PT-141

Overview

PT-141 (Bremelanotide) is a synthetic cyclic heptapeptide derived from Melanotan II through hydrolysis of the C-terminal amide. The compound has been studied in preclinical and clinical research as a selective MC3R/MC4R melanocortin receptor agonist, with research focus on melanocortin-mediated pathway biology in reproductive research models (Hadley, 2005 — PMID: 15849413).

History

PT-141 was developed in the 1990s through structural modification of Melanotan II, aimed at generating a melanocortin analog with reduced activity at pigmentation-related MC1R while retaining MC3R/MC4R agonist activity. Research has since characterized the compound across multiple pathway domains in reproductive behavior research (Wessells et al., 2000).

Structure & Molecular Data

CAS Number	189691-06-3
Molecular Formula	C₅₀H₆₈N₁₄O₁₀
Molecular Weight	1,025.18 g/mol
Amino Acid Count / Structure	7-amino-acid cyclic heptapeptide
PubChem CID	9941379
Sequence	Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH
Appearance	Lyophilized white powder
Storage	Store at -20°C. Protect from light.
Solubility	Soluble in sterile water and bacteriostatic water

 

Compound Class & Mechanism

PT-141 acts as a selective agonist at MC3R and MC4R melanocortin receptors, with significantly reduced affinity for MC1R compared to Melanotan II. Research has documented central nervous system effects mediated through hypothalamic melanocortin pathway activation in preclinical models.

Unlike phosphodiesterase-5-targeted research compounds, PT-141 operates through a centrally mediated mechanism rather than peripheral vascular pathways. Research has characterized MC4R-mediated signaling in the paraventricular nucleus of the hypothalamus as a key site of activity in preclinical reproductive behavior models (Shadiack et al., 2007).

Research Findings

PT-141 has been investigated in preclinical and clinical research spanning reproductive pathway research, melanocortin receptor pharmacology, and CNS research models. Published research has documented findings in the following domains:

Key Research Areas

• Reproductive Behavior Research: MC3R/MC4R-mediated pathway research in preclinical models
• Melanocortin Receptor Pharmacology: selective MC3R/MC4R binding profile studies
• CNS Pathway Research: hypothalamic pathway research in controlled experimental settings
• Hemorrhagic Shock Research: MC4R-mediated research in preclinical hemorrhagic shock models

Collectively, PT-141 has been established as a distinctive research reference compound for investigating MC3R/MC4R-selective melanocortin pharmacology, particularly in centrally mediated research contexts (Molinoff et al., 2003).

Research Context

Researchers study PT-141 to investigate MC3R/MC4R-selective melanocortin signaling in preclinical models. Its selectivity profile relative to Melanotan II makes it a preferred research tool for investigating receptor-specific pathway contributions to melanocortin-mediated research endpoints.

References

Hadley ME. (2005). Discovery that a melanocortin regulates sexual functions in male and female humans. Peptides. PMID: 15849413

Wessells H. et al. (2000). Melanocortin receptor agonists and male sexual behavior. Peptides.

Shadiack AM. et al. (2007). Melanocortins in the treatment of male and female sexual dysfunction. Current Topics in Medicinal Chemistry.

Molinoff PB. et al. (2003). PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Annals of the New York Academy of Sciences.

Rosen RC. et al. (2004). Bremelanotide for erectile dysfunction. International Journal of Impotence Research.

Diamond LE. et al. (2006). Bremelanotide: melanocortin-based therapy for disorders of female sexual function. Journal of Sexual Medicine.

 

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