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Melanotan-2 Structure And Receptor Pharmacology — Quick Reference

By Editorial Desk · published 2025-12-03 · last reviewed 2025-12-17 · News

Everything below concerns melanocortin receptor. We keep the language plain, cite what the science says, and separate well-supported claims from open questions.

Updated 2025-12-17. Numbers and descriptions here follow the published literature rather than marketing material.

Melanotan-2 Structure and Receptor Pharmacology

Melanotan-2 is a synthetic cyclic heptapeptide designed as a structural analogue of alpha-melanocyte-stimulating hormone, the endogenous tridecapeptide that regulates pigment production. Two modifications distinguish it from the natural hormone: norleucine replaces methionine at the N-terminus, which limits oxidation, and a D-phenylalanine substitution raises receptor affinity. The ring is closed through an aspartate-lysine lactam bridge, giving the molecule a constrained conformation. The free base has a molecular mass near 1024 daltons, and commercial material is usually supplied as an acetate salt. It appears in the literature as a research peptide rather than an approved therapeutic agent.

Receptor studies place melanotan-2 among non-selective melanocortin agonists, binding MC1R, MC3R, MC4R and MC5R rather than a single subtype. Activation of MC1R on cutaneous melanocytes raises tyrosinase activity and shifts pigment synthesis toward eumelanin, which is darker and more photostable than pheomelanin. Central receptors, particularly MC4R, are associated with appetite suppression and with reported effects on sexual function. Because subtype selectivity is low, the same molecule engages pigment, metabolic and vascular pathways at once, and this breadth is a common explanation offered for the range of adverse events described in user reports.

Peptide Identity and Structural Background

Melanotan-2 is a synthetic cyclic heptapeptide designed as an analogue of alpha-melanocyte-stimulating hormone, a naturally occurring peptide involved in pigmentation signalling. Its sequence incorporates modified residues that increase potency and extend biological activity relative to the native hormone. The compound binds receptors of the melanocortin family and is examined mainly in laboratory research. It does not occur naturally and exists only as a manufactured chemical entity produced by solid-phase synthesis.

The peptide was developed during the 1980s by researchers investigating melanocortin signalling and skin pigmentation pathways. Early work focused on analogues of alpha-melanocyte-stimulating hormone that would resist enzymatic breakdown more effectively than the parent molecule. Melanotan-2 emerged from that programme as a shortened, cyclised variant. Reports describing its synthesis and receptor activity later appeared in the scientific literature. Commercial availability grew through unregulated channels rather than through pharmaceutical approval.

Melanotan-2 at a glance

PropertyValueNotes
Molecular formulaC50H69N15O9Free base; salt forms add to total mass
Molecular massAbout 1024 daltonsCalculated for the free base
Structural classCyclic heptapeptideContains D-phenylalanine and norleucine
Parent hormoneAlpha-melanocyte-stimulating hormoneEndogenous tridecapeptide of 13 residues
Receptor profileNon-selective melanocortin agonistInteracts with MC1R, MC3R, MC4R and MC5R

Background and Mechanism of Melanotan-2

Melanotan-2, also written Melanotan II, is a synthetic cyclic heptapeptide designed as an analogue of alpha-melanocyte-stimulating hormone. Its sequence is Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2, and the lactam bridge between the aspartate and lysine side chains constrains the peptide into a ring. This structural change increases receptor affinity and metabolic stability relative to the native hormone. The compound was created in the 1980s as a research tool for studying pigmentation biology.

Melanocytes are the pigment-producing cells of the skin, and they carry melanocortin-1 receptors on their surface. When the receptor is activated, cyclic adenosine monophosphate rises inside the cell and raises the activity of enzymes such as tyrosinase, which increases melanin output. Melanotan-2 binds melanocortin-1 receptors in vitro and in animal models, and this binding is generally described as the basis for the tanning effect. Other receptors account for different effects: melanocortin-4 receptors contribute to appetite and erectile signalling, while melanocortin-3 and melanocortin-5 receptors contribute to energy balance and exocrine function.

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Melanotan-2 Identity And Regulatory Status

Melanotan II is a synthetic cyclic heptapeptide analogue of alpha-melanocyte-stimulating hormone, a naturally occurring peptide involved in pigmentation signalling. Its structure substitutes a lactam bridge between side chains to increase stability relative to the native hormone. The compound is also known by the shorthand MT-II and by several non-proprietary synonyms used in research catalogues. It is not an approved therapeutic product in any major jurisdiction; material sold under this name is typically offered as a laboratory reagent rather than as a medicine.

