en · de · es · pt
melanotan-2-notes.peptides1004.com › Info › Melanotan-2 Identity And Receptor Pharmacology — Complete Guide

Melanotan-2 Identity And Receptor Pharmacology — Complete Guide

By Editorial Desk · published 2025-11-19 · last reviewed 2025-12-09 · Info

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

Last reviewed on 2025-12-09. Where a claim depends on a specific study, the study is described rather than over-claimed.

Melanotan-2 Identity and Receptor Pharmacology

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.

Handling, Measurement, and Regulatory Context

Regulatory treatment varies by country. In the United States, melanotan-2 is not approved for any indication, and products marketed for human use fall outside the approved drug framework. Some other jurisdictions have placed it under prescription controls or listed it as a prohibited or restricted substance. Online listings frequently describe the material as a research chemical, a category that does not carry the same manufacturing and labelling requirements as approved medicines.

Solid peptide material is generally stable when kept cold and dry. Common practice is storage at -20 degrees Celsius or lower, with desiccant and protection from light. Repeated freeze-thaw cycles and exposure to moisture are associated with degradation, aggregation, or loss of material. Once dissolved, stability depends on solvent, concentration, and temperature, and solutions are usually treated as short-lived unless stability data support longer periods. Handling notes typically emphasise minimising time at ambient temperature.

Identity and purity are assessed with chromatographic and mass spectrometric techniques. Reversed-phase high-performance liquid chromatography separates the target peptide from related impurities and degradation products, and the resulting retention time is compared against a reference standard. Mass spectrometry, often coupled to liquid chromatography, confirms molecular mass. Amino acid analysis or peptide mapping can provide additional sequence-level confirmation when required. Results are only as reliable as the reference materials used alongside them.

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

Background and Receptor Mechanism

Melanotan II binds several melanocortin receptor subtypes rather than a single target. MC1R on melanocytes drives melanin synthesis, while MC3R and MC4R participate in energy balance, appetite, and sexual response pathways. This lack of selectivity explains why reported effects extend beyond skin darkening. Substitutions at positions four and seven, including norleucine and D-phenylalanine, increase potency and resistance to peptidases. Understanding which receptor mediates which effect remains an active area of investigation.

Published human data come mostly from small, short studies rather than large controlled trials. Reported outcomes include increased skin pigmentation and, in some reports, effects on appetite and libido, but sample sizes are small and follow-up is limited. Whether long-term use produces durable pigment changes or adverse effects is not established. Because products sold outside pharmacies are not standardized, the actual content of any given vial is often unknown. Independent testing of such material is uncommon.

Melanotan II is a synthetic cyclic heptapeptide analog derived from the core sequence of alpha-melanocyte-stimulating hormone. Researchers at the University of Arizona synthesized it during the 1980s while studying pigmentation and appetite signaling. The compound is not an approved medicine in any major jurisdiction and appears mainly in laboratory and research-chemical settings. Its structure incorporates a lactam bridge between side chains, which constrains the ring and slows enzymatic breakdown relative to the natural hormone.

Related pages on this site

Storage, Verification and Regulatory Status

Melanotan-2 appears on the World Anti-Doping Agency prohibited list within the peptide hormone class, and several national regulators treat it as an unapproved prescription substance. Some countries restrict importation or sale for personal use. Because the compound is widely traded as a research chemical, the practical legal picture differs between jurisdictions and shifts over time. Human safety data covering long periods are limited, and whether repeated pigmentation changes carry any lasting risk to melanocytes remains an open question.

Freeze-dried melanotan-2 is normally kept as a desiccated powder at minus twenty degrees Celsius or lower, shielded from light and moisture. Peptides of this size degrade through hydrolysis, oxidation and deamidation, and each pathway accelerates as temperature and water activity rise. Repeated freeze-thaw cycles promote aggregation and loss of material, so aliquoting a stock solution before freezing is standard laboratory practice. Once dissolved, the solution is markedly less stable than the powder. In laboratory work, solutions are generally refrigerated and used within days rather than kept for months.

Chemistry and Receptor Pharmacology

Receptor-binding studies classify melanotan II as a non-selective melanocortin agonist. It interacts with MC1R, MC3R, MC4R and MC5R, with reported affinities in the low nanomolar range and no strong subtype preference. Activation of MC1R on dermal melanocytes shifts pigment synthesis toward eumelanin, the dark polymer deposited in melanosomes and transferred to keratinocytes. Because the same peptide engages MC4R in the hypothalamus, it also appears in animal work on food intake and erectile response, which is why it is discussed in both pigment and metabolic research. Which receptor populations dominate after systemic exposure in humans is not fully established.

