What Is PT-141 (BREMELANOTIDE) 10MG?
PT-141, also known as bremelanotide, is a synthetic derivative of alpha-melanocyte-stimulating hormone. It is an FDA-approved drug for hypoactive sexual desire disorder treatment in postmenopausal women. Researchers are interested in investigating its effect on male sexual health and weight loss. At Pinnacle Peptides, PT-141 for sale is exclusively available for research purposes, not for human consumption.
Structure Of PT-141 (BREMELANOTIDE) 10MG
From Pubchem
Synonyms: Bremelanotide, PT-141
Molecular Formula: C50H68N14O10
Molecular Weight: 1025.2 g/mol
CAS number: 189691-06-3
PubChem CID: 9941379
History
In pursuit of a treatment for sexual dysfunction, Competitive Technologies licensed Melanotan II to Palatin Technologies. However, Palatin ceased the development of melanotan-II in 2000 and began working on bremelanotide, a derivative of melanotan-II with distinct chemical properties. Competitive Technologies sued Palatin for breach of contract and ownership claims regarding bremelanotide. The parties settled in 2008, with Palatin retaining rights to bremelanotide and returning MT-II rights to the other company. FDA accepted Bremelanotide's New Drug Application for female sexual dysfunction in June 2018 and approved the drug for clinical use in the United States in June 2019.
Mechanism Of PT-141 (BREMELANOTIDE) 10MG
PT-141 acts as a non-selective agonist of melanocortin receptors: MC1R, MC3R, MC4R and MC5R. MC4R is involved in various physiological functions, including sexual arousal and desire. When PT-141 activates MC4R, it triggers the cascade of neural and hormonal responses involved in sexual response. Further, it is believed that MC3R activation might also contribute to the drug’s response.
Pre-Clinical/Clinical Research
1. Weight Loss
Research shows that melanocortin receptors are involved in appetite regulation. Findings from two phase one trials provide evidence of bremelanotide's potential for weight loss. In the first study, postmenopausal women receiving Pt-141 experienced significant weight loss and an average decrease in daily caloric consumption (400 kcal/day) compared to the control group. The second study found similar outcomes, indicating that women who received PT-141 twice daily lost weight and reduced calorie intake [1].
2. Sexual Health
Research shows that MC4R activation improves sexual response. One study found that 10 mg bremelanotide administered 45 minutes prior to intercourse improved sexual response in men who previously didn’t respond to sildenafil [2]. Another study assessed the safety and effect of coadministration of sildenafil and PT-141 in men with erectile dysfunction. The response was greater in patients who received the combination therapy as compared to those who only took sildenafil. Further, the administration of PT-141 along with sildenafil was well-tolerated, suggesting that the combination might be effective in patients who don’t respond to monotherapy [3].
In a phase I clinical trial, the safety, tolerance, and pharmacokinetic effects of bremelanotide were assessed in both male and female participants. The participants were randomly assigned to receive either a 20mg dose of PT-141 via the nasal route or a placebo, with or without ethanol. The study results indicated that a 20 mg intranasal dose of BMT is safe and generally well-tolerated in women, with average peak ethanol concentrations exceeding 80 mg/dL [4].
Another phase II trial found that self-administered subcutaneous PT-141 was effective and safe for premenopausal women with sexual dysfunction [5]. FDA approved the use of PT-141 for hypoactive sexual desire disorder in postmenopausal women based on two phase 3 clinical trials. These studies demonstrated the efficacy and safety of 0.75mg bremelanotide administered subcutaneously in women with hypoactive sexual desire disorder. The results showed that women who took PT-141 experienced a reduction in sexual distress and an increase in desire compared to those who received a placebo. Common side effects associated with bremelanotide included nausea, vomiting, and flushing [6].
Summary
PT-141 is a synthetic peptide analog of alpha-melanocyte stimulating hormone. It binds to MC4R receptors in the hypothalamus and improves the sexual response. It is approved for the treatment of hypoactive sexual desire disorder in postmenopausal women. Furthermore, it has the potential to treat male sexual dysfunction. We don’t encourage its unwarranted use and offer PT-141 purchase for research only. Buy PT-141 from Pinnacle Peptides to elevate your research.
References
- Spana, C., R. Jordan, and S. Fischkoff, Effect of bremelanotide on body weight of obese women: Data from two phase 1 randomized controlled trials. Diabetes, Obesity and Metabolism, 2022. 24(6): p. 1084-1093.
- Safarinejad, M.R. and S.Y. Hosseini, Salvage of sildenafil failures with bremelanotide: a randomized, double-blind, placebo controlled study. J Urol, 2008. 179(3): p. 1066-71.
- Diamond, L.E., et al., Co-administration of low doses of intranasal PT-141, a melanocortin receptor agonist, and sildenafil to men with erectile dysfunction results in an enhanced erectile response. Urology, 2005. 65(4): p. 755-759.
- Clayton, A.H., J. Lucas, L.R. DeRogatis, and R. Jordan, Phase I Randomized Placebo-controlled, Double-blind Study of the Safety and Tolerability of Bremelanotide Coadministered With Ethanol in Healthy Male and Female Participants. Clin Ther, 2017. 39(3): p. 514-526.e14.
- Clayton, A.H., et al., Bremelanotide for Female Sexual Dysfunctions in Premenopausal Women: A Randomized, Placebo-Controlled Dose-Finding Trial. Women's Health, 2016. 12(3): p. 325-337.
- Kingsberg, S.A., et al., Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder: Two Randomized Phase 3 Trials. Obstet Gynecol, 2019. 134(5): p. 899-908.
Certificate of Analysis (COA)
High Performance Liquid Chromatography (HPLC)
Mass Spectrometry (MS)
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