Best PT-141 5 mg and 10mg Peptides GMP Factory

PT-141

PT-141

Other names:Vyleesi, PT141, Rekynda, bremelanotide acetate, Bremelanotide

Polypeptide PT-141 (Bremelanotide) is a synthetic peptide developed from Melanotan 2 (MT-II). It is also a man-made peptide that was originally developed as a sunless tanning agent, but it has shown a lot of promise as a possible treatment for sexual dysfunction. Especially, it has great helpful on the treatment of erectile dysfunction or impotence in men and HSDD (hypoactive sexual desire disorder) in women.

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Referenced Citations

[1] Alabsi W, Eedara BB,  Encinas-Basurto D, Polt R, Mansour HM. Nose-to-Brain Delivery of Therapeutic Peptides as Nasal Aerosols. Pharmaceutics. 2022 Sep 5;14(9):1870. doi: 10.3390/pharmaceutics14091870. PMID: 36145618; PMCID: PMC9502087.

[2] Mayer D, Lynch SE. Bremelanotide: New Drug Approved for Treating Hypoactive Sexual Desire Disorder. Ann Pharmacother. 2020 Jul;54(7):684-690. doi: 10.1177/1060028019899152. Epub 2020 Jan 1. PMID: 31893927.

[3] Bartlik B, Sugarman A, Seenaraine S, Green S. FDA-Approved (Bremelanotide, Flibanserin) and Off-Label Medications (Testosterone, Sildenafil) to Enhance Sexual Desire/Function in Women. On J Complement & Alt Med. 4(1): 2020. OJCAM. MS.ID.000578.

[4] Simon JA, Kingsberg SA, Portman D, Williams LA, Krop J, Jordan R, Lucas J, Clayton AH. Long-Term Safety and Efficacy of Bremelanotide for Hypoactive Sexual Desire Disorder. Obstet Gynecol. 2019 Nov;134(5):909-917. doi: 10.1097/AOG.0000000000003514. PMID: 31599847; PMCID: PMC6819023.

[5] Wessells H, Fuciarelli K, Hansen J, Hadley ME, Hruby VJ, Dorr R, et al. Synthetic melanotropic peptide initiates erections in men with psychogenic erectile dysfunction: Double-blind, placebo controlled crossover study. J Urol. 1998 Aug;160(2):389–93.

[6] King SH, Mayorov AV, Balse-Srinivasan P, Hruby VJ, Vanderah TW, Wessells H. Melanocortin receptors, melanotropic peptides and penile erection. Curr Top Med Chem. 2007;7(11):1098-1106. PMID: 17584130; PMCID: PMC2694735.

[7] Michelakis E, Tymchak W, Archer S. Sildenafil: from the bench to the bedside. CMAJ. 2000 Oct 31;163(9):1171-5. PMID: 11079066; PMCID: PMC80254.

[8] Safarinejad MR, Hosseini SY. Salvage of sildenafil failures with bremelanotide: a randomized, double-blind, placebo controlled study. J Urol. 2008 Mar;179(3):1066-71. doi: 10.1016/j.juro.2007.10.063. Epub 2008 Jan 18. PMID: 18206919.

[9] Sharot T, Guitart-Masip M, Korn CW, Chowdhury R, Dolan RJ. How dopamine enhances an optimism bias in humans. Curr Biol. 2012 Aug 21;22(16):1477-81. doi: 10.1016/j.cub.2012.05.053. Epub 2012 Jul 12. PMID: 22795698; PMCID: PMC3424419.

[10] Edinoff AN, Sanders NM, Lewis KB, Apgar TL, Cornett EM, Kaye AM, Kaye AD. Bremelanotide for Treatment of Female Hypoactive Sexual Desire. Neurol Int. 2022 Jan 4;14(1):75-88. doi: 10.3390/neurolint14010006. PMID: 35076581; PMCID: PMC8788464.

[11]Kim S, Cho MC, Cho SY, Chung H, Rajasekaran MR. Novel Emerging Therapies for Erectile Dysfunction. World J Mens Health. 2021 Jan;39(1):48-64. doi: 10.5534/wjmh.200007. Epub 2020 Mar 16. PMID: 32202086; PMCID: PMC7752520.

[12]Liu C, Kaeser PS. Mechanisms and regulation of dopamine release. Curr Opin Neurobiol. 2019 Aug;57:46-53. doi: 10.1016/j.conb.2019.01.001. Epub 2019 Feb 12. PMID: 30769276; PMCID: PMC6629510.

