PT-141: Safety Profile & Research Summary
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Comprar péptido PT-141 10mg (Bremelanotide)Research Summary
Foundational and Mechanistic Studies
| Study | Type | Subject of Report | Ref |
|---|---|---|---|
| Molinoff et al. (2003) | Compound characterization | Original description of PT-141 as a melanocortin agonist | [1] |
| Van der Ploeg et al. (2002) | Receptor genetics / pharmacology | Identification of an MC4R role in centrally mediated melanocortin pharmacology | [3] |
| Hadley & Dorr (2006) | Historical review | Melanocortin peptide development programme and its milestones | [2] |
| Zhang et al. (2021) | Structural biology (cryo-EM) | Ligand recognition and activation mechanism at MC4R | [4] |
| Pfaus et al. (2004) | Preclinical (rodent) | Behavioural pharmacology of a melanocortin receptor agonist in the female rat | [8] |
| Borland et al. (2025) | Preclinical (hamster) | Analyses of the compound in a female Syrian hamster model | [19] |
| Suzuki et al. (2024) | In vitro (oncology) | Cell death and growth inhibition in glioblastoma cells via survivin suppression | [18] |
| White et al. (2017) | Clinical pharmacology | Ambulatory blood-pressure monitoring applied to a melanocortin receptor agonist | [14] |
Analytical and Material-Identity Studies
| Study | Method | Subject of Report | Ref |
|---|---|---|---|
| Sauter et al. (2020) | UHPLC-MS/MS | Ultra-sensitive quantification of the cyclic peptide | [15] |
| Yuvaraaj & Sharma (2026) | LC-HRMS/MS + modelling | Characterization of bremelanotide acetate and its degradants; epimerization prediction | [16] |
| Mestria et al. (2021) | LC-HRMS | Characterization of melanotan II and bremelanotide material sold outside regulated supply chains | [17] |
Mechanistic Themes
- Non-selective melanocortin agonism — engages multiple receptor subtypes rather than one, which is why selective antagonists are co-applied in subtype-resolution experiments
- Conformationally constrained scaffold — a lactam bridge and D-amino acid substitution stabilize the bioactive turn and resist proteolysis
- Gαs / cAMP coupling — with reported calcium mobilization and β-arrestin-dependent receptor internalization
- Central localization — c-Fos mapping identifies hypothalamic sites of engagement in animal models
- Pharmacologically confined — no significant reported affinity across the classical neurotransmitter receptor panel
Literature Integrity
The published record for this compound contains flagged items. One randomized trial was subsequently retracted, and a further study by the same author group carries a formal Expression of Concern issued by The Journal of Urology.[23] A published re-analysis of the phase 3 programme contests the magnitude of the originally reported effects.[22] Neither the retracted study nor the study under Expression of Concern is relied upon as evidence anywhere on this page; the Expression of Concern is cited so that investigators can locate it directly.
The products offered on this website are furnished for in-vitro studies only. In-vitro studies (Latin: in glass) are performed outside of the body. These products are not medicines or drugs and have not been approved by the FDA to prevent, treat or cure any medical condition, ailment or disease. Bodily introduction of any kind into humans or animals is strictly forbidden by law.
For Laboratory Research Only. Not for human use, medical use, diagnostic use, or veterinary use.
ALL ARTICLES AND PRODUCT INFORMATION PROVIDED ON THIS WEBSITE ARE FOR INFORMATIONAL AND EDUCATIONAL PURPOSES ONLY.
“Research Summary Foundational and Mechanistic Studies StudyTypeSubject of ReportRef Molinoff et al.”
Referencias
- Molinoff PB, Shadiack AM, Earle D, Diamond LE, Quon CY. Ann N Y Acad Sci. 2003;994:96-102.
- Hadley ME, Dorr RT. Peptides. 2006;27(4):921-930.
- Van der Ploeg LH, Martin WJ, Howard AD, et al. 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. Nat Rev Endocrinol. 2023;19(9):507-519.
- Giuliano F. J Androl. 2004;25(5):683-691.
- Pfaus JG, Shadiack A, Van Soest T, Tse M, Molinoff P. Proc Natl Acad Sci U S A. 2004;101(27):10201-10204.
- Pfaus J, Giuliano F, Gelez H. J Sex Med. 2007;4 Suppl 4:269-279.
- Shadiack AM, Sharma SD, Earle DC, Spana C, Hallam TJ. Curr Top Med Chem. 2007;7(11):1137-1144.
- Shadiack AM, Althof S. Int J Impot Res. 2008;20 Suppl 1:S11-S16.
- Pfaus JG, Sadiq A, Spana C, Clayton AH. CNS Spectr. 2022;27(3):281-289.
- Dhillon S, Keam SJ. 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. 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. 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. Neuropharmacology. 2025;267:110299.
- Merlino F, Jia L, Boccino I, et al. 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. J Sex Res. 2021;58(9):1085-1105.
- 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
Related research
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Este contenido se proporciona solo para fines educativos e informativos. Los productos se suministran exclusivamente para estudios in vitro y no son medicamentos, fármacos ni suplementos. No están aprobados por la FDA para prevenir, tratar o curar ninguna condición.
