PT-141 10mg

PT-141 (Bremelanotide)

PT-141, also known as Bremelanotide, is a synthetic peptide analog of the melanocortin receptor agonist Melanotan II. Unlike other agents studied for sexual function that primarily act via vascular mechanisms, PT-141 is proposed to act directly on the central nervous system by stimulating melanocortin receptors (MC3R and MC4R) in the hypothalamus. These receptors are believed to play key roles in regulating sexual arousal, energy balance, and appetite. As such, PT-141 has been widely investigated in research focusing on sexual function, neuroendocrine modulation, and the melanocortin system.

Overview

PT-141 is a cyclic heptapeptide that has been studied primarily for its potential role in sexual function research across multiple animal models. Unlike phosphodiesterase type 5 (PDE5) inhibitors, which act on the vascular system, PT-141 is believed to act on the brain’s neural pathways. By activating MC3R and MC4R receptors, the peptide may influence sexual desire and arousal through direct stimulation of the central melanocortin system.

Chemical Characteristics

Other Known Titles: Bremelanotide, Palatin Technologies PT-141, Melanotan II derivative

Research and Clinical Studies

Preclinical studies have suggested that PT-141 may act through activation of the central melanocortin system to influence libido and sexual motivation. Activation of melanocortin receptors (especially MC4R) in the hypothalamus has been linked to increased copulatory behavior and sexual responsiveness in experimental models.In early human research, PT-141 has been observed to increase sexual arousal without significantly affecting systemic blood pressure or heart rate, in contrast to PDE5 inhibitors that act through vasodilation. This distinct mechanism of action has driven interest in further investigation of the melanocortin pathway as a central modulator of sexual function.Beyond sexual function studies, PT-141 has also been explored for its potential to modulate appetite and energy expenditure, since melanocortin signaling also contributes to metabolic homeostasis. However, these applications remain under preliminary investigation.

PT-141 (Bremelanotide) — References

• Shadiack, A. M., Sharma, S. D., Earle, D., Spana, C., Hallam, T. J. Melanocortins in the treatment of male and female sexual dysfunction: new strategies for clinical development. Peptides. 2007;28(2):208–218.https://doi.org/10.1016/j.peptides.2006.09.020
• Diamond, L. E., Earle, D. C., Heiman, J. R., Rosen, R. C., Perelman, M. A., Harning, R. An effect on the subjective sexual response in premenopausal women with sexual arousal disorder after administration of PT-141: a randomized, double-blind, placebo-controlled, crossover study. The Journal of Sexual Medicine. 2006;3(3):526–535.https://doi.org/10.1111/j.1743-6109.2006.00238.x
• Diamond, L. E., Earle, D. C., Rosen, R. C., Heiman, J. R., Harning, R. Double-blind, placebo-controlled evaluation of the safety, pharmacokinetics and pharmacodynamics of subcutaneous bremelanotide in premenopausal women with sexual arousal disorder. The Journal of Sexual Medicine. 2009;6(9):2443–2453.https://doi.org/10.1111/j.1743-6109.2009.01345.x
• Molinoff, P. B., Shadiack, A. M., Earle, D., Diamond, L. E. PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Annals of the New York Academy of Sciences. 2003;994(1):96–102.https://doi.org/10.1111/j.1749-6632.2003.tb03167.x
• Wessells, H., Fuciarelli, K., Hansen, J., Hadley, M. E., Hruby, V. J., Dorr, R., Levine, N. Synthetic melanotropic peptide initiates erections in men with psychogenic erectile dysfunction: double-blind, placebo-controlled crossover study. The Journal of Urology. 2000;164(2):440–443.https://doi.org/10.1016/S0022-5347(05)67374-5
• Dorr, R. T., Lines, R., Levine, N., Brooks, C., Xiang, L., Hruby, V. J., Hadley, M. E. Evaluation of melanotan-II, a superpotent cyclic melanotropic peptide, in a pilot phase I clinical study. Life Sciences. 1996;58(20):1777–1784.https://doi.org/10.1016/0024-3205(96)00136-8
• Kingsberg, S. A., Clayton, A. H., Portman, D. J., Kingsberg, E. S., Simon, J. A., Jordan, R., Lucas, J., Kaminetsky, J., Krop, J., Jordan, R., Jordan, J. Bremelanotide for the treatment of hypoactive sexual desire disorder in premenopausal women: two randomized phase 3 trials. Obstetrics & Gynecology. 2019;134(5):899–908.https://doi.org/10.1097/AOG.0000000000003515
• Kingsberg, S. A., Clayton, A. H., Lucas, J., Krop, J., Jordan, R., Jordan, J. Bremelanotide for hypoactive sexual desire disorder in women: a phase 3 randomized clinical trial. Journal of Sexual Medicine. 2019;16(11):1749–1761.https://doi.org/10.1016/j.jsxm.2019.07.018
• FDA Center for Drug Evaluation and Research. Bremelanotide NDA 210557, Clinical Review, 2019. U.S. Food and Drug Administration.https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/210557Orig1s000ClinR.pdf

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