What Is PT-141?

PT-141, also known as bremelanotide, has been nicknamed the “female Viagra” due to its previous investigation in phase IIb human clinical trials as a potential treatment for female hypoactive sexual desire disorder (HSDD). It belongs to the melanocortin family and primarily binds to the melanocortin 4 receptor (MC-4R) and MC-1R. In 2009, PT-141 was also studied as a treatment for acute hemorrhage. PT-141 is derived from another synthetic melanocortin called melanotan 2 (MT-2). [1]

PT-141 Molecular Structure

pt141 structure

Authoritative source:PubChem

Sequence: AC-Nle-Asp(1)-His-D-Phe-Arg-Trp-Lys(1)
Molecular Formula: CsoHogN14O10
Molecular Weight: 1025. 182 g/mol
PubChem CID: 9941379
CAS Number: 189691-06-3

PT-141 Research

PT-141 and Sexual Arousal

PT-141 is a distinctive peptide as it activates the MC-4R, which is recognized for inducing sexual arousal in the central nervous system and influencing sexual behavior. Research conducted on mice has demonstrated that agonist binding to the MC-4R receptor leads to sexual arousal and enhanced copulation in both males and females. Due to its distinct mechanism of action compared to drugs like Viagra, PT-141 offers the potential to address sexual arousal disorders in both men and women that arise from causes other than reduced blood flow to the genital area. [7]

In a study involving men with erectile dysfunction (ED) who did not respond to sildenafil (Viagra), it was found that approximately one-third of the participants achieved satisfactory erections for sexual intercourse when treated with PT-141, administered through a nasal spray. The trial also demonstrated a significant response dependent on the dosage, indicating the effectiveness of PT-141 in specific cases. These findings suggest that PT-141 could provide potential solutions for addressing ED in situations where sildenafil has been ineffective, and it may also contribute to a better understanding of the central factors contributing to hypoactive sexual desire.

pt141 arousal

Duration of penile base rigidity greater than 60% for placebo compared to various doses of PT-141.

Authoritative source:Nature

Interestingly, PT-141 was discontinued in clinical trials before receiving approval for use in women with hypoactive sexual desire disorder (HSDD). This decision was made despite indications that the drug increased the frequency of satisfying sexual events per month and significantly reduced female sexual distress scores, all without significant side effects. Many experts specializing in the treatment of female sexual dysfunction (FSD) were disappointed that the peptide was not being further developed despite positive outcomes. They attribute this setback to the lack of established trial endpoints for FSD and societal biases against women’s sexual health, which impede the approval of much-needed therapies. These experts hope for increased attention to the topic and urge the FDA to establish clearer guidelines for evaluating beneficial therapies like PT-141. Furthermore, they express disappointment that pharmacological treatments were not tested in conjunction with established methods of sexual dysfunction treatment, as they believe that combining approaches may have a synergistic effect. They suggest that peptides such as PT-141 could be instrumental in overcoming initial barriers and facilitating psychological treatment modalities.[2]

In 2017, in response to the concerns raised regarding the discontinuation of earlier trials, Phase II Reconnect trials were initiated to evaluate the use of subcutaneous injections of PT-141 for female sexual dysfunction (FSD). The latest formulation of PT-141, known as Rekynda, is expected to become available for use in the United States soon. Once approved, it would be permissible to use PT-141 off-label to treat both male and female sexual dysfunction. These new trials have incorporated modified endpoints that experts in FSD have advocated for, recognizing their value in facilitating the approval of such treatments.

PT-141 and Hemorrhage

In 2009, PT-141 underwent slight modifications and was explored as a potential therapy for hemorrhagic shock. Due to its binding affinity for both MC-1R and MC-4R, PT-141 exhibits properties that mitigate ischemia and safeguard tissues against inadequate blood supply in the context of hypovolemic (hemorrhagic) shock. Intravenous administration of the drug is associated with minimal side effects. PT-141 reached phase IIb trials and the modified version is now known as PL-6983.[4]

PT-141 and Infection

In a rat model of a specific fungal infection, the MC-1R has demonstrated significant anti-fungal and anti-inflammatory properties. This discovery is highly significant since current anti-fungal treatments have limitations in their mechanism of action and often result in severe side effects that can hinder treatment in certain patients. The availability of an alternative treatment for fungal infections could significantly reduce morbidity and mortality, particularly among individuals with compromised immune systems.[5][6]

