PT-141 (bremelanotide), a synthetic cyclic heptapeptide analog of α-melanocyte-stimulating hormone, functions as a non-selective melanocortin receptor agonist with primary activity at MC3R and MC4R in the central nervous system, particularly within hypothalamic regions governing sexual motivation, arousal, and appetitive behaviors. In preclinical models, including rodents and nonhuman primates, PT-141 elicits robust erectogenic responses in males and selectively enhances solicitational and pre-copulatory behaviors in females, demonstrating its ability to activate central neural pathways that promote sexual desire and function independent of peripheral vascular mechanisms. These effects arise from modulation of neurotransmitter systems, such as increased dopamine release in key brain areas, positioning PT-141 as a valuable investigational tool for exploring the neurobiology of sexual dysfunction in both sexes, including hypoactive sexual desire disorder, erectile dysfunction (including in non-responders to PDE5 inhibitors), and related conditions where central melanocortinergic signaling is implicated. Broader research applications include its potential role in appetite regulation and energy balance via MC4R agonism, as well as emerging inquiries into cognitive modulation, mood, and stress resilience through melanocortin pathway interactions, highlighting its utility in advancing understanding of CNS-mediated behaviors and potential therapeutic targets beyond traditional sexual health paradigms.