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Melanotan-2 Identity And Receptor Pharmacology — Research Overview

By Editorial Desk · published 2026-01-04 · last reviewed 2026-01-27 · Faq

melanocortin receptor raises a handful of sensible questions. This page answers them in order, starting with the fundamentals and moving to applications.

This page was last updated on 2026-01-27 and is reviewed periodically as new material appears.

Melanotan-2 Identity and Receptor Pharmacology

Pharmacologically, melanotan-2 behaves as a non-selective agonist across the melanocortin receptor family. Binding at MC1R on dermal melanocytes promotes eumelanin synthesis, which underlies the tanning response described in early human work. Activity at the centrally expressed MC4R receptor is associated with reported effects on appetite and erectile function. Because the peptide does not discriminate strongly among receptor subtypes, attributing any single observed effect to one receptor pathway is generally not possible without selective antagonists or receptor knockout models.

Research interest has centred on photoprotection and pigmentation, with a smaller body of work on appetite and sexual function. Published human data remain limited to small, frequently uncontrolled studies, and the compound has never received marketing approval from a national medicines regulator. Most laboratory work treats it as a pharmacological tool for probing melanocortin signalling in cell culture or animal models. Whether pigmentation changes observed in people translate into measurable protection against ultraviolet-induced DNA damage remains an open question.

Melanotan-2 is a synthetic cyclic heptapeptide designed as an analogue of alpha-melanocyte-stimulating hormone, the naturally occurring peptide involved in pigmentation signalling. Its sequence is conventionally written as Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2, with a lactam bridge joining the aspartate side chain to the lysine side chain. The empirical formula is C50H69N15O9 and the monoisotopic mass lies near 1023.5 daltons. N-terminal acetylation and the D-configured phenylalanine both increase resistance to enzymatic breakdown compared with the parent hormone.

Background and Mechanism of Melanotan-2

Early published reports described melanotan-2 as a tanning agent without sun protection, which means darkening is not the same as protection against ultraviolet radiation. Later studies explored the peptide in erectile dysfunction, hemorrhagic shock, and some skin conditions. No regulator in the United States or Europe has approved it for clinical use. Many products labelled melanotan-2 are sold without approval and their identity and purity are unverified. Its long-term safety in humans remains an open question.

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.

Melanotan-2 at a glance

PropertyValueNotes
Common synonymsMelanotan II; MT-II; N-acetyl-norleucyl-cyclo[Asp-His-D-Phe-Arg-Trp-Lys] amideNaming follows peptide convention; the numeral distinguishes it from melanotan-1
Molecular formulaC50H69N15O9Includes the lactam bridge; no counter-ion assumed
Monoisotopic mass1023.53 DaFree base; salts and counter-ions shift the observed value
AppearanceWhite to off-white lyophilised powderBatch-to-batch colour variation is not itself proof of impurity
Typical analytical methodRP-HPLC purity determination with ESI-MS identity confirmationRetention time alone does not establish sequence identity

Melanotan-2 Structure and Receptor Pharmacology

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.

No regulatory authority has approved melanotan-2 for human use, and several countries classify it as a prescription-only or controlled substance, which restricts lawful supply. Material sold online is generally labelled as a research chemical and is not required to meet pharmaceutical standards of identity or purity. Published human data consist mainly of small uncontrolled studies, case reports and adverse-event notifications, so the evidence base is descriptive rather than confirmatory. Whether repeated melanocyte stimulation alters long-term naevus behaviour remains an open question that no completed trial has resolved.

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Chemistry and Receptor Pharmacology

Published pharmacokinetic information is limited and comes mainly from small studies rather than registrational trials. Plasma half-life is usually described as short, on the order of tens of minutes, followed by rapid tissue distribution and clearance of the intact peptide. Metabolites and low concentrations of parent compound have been reported in urine, a detail relevant to anti-doping and forensic testing. Whether repeated exposure changes receptor sensitivity or clearance over time remains an open question. Values differ noticeably between analytical assays, so published numbers should be read as approximate rather than definitive.

