PT-141, known clinically as Bremelanotide, is a synthetic peptide drug acting as a potent agonist of the melanocortin receptors, specifically MC3R and MC4R, within the central nervous system. Unlike peripheral vasoactive agents, PT-141 is a neuromodulator that addresses sexual dysfunction by activating central pathways, leading to increased sexual desire and arousal in both men and women. It is a targeted therapeutic agent for hypoactive sexual desire disorder.
Origin
PT-141 is a derivative of the naturally occurring peptide hormone alpha-Melanocyte-Stimulating Hormone (α-MSH). The development of this compound stemmed from research into the melanocortin system, a key regulator of appetite, metabolism, and sexual function in the hypothalamus. The peptide was strategically modified to selectively target the central melanocortin receptors responsible for arousal.
Mechanism
The mechanism is centralized and neuroendocrine. Following administration, PT-141 crosses the blood-brain barrier and binds to the MC4R in specific brain regions, notably the paraventricular nucleus of the hypothalamus. Activation of this receptor initiates a downstream signaling cascade that ultimately modulates the activity of neural circuits involved in sexual motivation and response. This action bypasses peripheral vascular mechanisms, focusing instead on the core neurochemical drivers of sexual desire and arousal.
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