PT-141 (Bremelanotide) is a cyclic heptapeptide derived from Melanotan II, and is a non-selective melanocortin receptor agonist with significant affinity for MC1R, MC3R, MC4R, and MC5R. It was approved by the FDA in 2019 under the brand name Vyleesi for a specific clinical indication.
MC4R Central Nervous System Research
Preclinical research has extensively examined PT-141's interactions with MC4R in hypothalamic and limbic system nuclei, which have been linked to autonomic nervous system regulation and energy balance signaling in rodent models.
Receptor Selectivity and Pharmacology Research
Research has characterized PT-141's binding affinity profile across the melanocortin receptor family and its activation of downstream cAMP signaling and beta-arrestin recruitment in preclinical cell-based models.
Clinical Development Research Background
PT-141's progression through clinical development has generated substantial Phase 1, 2, and 3 clinical research data examining its pharmacokinetics and receptor engagement biomarkers in human subjects, distinguishing it from many research peptides that remain exclusively in preclinical investigation.
• Molinoff PB et al. (2003). PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Annals of the New York Academy of Sciences, 994, 96–102.
