PT-141

Product Overview: PT-141 (Bremelanotide)

PT-141 (Bremelanotide) is a synthetic cyclic heptapeptide analog of Alpha-Melanocyte-Stimulating Hormone ($\alpha$-MSH) and an active metabolite of Melanotan 2 (MT-2). Unlike MT-2, PT-141 lacks the C-terminal amide group, which shifts its binding profile to act primarily as a selective agonist at central Melanocortin-3 and Melanocortin-4 receptors (MC3R and MC4R) in the central nervous system. PT-141 serves as a cornerstone research compound for studying neuro-sexual dysfunction, central nervous system-mediated arousal, and hypothalamic melanocortin signaling pathways.

Primary Research Applications & Reasons for Study

• Central MC3R/MC4R Agonism: Activating melanocortin receptors in the medial preoptic area (mPOA) and hypothalamus to stimulate central neural pathways governing sexual desire and motivation.
• Non-Vascular Arousal Pathways: Investigating neurogenic erectile responses and sexual motivation mechanisms that operate independently of peripheral vasodilation (PDE5 inhibitor pathways).
• Female Hypoactive Sexual Desire Models: Evaluating central neurotransmitter shifts (dopamine and norepinephrine release) in premenopausal models of hypoactive sexual desire disorder (HSDD).
• Hemorrhagic Shock & Ischemia Defense: Studying secondary peripheral MC3R/MC4R-mediated anti-inflammatory and cardiovascular stabilization responses in acute ischemia-reperfusion models.

Expected Research Results & Timeline Metrics

• Phase 1 / Minutes 30–120
  Hypothalamic Receptor Binding & Dopamine Shift: Rapid crossing of the blood-brain barrier leading to central MC4R binding, accompanied by localized dopamine release in the medial preoptic area.
• Phase 2 / Hours 2–6
  Peak Central Arousal Response: Statistically significant increases in solicitation behaviors, lordosis quotient metrics, and intracavernosal pressure (ICP) readouts in experimental models.
• Phase 3 / Hours 6–12+
  Gradual Receptor Clearance: Progressive decline in central melanocortin signaling with a return to baseline neurotransmitter levels and low residual binding activity.

Key Research Benefits

• Central Mechanism of Action: Operates directly on brain neural circuits rather than targeting peripheral vascular muscle tissue.
• Reduced Pigmentary Activity: Demonstrates significantly lower MC1R binding affinity compared to Melanotan 2, minimizing melanogenesis (skin tanning) during trials.
• Cross-Gender Efficacy Model: Serves as an effective, dual-sex research peptide for investigating both male and female central arousal dysfunction.
• Selective Melanocortin Standard: Gold-standard reference compound for studying MC3R/MC4R signaling pathways in neurobiology and behavioral endocrinology.