurotransmitters associated with sexual function and arousal. However, the precise mechanisms by which it may regulate these pathways are still unclear

Additionally, research suggests that PT-141 may influence sexual function via its potential on serotonin and norepinephrine, among other neurotransmitters. For example, serotonin may impact arousal and is involved in regulating mood. The neurotransmitter and stress hormone norepinephrine may function in arousal and sexual response as well.

Researchers interested in studying PT-141 further are encouraged to navigate to the Core Peptides website for more educational articles and the highest-quality research compounds.

References

[i] Hedlund P. PT-141 Palatin. Current Opinion in Investigational Drugs (London, England : 2000). 2004 Apr;5(4):456-462. PMID: 15134289.

[ii] Diamond, L., Earle, D., Rosen, R. et al. Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction. Int J Impot Res 16, 51–59 (2004). https://doi.org/10.1038/sj.ijir.3901139

[iii] L.E. Diamond, D.C. Earle, W.D. Garcia, C. Spana, Co-administration of low doses of intranasal PT-141, a melanocortin receptor agonist, and sildenafil to men with erectile dysfunction results in an enhanced erectile response, Urology, Volume 65, Issue 4, 2005, Pages 755-759, ISSN 0090-4295, https://doi.org/10.1016/j.urology.2004.10.060.