Research Brief
What Is Melanotan 2?
Resposta Rapida
Visao Geral Melanotan II (MT-II) e um(a) sintetico(a), cyclic heptapeptide analog do(a) endogenous 13-amino-acid hormone α-melanocyte-stimulating hormone (α-MSH). It was originally synthesized no(a) University of Arizona no(a) late 1980s by Victor Hruby, Mac Hadley, and Robert Dorr.[1] Chemically, M...
Visao Geral
Melanotan II (MT-II) e um(a) sintetico(a), cyclic heptapeptide analog do(a) endogenous 13-amino-acid hormone α-melanocyte-stimulating hormone (α-MSH). It was originally synthesized no(a) University of Arizona no(a) late 1980s by Victor Hruby, Mac Hadley, and Robert Dorr.[1]
Chemically, MT-II is defined as Ac-Nle-c[Asp-His-D-Phe-Arg-Trp-Lys]-NH₂, a shortened variant of α-MSH with key modifications: a lactam bridge cyclization (Asp→Lys) aumenta enzymatic resistance, and D-Phenylalanine substitution aprimora potency. These make MT-II "superpotent" comparado(a) a native α-MSH and enable it to cross the blood-brain barrier — um(a) principal distinction do(a) linear Melanotan I (afamelanotide).[1][3]
MT-II acts como um(a) non-selective agonist at melanocortin receptors MC1R, MC3R, MC4R, and MC5R with alto(a) nanomolar affinity (Ki ~1.1–1.3 nM), but does NOT bind MC2R (the ACTH receptor). This broad receptor ativacao drives its diverse effects — tanning, erectogenic, anorexigenic, and social behavioral modulacao.[2]
The ativo(a) metabolite of MT-II — Bremelanotide (PT-141) — was aprovado(a) pela FDA in 2019 sob o(a) brand name Vyleesi for hypoactive sexual desire disorder in premenopausal women. MT-II itself remains unaprovado(a) por qualquer regulatory body.[3]
Referencias
- Dorr RT, Lines R, Levine N, et al. Evaluation of melanotan-II, a superpotent cyclic melanotropic peptide in a pilot phase-I clinical study. Life Sciences. 1996;58(20):1777-1784.
- Hadley ME, Dorr RT. Melanocortin peptide therapeutics: Historical milestones, clinical studies and commercialization. Peptides. 2006;27(4):921-930.
- Wessells H, Fuciarelli K, Hansen J, et al. Synthetic melanotropic peptide inicia erections in men with psychogenic erectile dysfunction: Double-blind, placebo controlled crossover study. The Journal of Urology. 1998;160(2):389-393.
- FDA Warning Letters regarding unauthorized marketing of Melanotan products.
- Vemulapalli R, Kurowski S, Salisbury B, et al. Activation of central melanocortin receptors by MT-II aumenta cavernosal pressure in rabbits pelo(a) neuronal release of NO. British Journal of Pharmacology. 2001;134(8):1705-1710.
- Côté I, et al. Activation do(a) central melanocortin system chronically reduz body mass sem the necessity of longo prazo caloric restriction. Canadian Journal of Physiology and Pharmacology. 2017.
- Ford CL, McDonough AA, Horie K, Young LJ. Melanocortin agonism in a social context ativa seletivamente nucleus accumbens in an oxytocin-dependent manner. Neuropharmacology. 2024;247:109848.
- Jain S, Panyutin A, Liu N, et al. Melanotan II causes hypothermia in mice by ativacao of mast cells and estimulacao of histamine 1 receptors. American Journal of Physiology-Endocrinology and Metabolism. 2018;315(3):E357-E366.
- Wessells H, Levine N, Hadley ME, Dorr RT, Hruby VJ. Effect of an alpha-melanocyte stimulating hormone analog on penile erection and sexual desire in men with organic erectile dysfunction. Urology. 2000;56(4):641-646.
- Eliason NL, Martin L, Low MJ, Sharpe AL. Melanocortin agonista do receptor melanotan-II microinjected no(a) nucleus accumbens diminui appetitive and consumptive responding for food. Neuropeptides. 2022;96:102289.
- Minakova E, Lang J, Medel-Matus JS, et al. Melanotan-II reverses autistic features in a maternal immune ativacao modelo de camundongo of autism. PLoS ONE. 2019;14(1):e0210389.
- Ter Laak MP, et al. Melanotan II promove periferico(a) regeneracao nervosa in a rat sciatic nerve crush model. 2003.
- Evans-Brown M, Dawson RT, Chandler MD, McVeigh J. Use of melanotan I and II no(a) general population. BMJ. 2009;338:b566.
- Wu JC, Tsai HE, Hsiao YH, et al. Topical MTII Therapy Suppresses Melanoma Through PTEN Upregulacao and Cyclooxygenase II Inhibition. International Journal of Molecular Sciences. 2020;21(2):681.
- Dreyer BA, Amer T, Fraser M. Melanotan-induziu priapism: a hard-earned tan. BMJ Case Reports. 2019;12(2):e227644.
- Nelson ME, Bryant SM, Aks SE. Melanotan II injection resultando em sistemico(a) toxicity and rhabdomyolysis. Clinical Toxicology. 2012;50(10):1169-1173.
- Peters B, Hadimeri H, Wahlberg R, Afghahi H. Melanotan II: a possible cause of renal infarction. CEN Case Reports. 2020;9(2):159-161.
- Sivyer GW. Dermatological changes with melanotan II use in a FAMMM patient. Dermatology Practical & Conceptual. 2012.
- Ryakhovsky VV, Khachiyan GA, Kosovova NF, et al. The primeiro(a) preparative solution phase synthesis of melanotan II. Beilstein Journal of Organic Chemistry. 2008;4:39.
- Hjuler KF, Lorentzen HF. Melanoma associado(a) com the use of melanotan-II. Dermatology. 2014;228(1):34-36.
- Giuliano F, Clement P, Droupy S, et al. Melanotan-II: Investigation do(a) inducer and facilitator effects on penile erection in anaesthetized rat. Neuroscience. 2006;138(1):293-301.
- Li G, Zhang Y, Wilsey JT, Scarpace PJ. Unabated anorexic and aprimorou thermogenic responses to melanotan II in diet-induziu ratos obesos. Journal of Endocrinology. 2004;182(1):123-132.
- King SH, et al. Melanocortin Receptors, Melanotropic Peptides and Penile Erection. Current Topics in Medicinal Chemistry. 2007;7(11):1111-1119.
- Wessells H, Levine N, Hadley ME, Dorr RT, Hruby VJ. Melanocortin agonista do receptors, penile erection, and sexual motivation: human studies with Melanotan II. International Journal of Impotence Research. 2000;12(Suppl 4):S74-S79.
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Este conteudo e fornecido apenas para fins educacionais e informativos. Os produtos sao fornecidos apenas para estudos in vitro e nao sao medicamentos, drogas ou suplementos. Nao aprovado pela FDA para prevenir, tratar ou curar qualquer condicao.