PT-141, also known as bremelanotide, is a synthetic melanocortin peptide previously investigated in human clinical research for female hypoactive sexual desire disorder (HSDD). PT-141 is primarily associated with melanocortin receptor signaling, with activity discussed most often in relation to melanocortin-4 receptor (MC4R) and melanocortin-1 receptor (MC1R). PT-141 is a derivative of another synthetic melanocortin, melanotan 2 (MT-2), and has also been explored in research contexts beyond sexual function, including investigations related to acute hemorrhage.

Source: PubChem

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 and Sexual Arousal

PT-141 has been studied for its relationship to central nervous system pathways involved in sexual behavior, with particular attention to MC4R signaling^{[1], [2]}. Preclinical studies in animal models have reported sexual behavior and arousal effects associated with melanocortin receptor agonism^{[3], [4]}. Because this pathway differs from PDE5 inhibitors (e.g., sildenafil), PT-141 has been investigated as a way to explore sexual dysfunction where vascular mechanisms are not the primary driver.

A study in men with erectile dysfunction who did not respond to sildenafil reported that a subset achieved erections adequate for intercourse after PT-141 exposure (nasal administration), with dose-dependent effects noted in that trial^[5].

Duration of penile base rigidity greater than 60% for placebo compared to various doses of PT-141.
Source: Nature

PT-141 was discussed in the context of female sexual dysfunction research and clinical development, including randomized dose-finding work in premenopausal women and commentary on trial endpoints and clinical assessment approaches^{[6], [7]}. Later-stage development efforts and licensing announcements also contributed to renewed attention toward subcutaneous formulations and trial designs^[8].

PT-141 and Hemorrhage

PT-141 analogs have been investigated for potential utility in hemorrhagic shock research, leveraging melanocortin receptor pathways (including MC1R and MC4R) that may influence ischemia-related tissue effects in hypovolemic settings. A modified variant referenced in this context has been described as PL-6983.

PT-141 and Infection

MC1R signaling has also been explored in inflammatory and infectious disease models. In a rat model of Candida albicans vaginitis, a synthetic melanocortin (CKPV)₂ was studied for anti-fungal and anti-inflammatory effects associated with macrophage polarization pathways^[9]. This line of research reflects broader interest in melanocortin pathways as adjunct targets for infection and inflammation biology.

PT-141 and Cancer / Photoprotection Pathways

MC1R is closely linked to pigmentation biology and is also discussed in relation to DNA repair and photoprotection signaling pathways, which can be relevant to skin cancer risk and prevention research^[10]. Variants of MC1R have been associated with increased risk for certain skin cancers, which has motivated ongoing interest in melanocortin signaling in dermatologic oncology contexts^[11].

PT-141 has received extensive attention in research related to sexual dysfunction and neurobehavioral signaling. Beyond that area, melanocortin receptor biology creates additional experimental avenues. For example, MC4R dysfunction has been associated with certain forms of early-onset obesity, and PT-141 offers a receptor-agonist framework for studying melanocortin signaling in energy balance pathways. MC1R signaling has also been discussed in relation to pain, inflammation, kidney pathology, host response, and other immune-adjacent mechanisms. These pathways represent broad areas where melanocortin agonists can be used as investigative tools.

PT-141 exhibits minimal side effects, low oral and excellent subcutaneous bioavailability in mice. Per kg dosage in mice does not scale to humans. PT-141 is limited to educational and scientific research only, not for human consumption. Only buy PT-141 if you are a licensed researcher.

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.

Dr. Sheryl A. Kingsberg is the chief of behavioral medicine at University Hospitals Case Medical Center and a professor in Reproductive Biology and Psychiatry at Case Western Reserve University. Her clinical and research focus includes sexual medicine, female sexual disorders, cognitive behavioral psychotherapy, menopause, pregnancy and postpartum mood disorders, psychological aspects of infertility, and sexuality-related quality of life. She led a randomized, placebo-controlled dose-finding trial evaluating bremelanotide (PT-141) in premenopausal women.