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.

Reference notes

=== 4. Alveolar bone (alveolar process) === The alveolar bone forms part of the maxilla and mandible and provides the osseous support for the teeth by forming their sockets. Its structure and density are maintained by functional forces transmitted through the periodontal ligament. In periodontitis, inflammatory mediators released during the host immune response stimulate osteoclastic activity, leading to alveolar bone resorption. This irreversible loss of supporting bone is a hallmark of clinical attachment loss and represents the most significant structural consequence of periodontal disease.

However, the same article reported that CBT and fluoxetine outperformed treatment with only fluoxetine. Combining fluoxetine with CBT appeared to bring no additional benefit in two different studies or, at the most, only marginal benefit, in a fourth study. Behavior therapy for depression is sometimes referred to as behavioral activation. In addition, behavioral activation appears to take less time and lead to longer lasting change. Two well-researched treatment manuals include Social skills training for depression and Behavioral activation treatment for depression. A meta-analysis from 2023 showed that behavioral activation have a clinically meaningful effect on depression. Emotionally focused therapy, founded by Sue Johnson and Les Greenberg in 1985, treats depression by identifying and processing underlying emotions. The treatment manual, Facilitating emotional change, outlines treatment techniques. This kind of therapy assumes that our emotions have a strong connection to our sense of identity. It believes that if we are able to foster and understand our emotions, our sense of identity will be healed as a result. Acceptance and commitment therapy (ACT), a mindfulness form of CBT, which has its roots in behavior analysis, also demonstrates that it is effective in treating depression, and can be more helpful than traditional CBT, especially where depression is accompanied by anxiety and where it is resistant to traditional CBT.

Fowler was initially skeptical but was ultimately convinced that Bohr was correct, and by 1915 "spectroscopists had transferred [the Pickering–Fowler series] definitively [from hydrogen] to helium." Bohr's theoretical work on the Pickering series had demonstrated the need for "a re-examination of problems that seemed already to have been solved within classical theories" and provided important confirmation for his atomic theory. In 1938, Russian physicist Pyotr Leonidovich Kapitsa discovered that helium-4 has almost no viscosity at temperatures near absolute zero, a phenomenon now called superfluidity. This phenomenon is related to Bose–Einstein condensation. In 1972, the same phenomenon was observed in helium-3, but at temperatures much closer to absolute zero, by American physicists Douglas D. Osheroff, David M. Lee, and Robert C. Richardson. The phenomenon in helium-3 is thought to be related to pairing of helium-3 fermions to make bosons, in analogy to the Cooper pairs of electrons producing superconductivity. In 1961, Vignos and Fairbank reported the existence of a different phase of solid helium-4, designated the gamma-phase. It exists for a narrow range of pressure between 1.45 K (−271.70 °C; −457.06 °F) and 1.78 K (−271.37 °C; −456.47 °F).

Moreover, both the refractive index and the optical absorption are found to be dispersionless over a broad wavelength range from visible to near infrared. Finally, GO film offers flexible patterning capability by using the maskless DLW method, which reduces the manufacturing complexity and requirements. As a result, a novel ultrathin planar lens on a GO thin film has been realized recently using the DLW method. The distinct advantage of the GO flat lens is that phase modulation and amplitude modulation can be achieved simultaneously, which are attributed to the giant refractive index modulation and the variable linear optical absorption of GO during its reduction process, respectively. Due to the enhanced wavefront shaping capability, the lens thickness is pushed down to subwavelength scale (~200 nm), which is thinner than all current dielectric lenses (~ μm scale). The focusing intensities and the focal length can be controlled effectively by varying the laser powers and the lens sizes, respectively. By using an oil immersion high numerical aperture (NA) objective during DLW process, 300 nm fabrication feature size on GO film has been realized, and therefore the minimum lens size has been shrunk down to 4.6 μm in diameter, which is the smallest planar micro lens and can only be realized with metasurface by FIB. Thereafter, the focal length can be reduced to as small as 0.8 μm, which would potentially increase the numerical aperture (NA) and the focusing resolution.