Activity is attributed to agonism at melanocortin receptors, particularly MC1R and MC4R. Activation of MC1R on melanocytes increases melanin synthesis, which underlies the reported tanning effect. MC4R engagement in the central nervous system is linked to appetite suppression and to effects on sexual arousal reported in early clinical studies. Those studies were small and were not designed to establish efficacy or long-term safety. Receptor selectivity among the melanocortin subtypes is not absolute, which complicates attribution of any effect to a single pathway.

Background from the literature

== Overdose == Finasteride has been studied in humans at single doses of up to 400 mg and at continuous dosages of up to 80 mg/day for three months, without adverse effects observed. There is no specific recommended antidote for finasteride overdose.

coli for animals and humans Kentucky Bioprocessing took over Large Scale Biology's facilities in Owensboro, Kentucky, and offers contract biomanufacturing services in tobacco plants, grown in greenhouses or in open fields. Medicago Inc. – Pre-clinical trials of Influenza vaccine made in transiently infected Nicotiana benthamiana (relative of tobacco) plants in greenhouses. Medicago grew virus-like particles in the Australian weed Nicotiana benthamiana, for development of a candidate vaccine against the COVID-19 virus, initiating a Phase I clinical trial in July 2020. PharmaPraxis – Developing biosimilars in collaboration with PlantForm (see below) and Fraunhofer. Pharming – C1 inhibitor, human collagen 1, fibrinogen (with American Red Cross), and lactoferrin in cow milk The intellectual property behind the fibrinogen project was acquired from PPL Therapeutics when PPL went bankrupt in 2004. Phyton Biotech uses plant cell culture systems to manufacture active pharmaceutical ingredients based on taxanes, including paclitaxel and docetaxel Planet Biotechnology – antibodies against Streptococcus mutans, antibodies against doxorubicin, and ICAM 1 receptor in tobacco PlantForm Corporation – biosimilar trastuzumab in tobacco – It is developing biosimilars in collaboration with PharmaPraxis (see above) and Fraunhofer. ProdiGene – was developing several proteins, including aprotinin, trypsin and a veterinary TGE vaccine in corn. Was in process of launching trypsin product in 2002 when later that year its field test crops contaminated conventional crops.

Nobel physics laureate Steven Weinberg said that the Nobel committee "fleeced" Dyson, but Dyson remarked in 2009, "I think it's almost true without exception if you want to win a Nobel Prize, you should have a long attention span, get hold of some deep and important problem and stay with it for ten years. That wasn't my style." Dyson was a regular contributor to The New York Review of Books, and published a memoir, Maker of Patterns: An Autobiography Through Letters in 2018. In 2012 Dyson published (with William H. Press) a fundamental new result about the prisoner's dilemma in the Proceedings of the National Academy of Sciences of the United States of America.

Sources: en.wikipedia.org

Further detail

Agouti signalling peptide adopts an inhibitor cystine knot motif. Along with the homologous Agouti-related peptide, these are the only known mammalian proteins to adopt this fold. The peptide consists of 131 amino acids.

Antioxidants: Three vitamins, ascorbic acid; α-tocopherol; and β-carotene, are well recognized for their antioxidant activities in human. Free radical-scavenging ability of antioxidants may reduce the oxidative stress and thus may protect against oxidative damage. Based on observational studies among healthy individuals, antioxidant concentrations were found to be inversely correlated with several biomarkers of insulin resistance or glucose intolerance.

=== Convenience, automation === In vitro methods can be miniaturized and automated, yielding high-throughput screening methods for testing molecules in pharmacology or toxicology. In toxicology, U.S. agencies such as the EPA use high-throughput in vitro screening to test large numbers of chemicals and reduce the need for animal-based toxicity tests.

