PT-141 — 10mg
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PT‑141 (Bremelanotide) is a selective melanocortin receptor agonist targeting central receptor subtypes (MC3 & MC4), frequently utilized in neuroscience and receptor signaling research.
MELANOCORTIN RECEPTOR AGONIST
Central Arousal Signaling: Where Viagra Cannot Reach
PT-141 (Bremelanotide) is a synthetic cyclic heptapeptide derived from α-MSH that activates melanocortin receptors MC4R and MC1R in the central nervous system. Unlike PDE5 inhibitors (Viagra, Cialis) which work peripherally on blood flow, PT-141 acts directly on hypothalamic arousal circuits — addressing desire at its neurological source. Two Phase 3 RECONNECT trials demonstrated statistically significant improvements in both desire and distress scores, leading to FDA approval in 2019 for hypoactive sexual desire disorder (HSDD).
- Cyclic heptapeptide: Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH₂
- Activates MC4R (central arousal) and MC1R (immune/repair)
- Works via CNS pathways — not peripheral blood flow
- Effective in sildenafil non-responders (~33% success rate)
- FDA-approved in 2019 for HSDD (marketed as Vyleesi)
For laboratory research use only. Not for human consumption.
MC4R PATHWAY RESEARCH
How PT-141 Activates Desire and Autonomic Arousal
PT-141 binds to melanocortin-4 receptors (MC4R) in the medial preoptic area (mPOA) of the hypothalamus, leading to increased release of dopamine — an excitatory neurotransmitter that enhances sexual desire. This receptor system is distinct from the vascular mechanisms targeted by traditional ED medications. In animal models, MC4R activation produces sexual arousal and increased copulation in both males and females. Research also indicates PT-141 influences oxytocinergic pathways at hypothalamic and spinal levels.
- MC4R: Hypothalamic sexual arousal and desire pathways
- Increases dopamine release in reward-related circuits
- Autonomic arousal independent of vascular effects
- Activates neurons in paraventricular nucleus (c-Fos expression)
- Interacts with oxytocinergic pathways for arousal
For laboratory research use only. Not for human consumption.
EXPANDING RESEARCH APPLICATIONS
From Sexual Function to Obesity and Energy Homeostasis
Beyond sexual function, PT-141 research extends into metabolic and immune territories. The MC4R pathway is heavily involved in appetite and energy balance — defective or missing MC4R accounts for approximately 6% of all cases of early-onset obesity. In the hypothalamus, α-MSH suppresses appetite via MC4R, making melanocortin agonists relevant to obesity research. MC1R’s role in immune modulation and DNA repair pathways makes PT-141 derivatives relevant to inflammation and cancer prevention research.
- Sexual dysfunction: Both male and female HSDD research
- Obesity: MC4R defects implicated in ~6% of early-onset cases
- Energy homeostasis: Appetite suppression via hypothalamic circuits
- Immune modulation: MC1R-mediated anti-inflammatory effects
- Cancer research: MC1R stimulates DNA repair pathways
For laboratory research use only. Not for human consumption.
The Science Behind Central Arousal: Why PT-141 Opens New Research Frontiers
PT-141 (Bremelanotide) represents a paradigm shift in sexual function research. As a synthetic cyclic heptapeptide derived from Melanotan II, it activates melanocortin receptors in the central nervous system rather than working peripherally on blood flow. This fundamental difference explains why PT-141 can help subjects who don’t respond to PDE5 inhibitors like sildenafil — it addresses desire at the neurological level, not just the vascular mechanics of arousal.
The clinical evidence is substantial. Two Phase 3 RECONNECT trials involving 1,267 premenopausal women demonstrated statistically significant improvements in both desire and distress scores. From baseline to end-of-study, women taking bremelanotide showed significant increases in sexual desire (P<0.001 in both studies) with effect sizes of 0.39 for desire and 0.27 for distress reduction. This led to FDA approval in June 2019 (marketed as Vyleesi) — making it the first on-demand pharmacologic option for HSDD in premenopausal women.
The melanocortin receptor system extends far beyond sexual function. MC4R is predominantly expressed in the medial preoptic area (mPOA) of the hypothalamus and is critical for regulating appetite, energy balance, and autonomic function. Animal studies suggest PT-141 activates presynaptic MC4Rs, leading to increased dopamine release in circuits that govern sexual desire. In rats, intranasal PT-141 produced significant increases in spontaneous erections, with immunostaining showing increased c-Fos expression in the paraventricular nucleus.
For research teams investigating sexual function, obesity, metabolic regulation, or neurobehavioral pathways, PT-141 provides access to a clinically validated melanocortin agonist with FDA-approved precedent, extensive Phase 3 data, and a well-characterized central mechanism of action that complements peripheral approaches to sexual dysfunction.
For research use only. Not for human consumption.
SCIENTIFIC REFERENCES
- Molinoff PB, et al. PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Ann N Y Acad Sci. 2003;994:96-102. PMID: 12851303
- Diamond LE, et al. An effect on the subjective sexual response in premenopausal women with sexual arousal disorder by bremelanotide (PT-141), a melanocortin receptor agonist. J Sex Med. 2006;3(4):628-638. PMID: 16839319
- Kingsberg SA, et al. Bremelanotide for the treatment of hypoactive sexual desire disorder: two randomized phase 3 trials. Obstet Gynecol. 2019;134(5):899-908. PMID: 31599840
- Dhillon S, Keam SJ. Bremelanotide: first approval. Drugs. 2019;79(14):1599-1606. PMID: 31429064
- Kingsberg SA, et al. The neurobiology of bremelanotide for the treatment of hypoactive sexual desire disorder in premenopausal women. CNS Spectr. 2021. PMID: 33455598
CERTIFICATE
A detailed summary of the analytical profile, purity, and molecular integrity of the research-grade peptide compound.
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