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Bremelanotide, which is also commonly known by PT-141, is a synthetic peptide composed of 7 amino acids (2). PT-141 synthetic peptide appears to be agonistic to melanocortin receptors, which is similar to the natural hormone alpha-MSH (3). Initial studies suggested that melanocortin hormones may regulate various physiological functions. When test animals were presented with the isolated hormone, it was reported to present elevated the sexual functions, which is one of the primary areas of research currently being conducted on PT-141 peptide.
Studies (3) have suggested that PT-141 shows agonistic properties towards melanocortin receptors, namely MC3R and MC4R, which may result in elevated reactions in the central nervous system. In these studies (3), it was reported by researchers that after binding with the MC3R and MC4R receptors, the peptide appeared to lead to the activation of the neurons found in the hypothalamus, leading to apparently increased immunoreactivity. Neurons in the surrounding region of the central nervous system may also be stimulated as they intake the chemicals which then reportedly lead to sexual arousal in the study animals.
Research and Clinical Studies
PT-141 Peptide Initial Studies
This early 2000 study (8) was conducted to understand the potential of PT-141 peptide in female rats. The female rat model was used as the subject in this study to determine how the peptide may impact their sexual behavior. After presentation, it was reported that the female rats appeared to exhibit elevated sexual desire without any increase/decrease in the sexual pace, lumbar lordosis, or any other behaviors. After analysis, it was suggested by the researchers that the peptide did not directly impact a generalized motor activation, instead it may have potential selective pharmacological impact that may stimulate the central nervous system, mainly the melanocortin receptor activities, which might result in elevated sexual arousal.
PT-141 Peptide and the Central Nervous System
In this study (9), the main focus was to understand the potential of the peptide in the central nervous system (CNS) and possibly also some brain regions. The study was carried out in prime age female rats with rich levels of the female sexual hormones. Researchers mainly focused on both the sexual behaviors of the rats i.e., appetitive behaviors such as increased pace and agitation, and consummatory behaviors such as lordosis. In this study, the rats were presented with the peptide, which apparently resulted in increased levels of appetitive behavior of solicitation, without impact on the sexual pace or lordosis. Researchers suggested that the primary reason for this reported behavior was induced mPOA, which may lead to the activation of the hypothalamic and other regions of the brain causing increased sexual behavior.
PT-141 peptide is available for research and laboratory purposes only. Please review and adhere to our Terms and Conditions before ordering.
1. AHFS Monographs – Bremelanotide. https://www.drugs.com/monograph/bremelanotide.html
2. National Center for Biotechnology Information. “PubChem Compound Summary for CID 9941379, Bremelanotide” PubChem, https://pubchem.ncbi.nlm.nih.gov/compound/Bremelanotide
3. Molinoff PB, Shadiack AM, Earle D, Diamond LE, Quon CY. PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Ann N Y Acad Sci. 2003 Jun;994:96-102. https://pubmed.ncbi.nlm.nih.gov/12851303/
4. Hadley ME. Discovery that a melanocortin regulates sexual functions in male and female humans. Peptides. 2005 Oct;26(10):1687-9. doi: 10.1016/j.peptides.2005.01.023. https://pubmed.ncbi.nlm.nih.gov/15996790/
5. Hadley ME, Dorr RT. Melanocortin peptide therapeutics: historical milestones, clinical studies and commercialization. Peptides. 2006 Apr;27(4):921-30. doi: 10.1016/j.peptides.2005.01.029. https://pubmed.ncbi.nlm.nih.gov/16412534/
6. Drug Profile, Bremelanotide – Palatin Technologies. https://adisinsight.springer.com/drugs/800014146
7. Drugs and Supplements, Bremelanotide (subcutaneous route). https://www.mayoclinic.org/drugs-supplements/bremelanotide-subcutaneous-route/description/drg-20466805
8. Pfaus JG, Shadiack A, Van Soest T, Tse M, Molinoff P. Selective facilitation of sexual solicitation in the female rat by a melanocortin receptor agonist. Proc Natl Acad Sci U S A. 2004 Jul 6;101(27):10201-4. doi: 10.1073/pnas.0400491101. Epub 2004 Jun 28. PMID: 15226502 https://pubmed.ncbi.nlm.nih.gov/15226502/
9. Pfaus J, Giuliano F, Gelez H. Bremelanotide: an overview of preclinical CNS effects on female sexual function. J Sex Med. 2007 Nov;4 Suppl 4:269-79. doi: 10.1111/j.1743-6109.2007.00610.x. PMID: 17958619. https://pubmed.ncbi.nlm.nih.gov/17958619/
10. Weinberger JM, Houman J, Caron AT, Patel DN, Baskin AS, Ackerman AL, Eilber KS, Anger JT. Female Sexual Dysfunction and the Placebo Effect: A Meta-analysis. Obstet Gynecol. 2018 Aug;132(2):453-458. doi: 10.1097/AOG.0000000000002733. https://pubmed.ncbi.nlm.nih.gov/29995725/
11. Clayton AH, Lucas J, DeRogatis LR, Jordan R. Phase I Randomized Placebo-controlled, Double-blind Study of the Safety and Tolerability of Bremelanotide Coadministered With Ethanol in Healthy Male and Female Participants. Clin Ther. 2017 Mar;39(3):514-526.e14. doi: 10.1016/j.clinthera.2017.01.018. Epub 2017 Feb 9. https://pubmed.ncbi.nlm.nih.gov/28189361/
12. Althof S, Derogatis LR, Greenberg S, Clayton AH, Jordan R, Lucas J, Spana C. Responder Analyses from a Phase 2b Dose-Ranging Study of Bremelanotide. J Sex Med. 2019 Aug;16(8):1226-1235. doi: 10.1016/j.jsxm.2019.05.012. Epub 2019 Jul 2. https://pubmed.ncbi.nlm.nih.gov/31277966/
13. Kingsberg SA, Clayton AH, Portman D, Williams LA, Krop J, Jordan R, Lucas J, Simon JA. Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder: Two Randomized Phase 3 Trials. Obstet Gynecol. 2019 Nov;134(5):899-908. doi: 10.1097/AOG.0000000000003500. https://pubmed.ncbi.nlm.nih.gov/31599840/
14. Carson, Sandra Ann MD, Boosting Female Sexual Response by RECONNECTing the Dots. Obstet Gynecol. 2019 Nov;134(5):897-898. doi: 10.1097/AOG.0000000000003534. https://journals.lww.com/greenjournal/Citation/2019/11000/
15. DailyMed Vyleesi – Bremelanotide injection. https://dailymed.nlm.nih.gov/dailymed/drugInfo
PT-141 Latest Post
For an overall PT-141 peptide review and its potential healing benefits refer to our recent PT-141 blog post.
NOTE: These products are intended for laboratory research use only. PT-141 peptide for sale is not intended for personal use. Please review our Terms and Conditions before ordering.
Dr. Marinov (MD, Ph.D.) is a researcher and chief assistant professor in Preventative Medicine & Public Health. Prior to his professorship, Dr. Marinov practiced preventative, evidence-based medicine with an emphasis on Nutrition and Dietetics. He is widely published in international peer-reviewed scientific journals and specializes in peptide therapy research.