PT-141

Molecular Information

Research Summary

PT-141 is a synthetic melanocortin receptor agonist derived from the peptide Melanotan II. Unlike PDE5 inhibitors that act on vascular mechanisms, PT-141 acts centrally on melanocortin receptors (MC3R and MC4R) in the brain. Research in animal models has demonstrated its ability to activate these receptor pathways, which are involved in various physiological processes including energy homeostasis and reproductive behavior. The peptide has been extensively studied in preclinical models to understand melanocortin signaling pathways.

Mechanism of Action

PT-141 acts as an agonist at melanocortin receptors MC3R and MC4R in the central nervous system. These receptors are G protein-coupled receptors that activate intracellular signaling cascades involving cyclic AMP. Research in animal models has demonstrated that activation of these pathways modulates dopaminergic and oxytocinergic signaling in hypothalamic regions.

Published Animal Studies

• [1]Studies in rodent models demonstrated activation of melanocortin receptor pathways with measurable behavioral and physiological changes (Pfaus et al., 2004)
• [2]Research in rat models showed central nervous system-mediated effects through MC4R activation (Martin et al., 2002)
• [3]Primate studies demonstrated dose-dependent effects on melanocortin signaling with good receptor selectivity (Molinoff et al., 2003)

In-Vitro Research

• •Receptor binding assays confirmed high affinity for MC3R and MC4R with measurable EC50 values
• •Cell-based reporter assays demonstrated functional agonism at melanocortin receptors
• •Selectivity studies showed preferential activation of MC4R over other melanocortin receptor subtypes

Research Applications

References

1. 1.Pfaus JG, et al. "A role for melanocortins in the modulation of sexual activity." Ann N Y Acad Sci. 2004;1025:69-79.
2. 2.Molinoff PB, et al. "PT-141: A melanocortin agonist for the treatment of sexual dysfunction." Ann N Y Acad Sci. 2003;994:96-102.