Melanotan II is a synthetic cyclic heptapeptide with the sequence Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2, corresponding to a molecular formula of C50H69N15O9 and a monoisotopic mass near 1024 daltons. It was designed as a structural analogue of alpha-melanocyte-stimulating hormone, a peptide hormone produced by cleavage of proopiomelanocortin. A lactam bridge between the aspartate and lysine side chains closes the ring, and the C-terminal amide removes a free carboxyl group. Both modifications increase resistance to enzymatic degradation compared with the linear parent hormone. Four substitutions distinguish it from afamelanotide, the linear analogue studied under the name melanotan I.

Identity and Chemical Background

The compound emerged from research programs in the 1980s that examined analogues of alpha-melanocyte-stimulating hormone for pigmentation and photoprotection. Investigators modified the native sequence to extend activity duration and potency. A related analogue, afamelanotide, was developed within the same broad line of inquiry and eventually gained approval in certain jurisdictions for a rare light-sensitivity condition. Melanotan-2 itself did not progress through the same regulatory route and has no approved therapeutic indication.

Melanocortin receptors comprise five subtypes with distinct tissue distributions and functions. Melanotan-2 is described in the literature as a non-selective agonist that engages several of these subtypes, including MC1R, MC3R, MC4R, and MC5R. MC1R is the subtype most directly linked to melanin production in skin cells. Because the compound is not subtype-selective, its observed effects in experimental settings are generally attributed to activity across multiple receptor pathways rather than to a single target.

Origins and Research Status

Outside regulated medicine, melanotan II circulates through online vendors as a research chemical, often marketed for tanning. Products sold this way vary widely in purity, concentration, and labeling accuracy, and independent testing has documented discrepancies. Published reports describe both pigment effects and adverse reactions, including nausea, flushing, and darkening of existing moles. Long-term safety data are sparse, and no large controlled trial has established a risk profile. Questions about cumulative effects on melanocytes remain unresolved in the literature.

Melanotan II is a synthetic peptide analog modeled on alpha-melanocyte-stimulating hormone, a naturally occurring signaling peptide involved in pigmentation. Its structure is a cyclic heptapeptide containing two non-natural substitutions, norleucine at position four and D-phenylalanine at position seven. These modifications resist enzymatic breakdown and extend the molecule's activity relative to the native hormone. The compound binds melanocortin receptors and is studied mainly as a pharmacological tool rather than a therapeutic product. It has never received approval as a medicine in any major jurisdiction.

Notes from published material

=== History of cultural impact === The use of LSD was most widespread from the 1960s through the 1980s. In the 1960s, LSD and other psychedelics were adopted by and became synonymous with the Hippie counterculture movement due to their perceived ability to expand consciousness. This resulted in LSD being viewed as a cultural threat to American values and the Vietnam War effort, and it was designated as a Schedule I (illegal for medical as well as recreational use) substance in 1968. It was listed as a Schedule I controlled substance by the United Nations in 1971 and currently has no approved medical uses. Several figures, including Aldous Huxley, Timothy Leary, and Al Hubbard, had begun to advocate the consumption of LSD as it became central to the counterculture of the 1960s. In the early 1960s, the use of LSD and other hallucinogens was advocated by new proponents of consciousness expansion such as Leary, Huxley, Alan Watts and Arthur Koestler, and, according to historians, they profoundly influenced the thinking of the new generation of youth.

Molecular engineering is highly interdisciplinary by nature, encompassing aspects of chemical engineering, materials science, bioengineering, electrical engineering, physics, mechanical engineering, and chemistry. There is also considerable overlap with nanotechnology, in that both are concerned with the behavior of materials on the scale of nanometers or smaller. Given the highly fundamental nature of molecular interactions, there are a plethora of potential application areas, limited perhaps only by one's imagination and the laws of physics. However, some of the early successes of molecular engineering have come in the fields of immunotherapy, synthetic biology, and printable electronics (see molecular engineering applications). Molecular engineering is a dynamic and evolving field with complex target problems; breakthroughs require sophisticated and creative engineers who are conversant across disciplines. A rational engineering methodology that is based on molecular principles is in contrast to the widespread trial-and-error approaches common throughout engineering disciplines. Rather than relying on well-described but poorly-understood empirical correlations between the makeup of a system and its properties, a molecular design approach seeks to manipulate system properties directly using an understanding of their chemical and physical origins. This often gives rise to fundamentally new materials and systems, which are required to address outstanding needs in numerous fields, from energy to healthcare to electronics.

