PT-141

Research Applications of PT-141 (Bremelanotide)

1. Neuroendocrine and Central Nervous System Research

PT-141 is a melanocortin receptor agonist that primarily targets the MC3R and MC4R receptors within the central nervous system [1]. These receptors are implicated in various neuroendocrine and autonomic processes, including stress response, energy balance, and behavior regulation [2].

Research studies using PT-141 explore G-protein-coupled receptor (GPCR) activation and downstream effects on intracellular signaling. Investigations have demonstrated its influence on hypothalamic neuronal activity, cAMP accumulation, and modulation of dopaminergic and serotonergic pathways [3]. This makes PT-141 an important tool in understanding CNS-mediated behavioral responses and neuromodulation in animal models.

2. Melanocortin Receptor and Peptide Signaling Studies

As a cyclic heptapeptide, PT-141’s structural stability allows precise receptor-specific binding studies, distinguishing it from its parent peptide Melanotan II [4]. Researchers use PT-141 to examine melanocortin receptor subtype selectivity, ligand binding kinetics, and receptor desensitization or internalization mechanisms [5].

Studies have also highlighted its role in exploring structure-activity relationships (SAR) within the melanocortin system, helping to design future analogs for neuropeptide receptor research [6].

3. Metabolic and Energy Homeostasis Research

The melanocortin system plays a major role in regulating food intake, metabolism, and energy expenditure [7]. By activating MC4R receptors in hypothalamic nuclei, PT-141 serves as a model compound in animal studies to understand energy balance regulation and sympathetic nervous system activation [8]. These studies contribute to understanding mechanisms underlying obesity, metabolic disorders, and appetite control from a biochemical perspective.

4. Behavioral Neuroscience and Neurochemical Pathways

PT-141’s effects on behavioral and reward pathways are also under investigation. In rodent models, it has been used to map neural circuits related to motivation and social behaviors through techniques like c-Fos expression mapping and microdialysis [9].

By influencing neurotransmitter systems—particularly dopamine and oxytocin signaling—PT-141 aids in identifying the interaction between neuropeptides and monoamine neurotransmitters [10].

Referenced Citations:

1. https://pubchem.ncbi.nlm.nih.gov/compound/PT-141 (PubChem)
2. Hruby, V. J., et al. “Design of novel melanocortin receptor selective agonists.” Peptides, 2000. PubMed
3. Wessells, H., et al. “Melanocortin receptor agonists in CNS signaling.” Endocrinology, 2003. PubMed
4. Hadley, M. E., et al. “Melanocortin peptides and their physiological roles.” Physiol Rev., 2006. PubMed
5. Tatro, J. B. “Receptor signaling mechanisms of melanocortin peptides.” Ann N Y Acad Sci., 1999. PubMed
6. Holder, J. R., et al. “Structure-activity relationships in melanocortin receptor ligands.” J Med Chem., 2002. PubMed
7. Cone, R. D. “The central melanocortin system and energy homeostasis.” Trends Endocrinol Metab., 2005. PubMed
8. Mountjoy, K. G. “Functions of the melanocortin system in energy regulation.” Eur J Pharmacol., 2010. PubMed
9. Pfaus, J. G., et al. “Neurochemical mapping of melanocortin-induced behaviors.” Neuroscience, 2007. PubMed
10. Yang, Y., et al. “Interactions of melanocortins with dopaminergic systems.” J Neurosci., 2009. PubMed