What is the Origin of PT-141 Melanocortin Agonism?

The term combines the drug's designation, PT-141, with its mechanism of action, "Melanocortin Agonism," where an agonist is a substance that initiates a physiological response when combined with a receptor. PT-141 was initially developed as a sunless tanning agent, but its unexpected side effect of inducing sexual arousal led to its repurposing and subsequent development as a novel treatment for hypoactive sexual desire disorder.

What is the Mechanism of PT-141 Melanocortin Agonism?

PT-141 is administered and travels to the central nervous system where it selectively binds to and activates the MC4R and MC3R. Activation of these receptors is thought to stimulate pro-erectile and pro-sexual signaling pathways in the hypothalamus and other brain regions. This central mechanism enhances the subjective experience of sexual desire and arousal, representing a neuroendocrine intervention that directly addresses the central regulatory component of sexual function.

PT-141 Melanocortin Agonism ∞ Area

PT-141 Melanocortin Agonism

Meaning

PT-141 Melanocortin Agonism refers to the pharmacological action of the synthetic peptide PT-141 (Bremelanotide), which functions as an agonist at specific melanocortin receptors (MCRs), particularly the MC4R and MC3R in the central nervous system. This specific agonism bypasses the vascular system to directly influence neuroendocrine pathways in the brain that regulate sexual arousal and desire. Unlike traditional treatments that affect peripheral blood flow, PT-141 modulates central neural circuits, making it a unique therapeutic approach for treating certain forms of sexual dysfunction in both men and women.