PT-141
PT-141 holds great promise as a possible treatment for sexual dysfunction, especially for the treatment of erectile dysfunction or impotence in men and HSDD (Hypoactive Sexual Desire Disorder) in women.
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PT-141 Structure
- Sequence:T
- CAS Number:T
- Molecular Formula:T
- Molecular Weight: T
What is PT-141?
PT-141, also known as Bremelanotide, is sometimes referred to as female Viagra because the peptide was previously studied in Phase IIb human clinical trials for the treatment of female hypoactive sexual desire disorder (HSDD).PT-141 is a melanocortin that binds primarily to the melanocortin 4 receptor (MC-4R) and MC-1R.In 2009, PT-141 was also studied for the treatment of acute hemorrhage. PT-141 is another derivative of the synthetic melanocortin Melanotan 2 (MT-2).
PT-141 Effects
PT-141 and sexual arousal
PT-141 is a unique peptide because it stimulates the MC-4R, which is known to produce sexual arousal in the central nervous system and influence sexual behavior. Studies in mice have shown that agonists bound to the MC-4R cause increased sexual arousal and copulation in both males and females. Since the mechanism of action of PT-141 is different from that of drugs such as Viagra, it may be useful for treating impaired sexual arousal in both males and females due to causes other than reduced blood flow to the genitals.
A study of men with erectile dysfunction (ED) who did not respond to sildenafil (Viagra) found that about one-third were able to achieve a full erection for sexual intercourse after using PT-141, which was administered via nasal spray. There was also a strong dose-dependent response in the trial, suggesting that PT-141 does work in some cases []. This suggests that PT-141 may provide insights into correcting ED in cases where sildenafil treatment fails, and may provide insights into the core causes of hypogonadism.
Interestingly, PT-141 was withdrawn from clinical trials before it was approved for use in women with HSDD. This was despite indications that the drug increased the number of satisfactory monthly sexual events and decreased scores of sexual distress in women in a statistically significant manner and without any substantial side effects. Many experts in the treatment of female sexual dysfunction (FSD) have been dismayed to find that this peptide has not progressed despite positive results. They point to the lack of established endpoints in FSD trials and socio-cultural biases against women’s sexual health as major barriers to approving what they see as a much-needed therapy. They would like to see more attention paid to this topic and would like to see the FDA develop more specific guidelines for evaluating therapies such as PT-141 that could be of benefit. These experts also expressed disappointment that medication has not been tested in conjunction with other established treatments for sexual dysfunction, as they believe that such combinations may be synergistic and that peptides like PT-141 may help to overcome initial barriers and initiate psychological disorders. Treatment modalities.
In 2017, in part in response to an outcry over the discontinuation of an earlier trial, the Phase II Reconnect trial for the treatment of FSD using subcutaneous injection of PT-141 was initiated.The newest version of PT-141, called Rekynda, may soon be available in the United States. At that point, it will be legal to use PT-141 off-label to treat both male and female sexual dysfunction. These new trials rely on modified endpoints touted by FSD experts as favoring approval of such treatments.
PT-141 and bleeding
In 2009, PT-141 was slightly modified and studied as a potential treatment for hemorrhagic shock. Because PT-141 binds to MC-1R and MC-4R, it reduces ischemia and protects tissues from inadequate blood supply in cases of hypovolemic (hemorrhagic) shock. The drug does not cause significant side effects when given intravenously. This is the last of the Phase IIb trials. A modified version of PT-141 is called PL-6983.
PT-141 and Infection
MC-1R was found to have important antifungal and anti-inflammatory properties in a rat model of specific fungal infections. This is particularly important because current antifungal drugs have limited mechanisms of action and all have serious, treatment-limiting side effects in some patients. Having alternative methods of treating fungal infections can significantly reduce morbidity and mortality, especially in immunocompromised patients.
PT-141 and Cancer
The MC-1R receptor is an important stimulator of the DNA repair pathway and is therefore important in cancer treatment and prevention. Studies have shown that people carrying MC-1R mutations have an increased risk of developing basal cell carcinoma and squamous cell carcinoma.11]. An altered PT-141 may be able to correct the problems associated with these mutations and prevent or treat these cancers.
Referenced Citations
- M. Sandrock, A. Schulz, C. Merkwitz, T. Schöneberg, K. Spanel-Borowski, and A. Ricken, “Reduction in corpora lutea number in obese melanocortin-4-receptor-deficient mice,” Reprod. Biol. Endocrinol. RBE, vol. 7, p. 24, Mar. 2009.