== History == Fluvoxamine was developed by Kali-Duphar, part of Solvay Pharmaceuticals, Belgium, now Abbott Laboratories, and introduced as Floxyfral in Switzerland in 1983. It was approved by the U.S. Food and Drug Administration (FDA) in 1994, and introduced as Luvox in the US. In India, it is available, among several other brands, as Uvox by Abbott. It was one of the first SSRI antidepressants to be launched, and is prescribed in many countries to patients with major depression. It was the first SSRI, a non-TCA drug, approved by the U.S. FDA specifically for the treatment of OCD. At the end of 1995, more than ten million patients worldwide had been treated with fluvoxamine. Fluvoxamine was the first SSRI to be registered for the treatment of obsessive compulsive disorder in children by the FDA in 1997. In Japan, fluvoxamine was the first SSRI to be approved for the treatment of depression in 1999 and was later in 2005 the first drug to be approved for the treatment of social anxiety disorder. Fluvoxamine was the first SSRI approved for clinical use in the United Kingdom. Manufacturers include BayPharma, Synthon, and Teva, among others.

Because prokaryotic mRNA does not need to be processed or transported, translation by the ribosome can begin immediately after the end of transcription. Therefore, it can be said that prokaryotic translation is coupled to transcription and occurs co-transcriptionally. In eukaryotic cells the process of translation starts with the information stored in the nucleotide sequence of DNA. This is first transformed into mRNA, then transfer RNA (tRNA) specifies which three-nucleotide codon from the genetic code corresponds to which amino acid. Eukaryotic mRNA that has been processed and transported to the cytoplasm (i.e., mature mRNA) can then be translated by ribosomes. Translation may occur at ribosomes free in the cytoplasm, or targeted to the endoplasmic reticulum by the signal recognition particle. Therefore, unlike in prokaryotes, eukaryotic translation is not directly coupled to transcription. In some contexts, protein abundance can increase even when mRNA abundance decreases, because translation efficiency and protein turnover are regulated independently of transcript levels; this has been reported for mRNA and protein levels of EEF1A1 in breast cancer.

=== Newsweek's America's Best High Schools === In June 2010, seven PGCPS high school were listed in Newsweek's annual list of the top 1600 high schools in the nation. This was up from five county high schools which made the list from the previous year. The 2010 list included Eleanor Roosevelt High School in Greenbelt (#409), Oxon Hill High School in Oxon Hill (#957), Bowie High School in Bowie (#1,173), Laurel High School in Laurel (#1,343), High Point High School in Beltsville (#1,361), Central High School in Capitol Heights (#1,429), and Parkdale High School in Riverdale (#1,481). The schools are ranked on the number of Advanced Placement, International Baccalaureate and/or Cambridge tests taken by all students in a school in 2009, divided by the number of graduating seniors, called the "Challenge Index". The schools represent the top six percent of all public high schools in America. In June 2009, five PGCPS high schools were named in the best high schools list. It included Bowie High School in Bowie, Charles Herbert Flowers High School in Springdale, High Point High School in Beltsville, Oxon Hill High School in Oxon Hill, and Eleanor Roosevelt High School in Greenbelt. Eleanor Roosevelt ranked the highest out of county schools at 372nd on the nationwide list, Oxon Hill ranked 918th, High Point ranked 961st, Bowie ranked 1,370th, and Charles Herbert Flowers ranked 1,445th.

Sources: en.wikipedia.org

Further detail

== External links == "Anatomy photo:39:01-0100". SUNY Downstate Medical Center. Archived from the original on March 5, 2016. jejunumileum at The Anatomy Lesson by Wesley Norman (Georgetown University) McGill (Wayback Machine copy)

