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

How does PT-141 work? What is its mechanism of action?

Reported Mechanism 1. Melanocortin Receptor Engagement Bremelanotide is described as a non-selective agonist across the melanocortin receptor family — MC1R, MC3R, MC4R and MC5R — all members of the rhodopsin-like (class A) GPCR superfamily.[1][5] Reported potency is graded rather than subtype-selective, which is the property that makes the compound useful as a broad-spectrum reference ligand and, equally, the property that requires selective antagonists to be co-applied when a single subtype is

What are the research applications of PT-141?

Research Applications Published investigations involving bremelanotide fall into the following areas of laboratory and clinical research. These describe the subject matter of the published record and are not statements of effect. Melanocortin receptor pharmacology — Molinoff et al. published the original characterization of the compound as a melanocortin agonist, and Yuan and Tao reviewed the broader ligand landscape for these receptors.[1][5] MC4R structural biology — Zhang et al. resolved liga

What does the research summary say about PT-141?

Research Summary Foundational and Mechanistic Studies StudyTypeSubject of ReportRef Molinoff et al. (2003)Compound characterizationOriginal description of PT-141 as a melanocortin agonist[1] Van der Ploeg et al. (2002)Receptor genetics / pharmacologyIdentification of an MC4R role in centrally mediated melanocortin pharmacology[3] Hadley & Dorr (2006)Historical reviewMelanocortin peptide development programme and its milestones[2] Zhang et al. (2021)Structural biology (cryo-EM)Ligand recognit

How should PT-141 be stored?

Store lyophilized PT-141 desiccated at -20°C for long-term stability, protected from light. After reconstitution, store at 2-8°C and avoid repeated freeze-thaw cycles.

PT-141: Safety Profile & Research Summary

24 Citacoes PubMedRevisado por EspecialistasCertificado GMPUltima Revisao: julho de 2026

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.

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Editorial Research Note

“Research Summary Foundational and Mechanistic Studies StudyTypeSubject of ReportRef Molinoff et al.”

Pure U.S. Peptides Research Standards TeamInternal editorial group summarising published peptide research for an audience of qualified independent investigators.

Referencias

Perguntas de Pesquisa Relacionadas

→ What Is PT-141?→ PT-141: Mechanism of Action → PT-141: Research Applications → PT-141: Chemical Properties → Storing PT-141: Best Practices

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