- R. C. Rosen, L. E. Diamond, D. C. Earle, A. M. Shadiack, and P. B. Molinoff, “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,” Int. J. Impot. Res., vol. 16, no. 2, pp. 135–142, Apr. 2004. [PubMed]
- H. Wessells, V. J. Hruby, J. Hackett, G. Han, P. Balse-Srinivasan, and T. W. Vanderah, “Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2 induces penile erection via brain and spinal melanocortin receptors,” Neuroscience, vol. 118, no. 3, pp. 755–762, 2003. [PubMed]
- A.-S. Rössler, J. G. Pfaus, H. K. Kia, J. Bernabé, L. Alexandre, and F. Giuliano, “The melanocortin agonist, melanotan II, enhances proceptive sexual behaviors in the female rat,” Pharmacol. Biochem. Behav., vol. 85, no. 3, pp. 514–521, Nov. 2006. [PubMed]
- M. R. Safarinejad and S. Y. Hosseini, “Salvage of sildenafil failures with bremelanotide: a randomized, double-blind, placebo controlled study,” J. Urol., vol. 179, no. 3, pp. 1066–1071, Mar. 2008. [PubMed]
- A. H. Clayton et al., “Bremelanotide for female sexual dysfunctions in premenopausal women: a randomized, placebo-controlled dose-finding trial,” Womens Health Lond. Engl., vol. 12, no. 3, pp. 325–337, 2016. [PubMed]
- M. K. Miller, J. R. Smith, J. J. Norman, and A. H. Clayton, “Expert opinion on existing and developing drugs to treat female sexual dysfunction,” Expert Opin. Emerg. Drugs, vol. 23, no. 3, pp. 223–230, 2018. [PubMed]
- “AMAG Pharmaceuticals and Palatin Technologies Enter Into Exclusive Licensing Agreement for North American Rights to RekyndaTM (bremelanotide), a Potential Treatment for a Common Female Sexual Disorder – AMAG Pharmaceuticals.” . [MarketWatch]
- H. Ji et al., “The Synthetic Melanocortin (CKPV)2 Exerts Anti-Fungal and Anti-Inflammatory Effects against Candida albicans Vaginitis via Inducing Macrophage M2 Polarization,” PLoS ONE, vol. 8, no. 2, Feb. 2013. [PLOS ONE]
- V. Maresca, E. Flori, and M. Picardo, “Skin phototype: a new perspective,” Pigment Cell Melanoma Res., vol. 28, no. 4, pp. 378–389, Jul. 2015. [PubMed]
- L. Feller, R. a. G. Khammissa, B. Kramer, M. Altini, and J. Lemmer, “Basal cell carcinoma, squamous cell carcinoma and melanoma of the head and face,” Head Face Med., vol. 12, p. 11, Feb. 2016. [PubMed]
- Clayton AH, Althof SE, Kingsberg S, et al. Bremelanotide for female sexual dysfunctions in premenopausal women: a randomized, placebo-controlled dose-finding trial. Womens Health (Lond). 2016;12(3):325–337. doi:10.2217/whe-2016-0018
- T. R. McMillan, M. A. M. Forster, L. I. Short, A. P. Rudecki, D. L. Cline, and S. L. Gray, “Melanotan II, a melanocortin agonist, partially rescues the impaired thermogenic capacity of pituitary adenylate cyclase-activating polypeptide deficient mice,Exp. Physiol. , vol. 106, no. 2, pp. 427–437, Feb. 2021, doi: 10.1113/EP088838.”
- C. Spana, R. Jordan, and S. Fischkoff, “Effect of bremelanotide on body weight of obese women: Data from two phase 1 randomized controlled trials,Diabetes Obes. Metab., vol. 24, no. 6, pp. 1084–1093, Jun. 2022, doi: 10.1111/dom.14672. ”
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In no way does this doctor/scientist endorse or advocate the purchase, sale, or use of this product for any reason. MOL Changes has no affiliation or relationship, implied or otherwise, with this physician. The purpose of citing this doctor is to acknowledge, acknowledge and commend the exhaustive research and development work done by the scientists working on this peptide.
HPLC test report
MS test report
Manufacturer Information
- PT-141 is manufactured by MOL Changes factory.
- PT-141 supplier MOL Changes.
- Maximum acceptable production volume: 100000 bottles.
- Content standard: net peptide.
- Purity: ≥98% for all products.
- Customization: 1mg-1g size customization is acceptable