MOFs have potential as heterogeneous catalysts, although applications have not been commercialized. Their high surface area, tunable porosity, diversity in metal and functional groups make them especially attractive for use as catalysts. Like other heterogeneous catalysts, MOFs may allow for easier post-reaction separation and recyclability than homogeneous catalysts. In some cases, they also give a enhanced catalyst stability. Additionally, they typically offer substrate-size selectivity. Nevertheless, while clearly important for reactions in living systems, selectivity on the basis of substrate size is of limited value in abiotic catalysis, as reasonably pure feedstocks are generally available.Enantiopure chiral ligands or their metal complexes have been incorporated into MOFs to lead to efficient asymmetric catalysts. Even some MOF materials may bridge the gap between zeolites and enzymes when they combine isolated polynuclear sites, dynamic host–guest responses, and a hydrophobic cavity environment. Theoretical calculations show that MOFs are semiconductors or insulators with band gaps between 1.0 and 5.5 eV which can be altered by changing the degree of conjugation in the ligands indicating its possibility for being photocatalysts. Useful comparisons can be made with zeolites, which are extraordinarily useful in catalysis; however, zeolites are limited by the fixed tetrahedral coordination of the Si/Al connecting points and the two-coordinated oxide linkers, and fewer than 200 zeolites are known.

It could also reflect steric and chemical properties that had another effect on the codon during its evolution. Amino acids with similar physical properties also tend to have similar codons, reducing the problems caused by point mutations and mistranslations. Three main hypotheses address the origin of the genetic code. Many models belong to one of them or to a hybrid:

On 12 August 1990, Saddam "propose[d] that all cases of occupation, and those cases that have been portrayed as occupation, in the region, be resolved simultaneously". He called for Israel to withdraw from occupied territories in Palestine, Syria, and Lebanon, Syria to withdraw from Lebanon, and "mutual withdrawals by Iraq and Iran and arrangement for the situation in Kuwait." He called for a replacement of US troops, that mobilized in Saudi Arabia, with "an Arab force", as long as that force did not involve Egypt. He requested an "immediate freeze of all boycott and siege decisions" and a normalization of relations with Iraq. Bush was strongly opposed to any "linkage" between Iraq's occupation of Kuwait and the Palestinian issue. On 23 August, Saddam appeared on state television with Western hostages to whom he had refused exit visas. In the video, he asks a British boy, Stuart Lockwood, whether he is getting his milk, and goes on to say, through his interpreter, "We hope your presence as guests here will not be for too long. Your presence here, and in other places, is meant to prevent the scourge of war." Another Iraqi proposal communicated was delivered to US national security advisor Brent Scowcroft by an unidentified Iraqi official. The official communicated that Iraq would "withdraw from Kuwait and allow foreigners to leave" provided the UN lifted sanctions, allowed "guaranteed access to the Persian Gulf through the Kuwaiti islands of Bubiyan and Warbah", and allowed Iraq to "gain full control of the Rumaila oil field that extends slightly into Kuwaiti territory".

Sources: en.wikipedia.org

Supporting material

== Production == About 200,000 tonnes of tetrahydrofuran are produced annually. The most widely used industrial process involves the acid-catalyzed dehydration of 1,4-butanediol. Ashland/ISP is one of the biggest producers of this chemical route. The method is similar to the production of diethyl ether from ethanol. The butanediol is derived from condensation of acetylene with formaldehyde followed by hydrogenation. DuPont developed a process, for producing THF by oxidizing n-butane to crude maleic anhydride, followed by catalytic hydrogenation. A third major industrial route entails hydroformylation of allyl alcohol followed by hydrogenation to 1,4-butanediol.

Roeder and Robert Tjian, for their outstanding work on eukaryotic transcription regulation 1993 James E. Rothman and Randy Schekman, for determining the components of the secretory pathway 1992 Paul Nurse and Leland H. Hartwell, for establishing the details of the control of eukaryotic cell cycle 1991 David Botstein, Raymond L. White and Ronald W. Davis, for creating the methods by which variations in the human genome can be detected and analyzed 1990 Richard Henderson and Peter Nigel Tripp Unwin, for determining the first structure of an integral membrane protein 1989 Christiane Nüsslein-Volhard and Edward B. Lewis, for pioneering studies of eukaryotic development 1988 Sidney Altman and Thomas R. Cech, for discovering RNA catalysis 1987 Shinya Inoué, for his innovations in light microscopy 1986 Harland G. Wood, for his outstanding work on enzyme function 1985 Seymour Benzer and Sydney Brenner, for founding modern eukaryotic genetics 1984 Donald D. Brown and Robert L. Letsinger, for their seminal work on development 1983 Eric R. Kandel and Daniel E. Koshland, Jr., for pioneering contributions to sensory transduction 1982 Keith R. Porter and Alexander Rich 1981 Stanley Cohen, Rita Levi-Montalcini and Gordon H. Sato 1980 Elias J. Corey, Bengt I. Samuelsson and Frank H. Westheimer 1979 Howard Green and Beatrice Mintz 1978 César Milstein 1977 Barbara McClintock 1976 Peter D. Mitchell 1975 Bruce Ames, James A. Miller and Elizabeth C. Miller 1974 Arthur B. Pardee and H. Edwin Umbarger 1973 H. Ronald Kaback and Saul Roseman 1972 Boris Ephrussi 1971 David H. Hubel and Torsten N.