Sources: en.wikipedia.org

Background from the literature

George Walker Bush was born on July 6, 1946, at Grace-New Haven Hospital in New Haven, Connecticut. He is the first child of George Herbert Walker Bush and Barbara Pierce, and was raised in Midland and Houston, Texas. His five siblings are Robin, Jeb, Neil, Marvin and Dorothy. Robin died from leukemia at the age of three in 1953. His paternal grandfather, Prescott Bush, was a U.S. senator from Connecticut. His father was Ronald Reagan's vice president from 1981 to 1989 and the 41st president of the United States from 1989 to 1993. Bush has distant English and German ancestry, along with more distant (over seven generations removed) Dutch, Welsh, Irish, French, and Scottish roots. Bush attended public schools in Midland, Texas, until the family moved to Houston after he had completed seventh grade. He then spent two years at The Kinkaid School, a college-preparatory school in Piney Point Village, Texas. Bush later attended Phillips Academy, a boarding school in Andover, Massachusetts, where he played baseball and was the head cheerleader during his senior year. He attended Yale University from 1964 to 1968, graduating with a Bachelor of Arts degree in history. During this time, he was a cheerleader and a member of the Delta Kappa Epsilon, serving as the president of the fraternity during his senior year. Bush became a member of the Skull and Bones society as a senior. Bush was a rugby union player and was on Yale's 1st XV. He characterized himself as an average student.

Two days after the execution, then-Governor Jeb Bush suspended all executions in the state and appointed a commission "to consider the humanity and constitutionality of lethal injections." The ban was lifted by Governor Charlie Crist when he signed the death warrant for Mark Dean Schwab on July 18, 2007. On November 1, 2007, the Florida Supreme Court unanimously upheld the state's lethal-injection procedures. A study published in 2007 in PLOS Medicine suggested that "the conventional view of lethal injection leading to an invariably peaceful and painless death is questionable." The execution of Romell Broom was abandoned in Ohio on September 15, 2009, after prison officials failed to find a vein after two hours of trying on his arms, legs, hands, and ankle. This stirred up more intense debate in the United States about lethal injection. Broom's execution was later rescheduled for March 2022, but he died in 2020 before the sentence could be carried out. Dennis McGuire was executed in Lucasville, Ohio, on January 17, 2014. According to reporters, McGuire's execution took more than 20 minutes, and he was gasping for air for 10–13 minutes after the drugs had been administered. It was the first use of a new drug combination, which was introduced in Ohio after the European Union banned sodium thiopental exports. This reignited criticism of the conventional three-drug method. Clayton Lockett died of a heart attack during a failed execution attempt on April 29, 2014, at Oklahoma State Penitentiary in McAlester, Oklahoma.

==== Canada ==== Cider is produced commercially in every Canadian province except Newfoundland and Labrador, usually with a 5–7% alcohol content although the term is also used for some non-fermented apple juices. According to the Canadian Food and Drug Regulations, alcoholic cider is an alcoholic fermentation of apple juice that does not contain more than 13% absolute alcohol by volume (ABV) or less than 2.5% ABV. Quebec cider is considered a traditional alcoholic beverage. It is generally sold in 750 ml bottles, has an alcohol content generally between 7% and 13% (with aperitifs ciders having alcohol content up to 20%), and can be served as a substitute for wine. As in the rest of the world, sparkling cider is getting more and more popular in Quebec and thanks to the law cider sold in the province can only be made from 100% pure apple juice. Cider making was, however, forbidden from the early years of British rule as it was in direct conflict with established British brewers' interests (most notably John Molson). In recent years, a new type called ice cider has been sold. This type of cider is made from apples with a particularly high level of sugar caused by natural frost. The regulations regarding cider in Canada are fairly strict in terms of sourcing and alcohol content. For it to be legally sold as cider, it must be the product of the alcoholic fermentation of apple juice and it must contain no less than 2.5 and no more than 13.0 per cent alcohol by volume.

Sources: en.wikipedia.org

Frequently asked questions

Is melanotan-2 approved for medical use?

No regulatory agency has authorised melanotan-2 as a medicine for any indication. It circulates mainly as a research chemical or through unregulated channels. As a result, identity, purity and content are not independently guaranteed.

How does melanotan-2 differ from melanotan-1?

Melanotan-1, also called afamelanotide, is a linear analogue with greater selectivity for MC1R and has received approval in some jurisdictions for a specific photosensitivity disorder. Melanotan-2 is cyclic, less selective, and reaches central receptors more readily. The two are often confused in online discussion despite different pharmacology and regulatory status.

What is the connection to alpha-MSH?

Alpha-MSH is an endogenous tridecapeptide derived from pro-opiomelanocortin. Melanotan-2 reproduces its core receptor-binding sequence inside a shortened, stabilised ring. The result is a molecule with a longer effective half-life and higher potency than the parent hormone.

What is Melanotan-2 chemically?

It is a synthetic cyclic heptapeptide and an analogue of alpha-melanocyte-stimulating hormone. The molecule is produced by chemical synthesis rather than extracted from a biological source.

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