• Лабораторное оборудование для синтеза пептидов
д
Икс
д

PT-141 (3 мг х 10 флаконов)

Контакт для заказа
Бактериостатическая вода

Бесплатно (1) 30 мл бактериостатической воды
с квалифицированными заказами более500 долларов США.
(без учета капсульной продукции, косметических пептидов, промокодов и доставки)

 

PT-141, также называемый бремеланотидом (общее клиническое название), представляет собой сильно модифицированное синтетическое производное альфа-меланоцитстимулирующего гормона. Он был протестирован в клинических испытаниях в качестве средства лечения гипоактивного расстройства полового влечения у мужчин и женщин и острого кровотечения. PT-141 является агонистом рецепторов меланокортина-4 и меланокортина-1. Исследования показывают, что он способствует сексуальному возбуждению и стимулирует иммунную систему.

Использование продукта:Этот ПРОДУКТ ПРЕДНАЗНАЧЕН ТОЛЬКО КАК ИССЛЕДОВАТЕЛЬСКИЙ ХИМИКАТ.Это обозначение позволяет использовать исследовательские химикаты исключительно для испытаний in vitro и лабораторных экспериментов. Вся информация о продуктах, доступная на этом сайте, предназначена только для образовательных целей. Любое телесное введение людям или животным строго запрещено законом. С этим продуктом должны работать только лицензированные и квалифицированные специалисты. Этот продукт не является лекарством, продуктом питания или косметическим средством, и его нельзя маркировать, использовать или маркировать как лекарство, продукт питания или косметику.

Что такое ПТ-141?

PT-141, также называемый бремеланотидом, иногда называют женской виагрой, поскольку пептид ранее исследовался в клинических испытаниях фазы IIb на людях для использования при лечении расстройства гипоактивного сексуального влечения у женщин (HSDD). PT-141 представляет собой меланокортин, который связывается преимущественно с рецепторами меланокортина 4 (MC-4R) и MC-1R. В 2009 году PT-141 также исследовался как средство лечения острого кровотечения. PT-141 является производным другого синтетического меланокортина,мелатонин 2(МТ-2).

Молекулярная структура PT-141

Молекулярная структура PT-141Источник:PubChem

Последовательность:Ac-Nle-Asp(1)-His-D-Phe-Arg-Trp-Lys(1)
Молекулярная формула:С50ЧАС68Н14О10
Молекулярный вес:1025,182 г/моль
Идентификатор клиента PubChem: 9941379
Номер КАС:189691-06-3

ПТ-141 Исследования

PT-141 и сексуальное возбуждение

PT-141 является уникальным пептидом, поскольку он стимулирует MC-4R, который, как известно, вызывает сексуальное возбуждение в центральной нервной системе и влияет на сексуальное поведение.[1], [2]. Studies in mice have shown that agonist binding to MC-4R causes sexual arousal and increased copulation in both males and females[3], [4]. Because PT-141 works via a different mechanism than drugs like Viagra, it is possible to treat sexual arousal disorders in both men and women that stem from 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 roughly one third experienced adequate erection for sexual intercourse with PT-141 (administered via nasal spray). There was also a strong dose-dependent response in the trial, indicating that PT-141 is indeed effective in certain cases[]. This suggests that PT-141 could offer insight into correcting ED in settings where sildenafil has failed and may offer insight into central causes of hypoactive sexual desire.

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

Interestingly, PT-141 was pulled from clinical trials before it reached approval for use in women suffering from HSDD. This is despite signs that the drug increased the number of satisfying sexual events per month and decreased female sexual distress scores in a statistically significant manner without any substantial side effects[6]. Many experts who treat female sexual dysfunction (FSD) were dismayed to find the peptide was not being advanced despite positive results. They point to a lack of established endpoints for trials of FSD and socio-cultural biases against women’s sexual health as the primary roadblocks that are inhibiting approval of what they see as much-needed therapies[7]. They hope that greater attention will be given to the topic and that the FDA will establish more concrete guidelines for evaluating therapies like PT-141 that can offer benefit. These experts also expressed dismay that the pharmacological treatments were not tested in conjunction with other established means of treating sexual dysfunction as they believe that the combination may prove synergistic and that peptides like PT-141 may be useful for overcoming initial barriers and jump-starting psychological treatment modalities.

In 2017, partly in response to the outcry against the cessation of earlier trials, Phase II Reconnect trials were launched using subcutaneous injections of PT-141 for FSD. The newest version of PT-141, called Rekynda, may soon be available for use in the United States. It would be legal to use PT-141 off-label, at that point, to treat both male and female sexual dysfunction[8]. These new trials have relied on the kind of modified endpoints that experts in FSD have touted as beneficial to seeing these kinds of treatments approved.

PT-141 and Hemorrhage

In 2009, PT-141 was modified slightly and investigated as a potential treatment for hemorrhagic shock. Because PT-141 binds to both MC-1R and MC-4R, it reduces ischemia and protects tissues against inadequate blood supply in the setting of hypovolemic (hemorrhagic) shock. The drug, when administered intravenously, does not produce substantial side effects. It was last in phase IIb trials. The modified version of PT-141 is referred to as PL-6983.