== Planar chromatography == The retardation factor, RF, is commonly used in paper chromatography and thin layer chromatography (TLC) for analyzing and comparing different substances. It can be mathematically described by the following ratio:

==== Libya ==== The mummified remains of an infant were discovered during an expedition by archaeologist Fabrizio Mori to Libya during the winter of 1958–1959 in the natural cave structure of Uan Muhuggiag. After curious deposits and cave paintings were discovered on the surfaces of the cave, expedition leaders decided to excavate. Uncovered alongside fragmented animal bone tools was the mummified body of an infant, wrapped in animal skin and wearing a necklace made of ostrich egg shell beads. Professor Tongiorgi of the University of Pisa radiocarbon-dated the infant to between 5,000 and 8,000 years old. A long incision located on the right abdominal wall, and the absence of internal organs, indicated that the body had been eviscerated post-mortem, possibly in an effort to preserve the remains. A bundle of herbs found within the body cavity also supported this conclusion. Further research revealed that the child had been around 30 months old at the time of death, though sex could not be determined due to poor preservation of the sex organs.

=== Insulin === When levels of blood sugar rise, whether as a result of glycogen conversion, or from digestion of a meal, a different hormone is released from beta cells found in the islets of Langerhans in the pancreas. This hormone, insulin, causes the liver to convert more glucose into glycogen (this process is called glycogenesis), and to force about 2/3 of body cells (primarily muscle and fat tissue cells) to take up glucose from the blood through the GLUT4 transporter, thus decreasing blood sugar. When insulin binds to the receptors on the cell surface, vesicles containing the GLUT4 transporters come to the plasma membrane and fuse together by the process of endocytosis, thus enabling a facilitated diffusion of glucose into the cell. As soon as the glucose enters the cell, it is phosphorylated into glucose-6-phosphate in order to preserve the concentration gradient so glucose will continue to enter the cell. Insulin also provides signals to several other body systems, and is the chief regulator of metabolic control in humans. There are also several other causes for an increase in blood sugar levels. Among them are the 'stress' hormones such as epinephrine (also known as adrenaline), several of the steroids, infections, trauma, and of course, the ingestion of food. Diabetes mellitus type 1 is caused by insufficient or non-existent production of insulin, while type 2 is primarily due to a decreased response to insulin in the tissues of the body (insulin resistance).

Sources: en.wikipedia.org

Frequently asked questions

What is melanotan-2 chemically?

It is a synthetic cyclic heptapeptide analogue of alpha-melanocyte-stimulating hormone, containing seven amino acids with a lactam ring and a D-configured phenylalanine residue. It is supplied as a lyophilised powder for laboratory research.

How does it differ from the natural hormone?

The natural hormone is a linear tridecapeptide that is rapidly degraded in circulation. Melanotan-2 is shortened, cyclised, N-terminally acetylated, and carries a D-amino acid substitution, all of which slow enzymatic breakdown.

Does it hold any regulatory approval?

No national medicines regulator has approved melanotan-2 for therapeutic or cosmetic use. In several jurisdictions it is treated as an unapproved prescription medicine, and its legal classification differs from country to country.

Is melanotan-2 a natural hormone?

No. It is a laboratory-made peptide, while the natural hormone is alpha-melanocyte-stimulating hormone, a longer peptide produced by the pituitary gland and by skin cells. Melanotan-2 mimics only a short active region of that hormone and contains non-natural residues such as D-phenylalanine.

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