Peptides > PT-141
PT-141
PT-141, also known by its generic clinical name Bremelanotide, is a synthetic peptide derived from alpha-melanocyte-stimulating hormone (α-MSH). It has undergone clinical trials as a potential treatment for hypoactive sexual desire disorder (HSDD) in both men and women, as well as for acute hemorrhage. It acts as an agonist for the melanocortin-4 receptor (MC4R) and the melanocortin-1 receptor (MC1R). Research indicates that it has the ability to enhance sexual arousal and stimulate the immune system.
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This PRODUCT IS INTENDED AS A RESEARCH CHEMICAL ONLY. This designation allows the use of research chemicals strictly for in vitro testing and laboratory experimentation only. All product information available on this website is for educational purposes only. Bodily introduction of any kind into humans or animals is strictly forbidden by law. This product should only be handled by licensed, qualified professionals. This product is not a drug, food, or cosmetic and may not be misbranded, misused or mislabled as a drug, food or cosmetic.
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What Is PT-141?
PT-141, also known as bremelanotide, has earned the nickname “female Viagra” due to its investigation in phase IIb human clinical trials as a potential treatment for female hypoactive sexual desire disorder (HSDD). This synthetic melanocortin primarily binds to the melanocortin 4 receptor (MC-4R) and melanocortin 1 receptor (MC1R). In addition to its application in HSDD, It was also studied in 2009 as a treatment for acute hemorrhage. It is derived from another synthetic melanocortin called melanotan 2 (MT-2).
PT-141 Molecular Structure
Sequence: Ac-Nle-Asp(1)-His-D-Phe-Arg-Trp-Lys(1)
Molecular Formula: C50H68N14O10
Molecular Weight: 1025.182 g/mol
PubChem CID: 9941379
CAS Number: 189691-06-3
PT-141 Research
PT-141, through its stimulation of the MC-4R, plays a unique role in promoting sexual arousal. Studies in mice have demonstrated that activation of the MC-4R leads to sexual arousal and increased copulation in both male and female rodents. Unlike medications like Viagra, which primarily address issues related to blood flow, Bremelanotide operates through a different mechanism, making it a potential treatment for sexual arousal disorders in both men and women stemming from various causes.
In a study involving men with erectile dysfunction (ED) who did not respond to sildenafil (Viagra), approximately one-third of them experienced sufficient erection for sexual intercourse when treated with Bremelanotide in the form of a nasal spray. Furthermore, the trial showed a strong dose-dependent response, indicating the effectiveness of Bremelanotide in specific cases. This suggests that Bremelanotide may offer a viable option for addressing ED in situations where sildenafil has proven ineffective and may shed light on central causes of hypoactive sexual desire.
PT-141 and Female Sexual Dysfunction PT-141, although showing promise in clinical trials for treating Hypoactive Sexual Desire Disorder (HSDD) in women by increasing satisfying sexual events and reducing sexual distress, was halted before approval. This decision has left experts in female sexual dysfunction (FSD) disappointed, citing a lack of clear trial endpoints and societal biases as major obstacles to approval. They call for increased attention to women’s sexual health and the establishment of firm FDA guidelines for evaluating such therapies. Additionally, experts believe that combining pharmacological treatments like Bremelanotide with established methods could yield synergistic benefits.
Reconnect Trials and the Future of PT-141 In response to the discontinuation of earlier PT-141 trials, Phase II Reconnect trials were initiated in 2017, involving subcutaneous Bremelanotide injections for FSD. A new version of PT-141, known as Rekynda, may soon become available in the United States. This could open the door for off-label use of Bremelanotide to address both male and female sexual dysfunction. These trials have incorporated modified endpoints recommended by FSD experts to facilitate treatment approvals.
PT-141 and Hemorrhage In 2009, PT-141 was slightly modified and explored as a potential treatment for hemorrhagic shock. Its binding to both MC-1R and MC-4R receptors helps reduce ischemia and protect tissues in cases of hypovolemic (hemorrhagic) shock when administered intravenously. Notably, this version of PT-141, referred to as PL-6983, demonstrated minimal side effects during phase IIb trials.
PT-141 and Infection MC-1R, the receptor targeted by Bremelanotide, has exhibited significant anti-fungal and anti-inflammatory properties in a rat model of a specific fungal infection. This is particularly significant due to the limitations and severe side effects associated with current antifungal medications. An alternative like PT-141 could potentially reduce morbidity and mortality, especially among immune-compromised patients.
PT-141 and Cancer MC-1R receptor’s role in stimulating DNA repair pathways has raised interest in cancer treatment and prevention. Research indicates that individuals with MC-1R variants face an increased risk of basal cell and squamous cell carcinoma. Altered versions of PT-141 may have the potential to address issues related to these variants and aid in the prevention or treatment of these types of cancers.
Research Directions
PT-141: Beyond Sexual Dysfunction and Hemorrhage While PT-141 has garnered significant attention as a potential treatment for sexual dysfunction and hemorrhage, its applications extend beyond these areas. For example, MC-4R, a receptor targeted by PT-141, is known to be defective or absent in certain cases of obesity, possibly contributing to up to 6% of early-onset obesity cases. PT-141 presents a unique avenue for investigating this specific cause of obesity and exploring potential intervention strategies.
Versatility of MC-1R and PT-141 MC-1R, another receptor affected by PT-141, plays diverse roles in pain, inflammation, kidney pathology, and the spread of infection. PT-141 holds the potential to shed light on these various facets through research. It is worth noting that PT-141 has demonstrated minimal side effects and exhibits favorable bioavailability when administered subcutaneously or orally in mice. However, it’s crucial to emphasize that the dosage per kilogram in mice does not directly translate to humans. Any PT-141 purchase from Peptide Sciences is strictly intended for educational and scientific research purposes and is not intended for human consumption. Only licensed researchers should consider acquiring PT-141 for their studies.
Article Author
The above literature was researched, edited and organized by Dr. Logan, M.D. Dr. Logan holds a doctorate degree from Case Western Reserve University School of Medicine and a B.S. in molecular biology.
ALL ARTICLES AND PRODUCT INFORMATION PROVIDED ON THIS WEBSITE ARE FOR INFORMATIONAL AND EDUCATIONAL PURPOSES ONLY.
The product information featured on this website pertains exclusively to in-vitro studies. In-vitro studies, also known as ‘in glass’ studies, are conducted outside of living organisms. It’s important to emphasize that these products do not constitute medicines or drugs and have not received FDA approval for the prevention, treatment, or cure of any medical conditions, ailments, or diseases. It is crucial to note that the introduction of these products into the bodies of humans or animals is strictly prohibited by law.