MetaPred: A webserver for the prediction of cytochrome P450 isoforms responsible for metabolizing a drug molecule. The MetaPred server predicts metabolizing CYP isoforms of a drug molecule/substrate based on SVM models developed using CDK descriptors. This server is intended to help researchers working in the field of drug discovery. The effort also demonstrates that it is possible to develop free web servers in the field of cheminformatics. This may encourage other researchers to develop web servers for public use, leading to decreased cost of discovering new drug molecules. ToxiPred: A server for prediction of aqueous toxicity of small chemical molecules in T. pyriformis. KetoDrug: A user friendly web server for binding affinity prediction of ketoxazole derivatives and small chemical molecules against Fatty Acid Amide Hydrolase (FAAH). KiDoQ: A web server to serve researchers working in the field of designing inhibitors against dihydrodipicolinate synthase (DHDPS), a potential drug target enzyme of a unique bacterial DAP/Lysine pathway. GDoQ: GDoQ (Prediction of GLMU inhibitors using QSAR and AutoDock) is an open source platform for predicting inhibitors against Mycobacterium tuberculosis (M.Tb) drug target N-acetylglucosamine-1-phosphate uridyltransferase (GLMU) protein. This is a potential drug target involved in bacterial cell wall synthesis. This server uses molecular docking and QSAR strategies to predict inhibitory activity value (IC50) of chemical compounds for GLMU protein. ROCR: The ROCR is an R package for evaluating and visualizing classifier performance.

Sources: en.wikipedia.org

Notes from published material

=== Human metabolism and deficiency === Molybdenum is an essential trace dietary element. Four mammalian Mo-dependent enzymes are known, all of them harboring a pterin-based molybdenum cofactor (Moco) in their active site: sulfite oxidase, xanthine oxidoreductase, aldehyde oxidase, and mitochondrial amidoxime reductase. People severely deficient in molybdenum have poorly functioning sulfite oxidase and are prone to toxic reactions to sulfites in foods. The human body contains about 0.07 mg of molybdenum per kilogram of body weight, with higher concentrations in the liver and kidneys and lower in the vertebrae. Molybdenum is also present within human tooth enamel and may help prevent its decay. Acute toxicity has not been seen in humans, and the toxicity depends strongly on the chemical state. Studies on rats show a median lethal dose (LD50) as low as 180 mg/kg for some Mo compounds. Although human toxicity data is unavailable, animal studies have shown that chronic ingestion of more than 10 mg/day of molybdenum can cause diarrhea, growth retardation, infertility, low birth weight, and gout; it can also affect the lungs, kidneys, and liver. Sodium tungstate is a competitive inhibitor of molybdenum. Dietary tungsten reduces the concentration of molybdenum in tissues. Low soil concentration of molybdenum in a geographical band from northern China to Iran results in a general dietary molybdenum deficiency and is associated with increased rates of esophageal cancer.

Certain diseases' causation (such as neuronal pathologies, cancer, disturbed metabolic conditions, and autoimmune disorders) have been correlated to specific mutations of aminoacyl-tRNA synthetases. Charcot-Marie-Tooth (CMT) disease is the most frequent heritable disorder of the peripheral nervous system (a neuronal disease) and is caused by a heritable mutation in glycol-tRNA and tyrosyl-tRNA. Diabetes, a metabolic disease, induces oxidative stress, which triggers a build up of mitochondrial tRNA mutations. It has also been discovered that tRNA synthetases may be partially involved in the etiology of cancer. A high level of expression or modification of aaRSs has been observed within a range of cancers. A common outcome from mutations of aaRSs is a disturbance of dimer shape/formation which has a direct relationship with its function. These correlations between aaRSs and certain diseases have opened up a new door to synthesizing therapeutics.

Numerous events are hosted on the lawn at Bryant Park. Bryant Park Movie Nights, begun in the early 1990s, take place on Monday evenings during the summer. Various free musical performances are sponsored by corporations during months with warm weather, including Broadway in Bryant Park, sponsored by iHeartMedia and featuring performers from current Broadway musicals, integrated with content provided by event sponsors. The park has various activity areas open all day long, including board games, chess and backgammon, a putting green and Kubb area, an Art Cart, ping pong tables, and Petanque courts. The parks also offer free classes in juggling, yoga, tai chi, and knitting. In the 40th Street plaza of the park, there is a station called Bryant Park Games where visitors can borrow an array of games, including Chinese chess and quoits. In addition, chess and table tennis can also be played at Bryant Park. Food and drink are served at four park-operated concessionary kiosks. There are two additional kiosks on Fifth Avenue, bringing the total of concessionaires near Bryant Park to six.

