PT-141 (Bremelanotide): Melanocortin System Research Guide

Comprehensive overview of PT-141/Bremelanotide, a melanocortin receptor agonist, including its mechanism of action, research applications in sexual function studies, and key scientific findings.

> Educational Content Only: This compound is discussed for educational purposes only and is not currently offered by our company. PT-141, also known as Bremelanotide, is a synthetic peptide analog of alpha-melanocyte-stimulating hormone (α-MSH). Originally developed from the tanning peptide Melanotan II, PT-141 has become a subject of significant research interest due to its unique mechanism of action through the central nervous system rather than the vascular system. PT-141 is a cyclic heptapeptide with the sequence Ac-Nle-cycloAsp-His-D-Phe-Arg-Trp-Lys-OH. Key characteristics include: - Molecular Weight: 1,025 Da - Water solubility: Good - Stability: Requires refrigeration - Half-life: Approximately 2-4 hours PT-141 exerts its effects primarily through melanocortin receptors, particularly MC3R and MC4R in the central nervous system. - MC4R Agonism: Primary target in the hypothalamus, involved in sexual response pathways - MC3R Interaction: Secondary binding site with potential metabolic implications - CNS-Mediated Effects: Unlike PDE5 inhibitors, PT-141 works through neural pathways 1. Binds to melanocortin receptors in the hypothalamus 2. Activates dopaminergic and oxytocinergic pathways 3. Modulates neural circuits involved in arousal and motivation Primary research areas include: - Female sexual interest/arousal disorder models - Male erectile function investigations - Central nervous system role in sexual response - Comparison with vascular-targeted approaches Research has explored: - Reward pathway modulation - Motivation and appetitive behaviors - Social behavior effects - Stress response interactions PT-141 serves as a tool compound for studying: - MC3R/MC4R receptor pharmacology - Hypothalamic signaling pathways - Neuroendocrine regulation | Research Area | Notable Finding | |---------------|-----------------| | Mechanism | Works independently of nitric oxide pathway | | CNS Action | Activates hypothalamic neurons involved in sexual response | | Time Course | Effects observed within 30-60 minutes of administration | | Duration | Active period of approximately 4-6 hours | Research-grade PT-141 requires: - Storage at -20°C as lyophilized powder - Reconstitution with bacteriostatic water - Protection from light - Use within 4 weeks of reconstitution when refrigerated Documented observations in studies include: - Transient nausea at higher doses - Facial flushing - Blood pressure variations - These effects are typically dose-dependent 1. Molinoff PB, et al. (2003). PT-141: A melanocortin agonist for the treatment of sexual dysfunction. Ann NY Acad Sci. 2. Diamond LE, et al. (2004). An effect on the subjective sexual response in premenopausal women with sexual arousal disorder. J Sex Med. 3. Pfaus JG, et al. (2007). Bremelanotide: An overview of preclinical CNS effects on female sexual function. J Sex Med. 4. Clayton AH, et al. (2016). Bremelanotide for female sexual dysfunctions. Expert Opin Investig Drugs.

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