PT-141 (Bremelanotide)

Overview

PT-141, also known as Bremelanotide, is a synthetic cyclic heptapeptide derivative of Melanotan II. While it shares structural similarities with other melanocortin analogues, PT-141 is unique in that it lacks significant melanogenic (tanning) activity.

In research settings, PT-141 is recognized as a potent agonist for the melanocortin receptors, specifically MC3R and MC4R. Unlike PDE5 inhibitors, which act peripherally on vascular blood flow, PT-141 is studied for its ability to act centrally via the hypothalamus and limbic system. It is a vital tool for investigating neuroendocrine signaling pathways related to sexual desire, arousal, and libido. While FDA-approved for specific clinical indications under the name Vyleesi, it remains a primary compound for laboratory research into female sexual dysfunction and male erectile dysfunction.

Key Research Applications

PT-141 is extensively utilized in neurobiology and endocrine research:

• Central Nervous System Signaling: Investigating MC3R and MC4R receptor activation in the hypothalamus and its role in sexual motivation.
• GPCR-Mediated Pathways: Research involving G protein-coupled receptor signaling and intracellular cAMP production.
• Sexual Dysfunction Models: Experimental research into libido enhancement and arousal mechanisms in both male and female biological models.
• Receptor Selectivity: Comparative studies examining binding affinity and selectivity across the melanocortin receptor family (MC1R–MC5R).
• Peptide Stability: In vitro studies focusing on the structural integrity and degradation profiles of cyclic peptides.

Additional Details

• Synonyms: PT-141, MT-II Analogue
• Peptide Type: Synthetic Cyclic Heptapeptide

Handling & Reconstitution

To maintain the high-purity profile of this cyclic heptapeptide:

• Reconstitution: Use sterile water or an appropriate buffered aqueous solution.
• Technique: Gently swirl the vial until the powder is fully dissolved. Avoid vigorous agitation, as mechanical stress can lead to peptide degradation.
• Stability: Immediately aliquot reconstituted solutions to minimize repeated freeze-thaw cycles. Store refrigerated for short-term use or frozen at –20°C for long-term stability.
• Sterilization: If required for sensitive assays, filter sterilize (0.22 µm) the solution before use.

Important Safety Information

For Research Use Only. This product is a synthetic peptide intended strictly for laboratory and in-vitro research. It is not for human or veterinary use, nor is it intended for diagnostic, therapeutic, or cosmetic applications. Researchers should be aware that common experimental observations include nausea and flushing, which are dependent on concentration and the specific experimental model utilized.

References

• Molinoff P.B. et al. PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Annals of the New York Academy of Sciences, 2003. https://pubmed.ncbi.nlm.nih.gov/12851303/
• Rosen R.C. et al. Evaluation of the safety, pharmacokinetics and pharmacodynamic effects of subcutaneously administered PT-141, a melanocortin receptor agonist, in healthy male subjects and in patients with an inadequate response to Viagra. International Journal of Impotence Research, 2004. https://pubmed.ncbi.nlm.nih.gov/14963471/
• Kingsberg S.A. et al. Bremelanotide for the treatment of hypoactive sexual desire disorder: two randomized phase 3 trials. Obstetrics & Gynecology, 2019. https://pubmed.ncbi.nlm.nih.gov/31599840/