== Combination hemoglobinopathies == A combination hemoglobinopathy occurs when someone inherits two different abnormal hemoglobin genes. If these are different versions of the same gene, one having been inherited from each parent it is an example of compound heterozygosity. Both alpha- and beta- thalassemia can coexist with other hemoglobinopathies. Combinations involving alpha thalassemia are generally benign. Some examples of clinically significant combinations involving beta thalassemia include:

Sources: en.wikipedia.org

Further detail

==== Clay ==== The clay hypothesis was proposed by Graham Cairns-Smith in 1985. It postulates that complex organic molecules arose gradually on pre-existing, non-organic replication surfaces of silicate crystals in contact with an aqueous solution. The clay mineral montmorillonite has been shown to catalyze the polymerization of RNA in aqueous solution from nucleotide monomers, and the formation of membranes from lipids. In 1998, Hyman Hartman proposed that "the first organisms were self-replicating iron-rich clays which fixed carbon dioxide into oxalic acid and other dicarboxylic acids. This system of replicating clays and their metabolic phenotype then evolved into the sulfide rich region of the hot spring acquiring the ability to fix nitrogen. Finally phosphate was incorporated into the evolving system which allowed the synthesis of nucleotides and phospholipids."

== Laboratory scale == Centrifugal partition chromatography has been extensively used for isolation and purification of natural products for 40 years. Due to the ability to get very high selectivity, and the ability to tolerate samples containing particulated matter, it is possible to work with direct extracts of biomass, opposed to traditional liquid chromatography, where impurities degrade the solid stationary phase so that separation become impossible. There are numerous laboratory scale centrifugal partition chromatography manufacturers around the world, like Gilson (Armen Instrument), Kromaton (Rousselet Robatel), and AECS-QUIKPREP. These instruments operate at flow rates of 1–500 mL/min. with stationary phase retentions of 40–80%. With the new rotor system created after 2022, LiLiChro was able to create a truly analytical instrument (miniLiLi) with a rotor internal volume of only 34ml, which means it can operate at a flow rate of 1ml/min. On the other hand, both the miniLiLi and the 140ml midiLiLi can operate with 90+% stationary phase retention.

Dominant genes associated with PD but now believed unlikely to be pathogenic include HTRA2, UCHL1 (PARK5), GIGYF2 (PARK11), and EIF4G1. Autosomal recessive genes include PRKN (PARK2, PARKIN), PINK1 (PARK6), PARK7 (DJ-1), ATP13A2 (PARK9), PLA2G6 (PARK14, IPLA2), FBXO7 (PARK15, FBX7), DNAJC6 (PARK19, DJC6), SYNJ1 (PARK20), and VPS13C (PARK23). Most common risk genes (like GBA) affect both sexes equally. The overall genetic risk for PD appears to be similar for males and females. However, there are sex- and gender-related differences between men and women in PD clinical features, disease development and response to treatment. Men are consistently found to have a higher occurrence of Parkinson's disease, with an estimated prevalence rate 1.5 times greater among males than females across all ages. These differences appear to reflect complex interactions among hormones, gene regulation, and other biological, environmental and sociocultural factors. Some sex-linked factors may differently affect brain activity and dopamine pathways. In adult males, the SRY gene (Sex-determining Region on the Y chromosome) is involved in regulation of dopamine, and SRY overactivity may increase PD risk. In women, hormones such as estrogen have been suggested to have a protective effect against PD, but little research has been done.

The Hippocratic Oath for physicians, attributed to fifth century BC Greece, refers to the existence of "deadly drugs", and ancient Greek physicians imported drugs from Egypt and elsewhere. The pharmacopoeia De materia medica, written between 50 and 70 CE by the Greek physician Pedanius Dioscorides, was widely read for more than 1,500 years.

== Degradation == Polystyrene is relatively chemically inert. While it is waterproof and resistant to breakdown by many acids and bases, it is easily attacked by many organic solvents (e.g. it dissolves quickly when exposed to acetone), chlorinated solvents, and aromatic hydrocarbon solvents. Because of its resilience and inertness, it is used for fabricating many objects of commerce. Like other organic compounds, polystyrene burns to give carbon dioxide and water vapor, in addition to other thermal degradation by-products. Polystyrene, being an aromatic hydrocarbon, typically combusts incompletely as indicated by the sooty flame. The process of depolymerizing polystyrene into its monomer, styrene, is called pyrolysis. This involves using high heat and pressure to break down the chemical bonds between each styrene compound. Pyrolysis usually goes up to 430 °C (806 °F). The high energy cost of doing this has made commercial recycling of polystyrene back into styrene monomer difficult.

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.

How is a sample checked for identity?

Laboratory confirmation typically combines retention time matching on a chromatographic system with mass measurement. A reference standard of known identity is needed for a meaningful comparison. Sequence-level techniques can add further confirmation.

Network