Mechanism of Action of PT-141 (Bremelanotide)
PT-141 works by activating melanocortin receptors (MC1R and MC4R) in the hypothalamus, a brain region responsible for regulating sexual behavior and arousal. Unlike PDE5 inhibitors (such as Viagra), which improve blood flow to the genitals, PT-141 directly influences the central nervous system (CNS) to enhance sexual desire.
Step-by-Step Action:
1. Melanocortin Receptor Activation
- PT-141 binds to MC4R receptors in the brain, which are linked to sexual function and arousal.
- This receptor activation triggers neurotransmitter release, leading to increased sexual desire and motivation.
2. Dopamine Release
- PT-141 stimulates dopamine, the "pleasure and reward" neurotransmitter, which plays a crucial role in sexual excitement and mood enhancement.
3. Enhanced Neural Signaling for Sexual Response
- The increased dopamine activity leads to heightened arousal, improved sexual satisfaction, and stronger sexual response in both men and women.
- Unlike PDE5 inhibitors, which primarily work on vascular function, PT-141's effects are neurological, meaning it works even for individuals with normal blood flow but low libido.
4. Increased Blood Flow as a Secondary Effect
- While PT-141 does not directly act as a vasodilator, its activation of the CNS indirectly improves blood flow, making it beneficial for men with erectile dysfunction (ED) and women with reduced sensitivity or arousal issues.
5. Why Is PT-141 Unique?
- Works for Both Men & Women (unlike Viagra, which is mainly for men)
- Does Not Depend on Blood Flow, making it effective for non-vascular causes of sexual dysfunction
- Long-Lasting Effects (can last 24-48 hours)