PT-141 and Infection

The MC-1R has been found, in a rat model of a specific fungal infection, to possess important anti-fungal and anti-inflammatory properties[9]. This is of particular importance because current anti-fungals are limited in terms of their mechanism of action and all produce serious and treatment-limiting side effects in certain patients. Having an alternative to use in the treatment of fungal infections could reduce morbidity and mortality substantially, especially in patients with immune compromise.

PT-141 and Cancer

The MC-1R receptor is an important stimulus of DNA repair pathways and thus is of interest in cancer treatment and prevention[10]. Research shows that people with variants of MC-1R are at increased risk for both basal cell and squamous cell carcinoma[11]. Altered PT-141 may be able to correct the problems experienced as a result of these variants and prevent or treat these cancers.

Research Directions

Right now, PT-141 has received widespread and intense attention as a treatment for sexual dysfunction. There is, however, a great deal of potential research outside of sexual dysfunction and hemorrhage that PT-141 could be applied to. For instance, MC-4R is well-known to be defective or missing in certain cases of obesity and may account for as much as 6% of all cases of early-onset obesity. PT-141 offers a unique means of exploring this particular cause of obesity and potentially illustrating a pathway for intervention. MC-1R plays roles in both pain and inflammation as well as kidney pathology and the spread of infection. There is a plethora of available research that PT-141 could help to shed light on.

PT-141 exhibits minimal side effects, low oral and excellent subcutaneous bioavailability in mice. Per kg dosage in mice does not scale to humans. PT-141 for sale at

Peptide Gurus is limited to educational and scientific research only, not for human consumption. Only buy PT-141 if you are a licensed researcher.

Article Author

The above literature was researched, edited and organized by Dr. Logan, M.D. Dr. Logan holds a doctorate degree from Case Western Reserve University School of Medicine and a B.S. in molecular biology.

Scientific Journal Author

Dr. Sheryl A. Kingsberg is the chief of behavioral medicine at University Hospitals Case Medical Center and professor in Reproductive Biology and Psychiatry at Case Western Reserve University. Her areas of clinical specialization include sexual medicine, female sexual disorders, cognitive behavioral psychotherapy, menopause, pregnancy and postpartum mood disorders, psychological aspects of infertility, and psychological and sexual aspects of cancer. Dr. Kingsberg’s primary research interests are in treatments for female sexual disorders and the psychological aspects of infertility and menopause. She led a randomized, placebo-controlled dose-finding trial for PT-141. She has numerous publications in many national and international journals, sits on the editorial board of Menopause and has authored numerous chapters on topics including perimenopause and sexuality, oocyte donation, infertility and aging, the treatment of psychogenic erectile dysfunction and sexuality after cancer. Dr. Kingsberg received her PhD from the University of South Florida in Tampa and completed her fellowship in sexual medicine at University Hospitals Case Medical Center. She is an active member in a number of national and international organizations including the American Psychological Association and the American Society for Reproductive Medicine. She currently sits on the Board of Trustees of The North American Menopause Society, and serves as the current treasurer of the Society for Assisted Reproductive Technologies. Dr. Kingsberg s a past president of The International Society for the Study of Women’s Sexual Health.

Dr. Sheryl A. Kingsberg is being referenced as one of the leading scientists involved in the research and development of PT-141. In no way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between

Peptide Gurus and this doctor. The purpose of citing the doctor is to acknowledge, recognize, and credit the exhaustive research and development efforts conducted by the scientists studying this peptide. Dr. Kingsberg is listed in [12] under the referenced citations.

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.
  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. 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]
  8. “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]
  9. 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]
  10. 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]
  11. 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]
  12. 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
  13. 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.”
  14. 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. ”

ALL ARTICLES AND PRODUCT INFORMATION PROVIDED ON THIS WEBSITE ARE FOR INFORMATONAL AND EDUCATIONAL PURPOSES ONLY.

The products offered on this website are furnished for in-vitro studies only. In-vitro studies (Latin: in glass) are performed outside of the body.  These products are not medicines or drugs and have not been approved by the FDA to prevent, treat or cure any medical condition, ailment or disease.  Bodily introduction of any kind into humans or animals is strictly forbidden by law.

Request Inquery

About us

PeptideGurus is a leading supplier of American-made research peptides, offering top-quality products at competitive prices. With a focus on excellence and customer service, they ensure a secure and convenient ordering process with global shipping.

Request a Quote

Peptide Gurus
  • Peptide Gurus
  • info@peptidegurus.com
  • Glendale, AZ, USA
  • © Copyright Peptide Gurus 2024. All rights reserved.
    All products on this site are for Research, Development use only. Products are Not for Human consumption of any kind. The statements made within this website have not been evaluated by the US Food and Drug Administration or HEALTH CANADA. The statements and the products of this company are not intended to diagnose, treat, cure or prevent any disease.
    PeptideGurus is a chemical supplier. PeptideGurus is not a compounding pharmacy or chemical compounding facility as defined under 503A of the Federal Food, Drug, and Cosmetic act. Peptide Sciences is not an outsourcing facility as defined under 503B of the Federal Food, Drug, and Cosmetic act.

    CONTACT

    Request Inquery