PT-141 and Cancer

The MC-1R receptor plays a crucial role in stimulating DNA repair pathways, making it a promising target for cancer treatment and prevention. Studies have indicated that individuals with MC-1R variants have a higher susceptibility to basal cell and squamous cell carcinomas. Modified versions of PT-141 hold potential in addressing the issues associated with these variants and may offer opportunities for the prevention and treatment of these types of cancers.[7]

PT-141 and Weight Loss

Research indicates that the MC-4R receptor plays a pivotal role in the regulation of appetite. Agonists of the MC-4R, such as melanotan 2 and PT-141, have been shown to induce satiety and reduce overall calorie consumption. Additionally, PT-141 seems to interact with leptin signaling pathways, contributing to the intricate regulation of food intake. This correlation is not unexpected, considering that PT-141 is derived from α-MSH, which has been shown to negatively regulate food intake through its interaction with the ghrelin-leptin system.

Animal studies provide evidence indicating that PT-141 may enhance energy expenditure by decoupling specific energy pathways, thereby leading to an elevation in basal metabolism. Research conducted on mice demonstrates that activation of the MC-4R receptor can stimulate thermogenesis, even in mice lacking the proteins responsible for regulating this process. Consequently, there is an augmentation in calorie expenditure, including a substantial portion occurring in adipose tissue, even during periods of rest.

Recent double-blind, randomized, placebo-controlled trials have provided further support for the aforementioned physiological findings and have confirmed that PT-141 elicits significant weight loss, primarily attributed to reduced caloric intake. Participants receiving PT-141 exhibited approximately twice the weight loss compared to those in the placebo group. On average, the reduction in caloric intake amounted to nearly 400 kcal/day. Additionally, the study demonstrated a dose-response relationship, with subjects experiencing greater weight loss when PT-141 was administered twice daily rather than once daily[14]. Ongoing investigations are actively exploring PT-141 and its interactions with melanocortin receptors to gain a deeper understanding of the melanocortin system’s role in weight loss and energy balance.

PT-141 Research Directions

Currently, PT-141 is garnering significant attention as a treatment for sexual dysfunction. However, it holds great potential for research beyond the realms of sexual dysfunction and hemorrhage. For instance, MC-4R has been implicated in certain cases of obesity where it is defective or absent, accounting for approximately 6% of early-onset obesity cases. PT-141 provides a unique opportunity to investigate this specific cause of obesity and potentially identify intervention pathways. Moreover, MC-1R is involved in pain perception, inflammation, kidney pathology, and the spread of infection, presenting a wide range of research opportunities where PT-141 could contribute valuable insights.

PT-141 demonstrates minimal side effects and has low oral bioavailability, but it exhibits excellent subcutaneous bioavailability in mice. However, it’s important to note that dosage per kilogram in mice does not directly translate to humans. PT-141 available for purchase at Peptide Sciences is strictly limited to educational and scientific research purposes, and it should not be consumed by humans. It is advised to only acquire PT-141 if you hold a valid research license.

Referenced Citations

[1] 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. [PMC]

[2] 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].

[3] 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]

[4] 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]

[5] [5] 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]

[6] 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]

[7]  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]

Author of this article:
Dr. Jean Zeng graduated from king’s college london Faculty of Life Sciences & Medicine.

Scientific Journal paper Author:

E. Diamond

Palatin Technologies, Inc., Cranbury, New Jersey, USA

B. MOLINOFF

Palatin Technologies, Inc., Cranbury, New Jersey 08512, USA

C. Earle

Palatin Technologies, Inc., Cranbury, New Jersey, USA

Songlong Jiao

Jiangsu Key Laboratory for Design and Manufacture of Micro-Nano Biomedical Instruments, School of Mechanical Engineering, Southeast University, Nanjing 211189, People’s Republic of China

In no way does this doctor/scientist endorse or advocate the purchase, sale, or use of this product for any reason. peptide.ltd 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.

Author of this article:

Dr. Jean Zeng graduated from king's college london Faculty of Life Sciences & Medicine.

Scientific Journal paper Author:

Stephen C. Bain
Diabetes Research Group, Swansea University Medical School, Swansea, SA2 8PP, UK
Department of Diabetes and Endocrinology, Singleton Hospital, Swansea Bay University Health Board, Swansea, SA2 8QA, UK

In no way does this doctor/scientist endorse or advocate the purchase, sale, or use of this product for any reason. Polypeptide.ltd 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.