What Is PT-141?
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Overview PT-141 is the catalog designation for bremelanotide, a synthetic cyclic heptapeptide lactam described in the peer-reviewed literature as a non-selective agonist at the melanocortin receptor family.[1] Molinoff and colleagues published the original characterization of the compound as a melan...
Overview
PT-141 is the catalog designation for bremelanotide, a synthetic cyclic heptapeptide lactam described in the peer-reviewed literature as a non-selective agonist at the melanocortin receptor family.[1] Molinoff and colleagues published the original characterization of the compound as a melanocortin agonist in Annals of the New York Academy of Sciences.[1]
The molecule derives from the melanotropin structure-activity programme conducted at the University of Arizona, reviewed by Hadley and Dorr, which produced a series of superpotent α-MSH analogues including Melanotan II.[2] Bremelanotide is the deaminated derivative of that parent compound, carrying a C-terminal free acid where Melanotan II carries an amide — a single terminal change that alters the receptor-engagement profile while retaining the cyclic scaffold.[1][2]
Why the compound appears in the literature
Melanocortin receptors are a five-member family of class A G-protein-coupled receptors with distinct tissue distributions. Because bremelanotide engages several of these subtypes rather than one, it is used in receptor pharmacology as a non-selective tool ligand — typically alongside subtype-selective antagonists — to separate the contributions of individual melanocortin receptors in a given model system.[5][7] Van der Ploeg et al. established MC4R as the receptor subtype of interest for centrally mediated melanocortin pharmacology, and Cone and colleagues have reviewed the central melanocortin system in energy homeostasis.[3][6]
Regulatory status, reported factually
A pharmaceutical formulation of bremelanotide received U.S. FDA approval in 2019; Dhillon and Keam summarized that approval in Drugs.[13] That approval attaches to a specific manufactured pharmaceutical product under defined clinical conditions. The research-grade material supplied here is not that product, and nothing on this page describes or implies a clinical use for it.
A note on the published record
Investigators working with this compound should be aware that the bremelanotide clinical literature contains flagged records. One randomized trial of the compound was subsequently retracted, and a second study by the same author group carries a formal Expression of Concern issued by The Journal of Urology in 2023.[23] Separately, Spielmans published a re-analysis of the phase 3 programme contesting the magnitude of the reported effects.[22] Neither retracted nor Expression-of-Concern-flagged studies are cited as evidence anywhere on this page.
Research framework
Within the melanocortin research domain, PT-141 is most directly compared with Melanotan II for the amide-versus-free-acid terminal distinction and with KPV for the receptor-engagement versus PepT1-uptake distinction. The compound is supplied here strictly as a research reference standard for in vitro and animal-model investigation, and is not intended for human or veterinary use.
“Research Summary Foundational and Mechanistic Studies StudyTypeSubject of ReportRef Molinoff et al.”
Referencias
- 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;994:96-102.
- Hadley ME, Dorr RT. Melanocortin peptide therapeutics: historical milestones, clinical studies and commercialization. Peptides. 2006;27(4):921-930.
- Van der Ploeg LH, Martin WJ, Howard AD, et al. A role for the melanocortin 4 receptor in sexual function. Proc Natl Acad Sci U S A. 2002;99(17):11381-11386.
- Zhang H, Chen LN, Yang D, et al. Structural insights into ligand recognition and activation of the melanocortin-4 receptor. Cell Res. 2021;31(11):1163-1175.
- Yuan XC, Tao YX. Ligands for Melanocortin Receptors: Beyond Melanocyte-Stimulating Hormones and Adrenocorticotropin. Biomolecules. 2022;12(10):1407.
- Sweeney P, Gimenez LE, Hernandez CC, Cone RD. Targeting the central melanocortin system for the treatment of metabolic disorders. Nat Rev Endocrinol. 2023;19(9):507-519.
- Giuliano F. Control of penile erection by the melanocortinergic system: experimental evidences and therapeutic perspectives. J Androl. 2004;25(5):683-691.
- 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;101(27):10201-10204.
- Pfaus J, Giuliano F, Gelez H. Bremelanotide: an overview of preclinical CNS effects on female sexual function. J Sex Med. 2007;4 Suppl 4:269-279.
- Shadiack AM, Sharma SD, Earle DC, Spana C, Hallam TJ. Melanocortins in the treatment of male and female sexual dysfunction. Curr Top Med Chem. 2007;7(11):1137-1144.
- Shadiack AM, Althof S. Preclinical effects of melanocortins in male sexual dysfunction. Int J Impot Res. 2008;20 Suppl 1:S11-S16.
- Pfaus JG, Sadiq A, Spana C, Clayton AH. The neurobiology of bremelanotide for the treatment of hypoactive sexual desire disorder in premenopausal women. CNS Spectr. 2022;27(3):281-289.
- Dhillon S, Keam SJ. Bremelanotide: First Approval. Drugs. 2019;79(14):1599-1606.
- White WB, Myers MG, Jordan R, Lucas J. Usefulness of ambulatory blood pressure monitoring to assess the melanocortin receptor agonist bremelanotide. J Hypertens. 2017;35(4):761-768.
- Sauter M, Uhl P, Burhenne J, Haefeli WE. Ultra-sensitive quantification of the therapeutic cyclic peptide bremelanotide utilizing UHPLC-MS/MS for evaluation of its oral plasma pharmacokinetics. J Pharm Biomed Anal. 2020;186:113276.
- Yuvaraaj VK, Sharma N. Comprehensive characterization of bremelanotide acetate and its degradants by LC-HRMS/MS and predicting epimerization through computational modelling. Anal Methods. 2026.
- Mestria S, Odoardi S, Frison G, Strano Rossi S. LC-HRMS characterization of the skin pigmentation and sexual enhancers melanotan II and bremelanotide sold on the black market of performance and image enhancing drugs. Drug Test Anal. 2021;13(4):876-882.
- Suzuki S, Kitanaka C, Okada M. Melanocortin Receptor Agonist Bremelanotide Induces Cell Death and Growth Inhibition in Glioblastoma Cells via Suppression of Survivin Expression. Anticancer Res. 2024;44(9):3875-3883.
- Borland JM, Kohut-Jackson AL, Peyla AC, Hall MA, Mermelstein PG, Meisel RL. Female Syrian hamster analyses of bremelanotide, a US FDA approved drug for the treatment of female hypoactive sexual desire disorder. Neuropharmacology. 2025;267:110299.
- Merlino F, Jia L, Boccino I, et al. Goldilocks-Inspired Design of Mid-Size Macrocycles for Selective Targeting of Human Melanocortin Receptors. J Med Chem. 2026.
- Bardhan M, Anand A, Javed A, et al. Polymorphism of Melanocortin Receptor Genes-Association with Inflammatory Traits and Diseases. Diseases. 2025;13(9):305.
- Spielmans GI. Re-Analyzing Phase III Bremelanotide Trials for “Hypoactive Sexual Desire Disorder” in Women. J Sex Res. 2021;58(9):1085-1105.
- Expression of Concern: Salvage of Sildenafil Failures With Bremelanotide: A Randomized, Double-Blind, Placebo Controlled Study. J Urol. 2023 Jan 10.
- National Center for Biotechnology Information. PubChem Compound Summary for CID 9941379, Bremelanotide. PubChem. Accessed 2026-07-31.
Preguntas de Investigación Relacionadas
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