PT-141

PT-141

$55.00 – $65.00

PT-141, also called Bremelanotide (generic clinical name), is a heavily modified synthetic derivative of alpha-melanocyte-stimulating hormone. It has been tested in clinical trials as a treatment for both male/female hypoactive sexual desire disorder and acute hemorrhage. PT-141 is an agonist for the melanocortin-4 and melanocortin-1 receptors. Research shows that it promotes sexual arousal and stimulates the immune system.

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Description

PT-141, also called bremelanotide, is sometimes referred to as the female Viagra because the peptide was previously investigated in phase IIb human clinical trials for use in treating female hypoactive sexual desire disorder (HSDD). PT-141 is a melanocortin that binds primarily to melanocortin 4 receptor (MC-4R) and MC-1R. In 2009, PT-141 was also investigated as a treatment for acute hemorrhage. PT-141 is a derivative of another synthetic melanocortin, melanotan 2 (MT-2).

Sequence: Ac-Nle-Asp(1)-His-D-Phe-Arg-Trp-Lys(1)
Molecular Formula: C50H68N14O10
Molecular Weight: 1025.182 g/mol
PubChem CID: 9941379
CAS Number: 189691-06-3

Research

PT-141 has been investigated for its potential therapeutic effects in treating sexual dysfunction in both men and women. It acts primarily on the central nervous system, particularly targeting melanocortin receptors MC3R and MC4R, which are involved in sexual arousal and desire.

Research explores its dual application in treating hypoactive sexual desire disorder (HSDD) in women and erectile dysfunction in men, with studies showing improved sexual desire, arousal, and orgasmic function.

PT-141 and Male Sexual Dysfunction

Clinical studies have demonstrated that PT-141 can induce a significant erectile response in both healthy males and those with mild-to-moderate ED. The response is dose-dependent and the onset of action is rapid, with erections occurring approximately 30 minutes post-administration.1

PT-141 has also shown efficacy in patients who do not respond adequately to phosphodiesterase type 5 inhibitors like Viagra, suggesting it may be a viable alternative or adjunctive therapy.2

PT-141 and Female Sexual Dysfunction

Female sexual dysfunction (FSD) is a prevalent issue affecting approximately 30% of women in North America and Europe, with complex etiologies involving interpersonal, personal, and physiological factors.

Studies have shown that PT-141 selectively stimulates solicitational behaviors in female rats, which are analogous to sexual arousal in humans, without affecting other sexual behaviors such as lordosis or pacing. This indicates a specific effect on appetitive sexual behavior, suggesting its potential use in treating female sexual arousal disorders.3

Preliminary clinical data also support its role in promoting sexual desire and libido in women.4

Neurogenic Effects

Unlike PDE5 inhibitors, which augment genital blood flow via nitric oxide signaling, PT-141’s primary effects are neurogenic. By increasing dopaminergic tone in limbic circuits, it elevates sexual desire and reduces inhibitory signals from serotoninergic systems.

References: 

  1. Diamond, L., Earle, D., Rosen, R., Willett, M., & Molinoff, P. (2004). Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction. International Journal of Impotence Research, 16, 51-59. https://doi.org/10.1038/sj.ijir.3901139.
  1. Rosen, R., Diamond, L., Earle, D., Shadiack, A., & Molinoff, P. (2004). 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, 16, 135-142. https://doi.org/10.1038/sj.ijir.3901200.
  2. Pfaus, J., Shadiack, A., Van Soest, T., Tse, M., & Molinoff, P. (2004). Selective facilitation of sexual solicitation in the female rat by a melanocortin receptor agonist.. Proceedings of the National Academy of Sciences of the United States of America, 101 27, 10201-4 . https://doi.org/10.1073/PNAS.0400491101.
  3. Shadiack, A., Sharma, S., Earle, D., Spana, C., & Hallam, T. (2007). Melanocortins in the treatment of male and female sexual dysfunction.. Current topics in medicinal chemistry, 7 11, 1137-44 . https://doi.org/10.2174/156802607780906681.
  4. Pfaus, J. G., Sadiq, A., Spana, C., & Clayton, A. H. (2022). The neurobiology of bremelanotide for the treatment of hypoactive sexual desire disorder in premenopausal women. CNS spectrums, 27(3), 281–289. https://doi.org/10.1017/S109285292100002X.

 

 

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