Dr. Sheryl A. Kingsberg is referenced here to acknowledge published research related to PT-141. This reference does not imply endorsement or advocacy of purchase, sale, or use of this product. No affiliation or relationship is implied between Peptide Sciences and this scientist. Dr. Kingsberg is listed in the citations below.

1. M. Sandrock, A. Schulz, C. Merkwitz, T. Schöneberg, K. Spanel-Borowski, and A. Ricken, “Reduction in corpora lutea number in obese melanocortin-4-receptor-deficient mice,” Reprod. Biol. Endocrinol., vol. 7, p. 24, Mar. 2009.
2. R. C. Rosen, L. E. Diamond, D. C. Earle, A. M. Shadiack, and P. B. Molinoff, “Evaluation of the safety, pharmacokinetics and pharmacodynamic effects of subcutaneously administered PT-141…,” Int. J. Impot. Res., vol. 16, no. 2, pp. 135–142, Apr. 2004.
3. H. Wessells, V. J. Hruby, J. Hackett, G. Han, P. Balse-Srinivasan, and T. W. Vanderah, “Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2 induces penile erection…,” Neuroscience, vol. 118, no. 3, pp. 755–762, 2003.
4. A.-S. Rössler, J. G. Pfaus, H. K. Kia, J. Bernabé, L. Alexandre, and F. Giuliano, “The melanocortin agonist, melanotan II, enhances proceptive sexual behaviors…,” Pharmacol. Biochem. Behav., vol. 85, no. 3, pp. 514–521, Nov. 2006.
5. M. R. Safarinejad and S. Y. Hosseini, “Salvage of sildenafil failures with bremelanotide…,” J. Urol., vol. 179, no. 3, pp. 1066–1071, Mar. 2008.
6. A. H. Clayton et al., “Bremelanotide for female sexual dysfunctions in premenopausal women…,” Womens Health (Lond), vol. 12, no. 3, pp. 325–337, 2016.
7. M. K. Miller, J. R. Smith, J. J. Norman, and A. H. Clayton, “Expert opinion on existing and developing drugs to treat female sexual dysfunction,” Expert Opin. Emerg. Drugs, vol. 23, no. 3, pp. 223–230, 2018.
8. “AMAG Pharmaceuticals and Palatin Technologies Enter Into Exclusive Licensing Agreement for North American Rights to Rekynda™ (bremelanotide)…” MarketWatch, 09-Jan-2017.
9. H. Ji et al., “The Synthetic Melanocortin (CKPV)2 Exerts Anti-Fungal and Anti-Inflammatory Effects…,” PLOS ONE, vol. 8, no. 2, Feb. 2013.
10. V. Maresca, E. Flori, and M. Picardo, “Skin phototype: a new perspective,” Pigment Cell Melanoma Res., vol. 28, no. 4, pp. 378–389, Jul. 2015.
11. L. Feller, R. a. G. Khammissa, B. Kramer, M. Altini, and J. Lemmer, “Basal cell carcinoma, squamous cell carcinoma and melanoma of the head and face,” Head Face Med., vol. 12, p. 11, Feb. 2016.
12. Clayton AH, Althof SE, Kingsberg S, et al. “Bremelanotide for female sexual dysfunctions in premenopausal women: a randomized, placebo-controlled dose-finding trial.” Womens Health (Lond). 2016;12(3):325–337. doi:10.2217/whe-2016-0018
13. T. R. McMillan et al., “Melanotan II… partially rescues the impaired thermogenic capacity…,” Exp. Physiol., vol. 106, no. 2, pp. 427–437, Feb. 2021.
14. C. Spana, R. Jordan, and S. Fischkoff, “Effect of bremelanotide on body weight of obese women…,” Diabetes Obes. Metab., vol. 24, no. 6, pp. 1084–1093, Jun. 2022.

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