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Melanotan-2 Identity And Receptor Pharmacology — Reference Sheet

By Editorial Desk · published 2026-04-12 · last reviewed 2026-05-02 · Guide

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

Last reviewed on 2026-05-02. 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.

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.

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.

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

Notes from published material

There is a trend towards prohibition of beak trimming in Europe over the course of decades. Analysts expect the practice to be gradually banned across the continent. EU law allows member states to debeak poultry according to two regulations: Directive 1999/74/EC for laying hens allows beak trimming, while Directive 2007/43/EC for broilers permits beak trimming only in certain cases. As of April 2019, 80% of laying hens in the EU were estimated to be beak-trimmed.

In a complementary technique, peptide mass fingerprinting involves digestion of the native and modified protein with a protease such as trypsin. This will produce a set of peptides that can be analysed using a mass spectrometer. The peptide that changes in mass after reaction with the inhibitor will be the one that contains the site of modification.

== Uses == The compound is a highly reactive, versatile chemical used in synthesizing polymers, agrochemicals, and advanced materials, notably acting as a linker in click chemistry for drug discovery.

=== Foreign === Order of the Most Holy Annunciation (Kingdom of Italy). Order of Saints Maurice and Lazarus (Kingdom of Italy). Order of the Crown of Italy (Kingdom of Italy). Order of Saint Januarius (Royal House of Bourbon-Two Sicilies) Sacred Military Constantinian Order of Saint George (Royal House of Bourbon-Two Sicilies) Imperial Order of Dom Pedro I (The Imperial House of Brazil) The Imperial Order of the Rose (The Imperial House of Brazil) Order of the Immaculate Conception of Vila Viçosa (Royal House of Braganza of Portugal) Bailiff’s Cross of the Order of Malta (Sovereign Military Order of Malta). National Order of the Legion of Honour in the rank of Commander (Republic of France). Jubilee medal on the occasion of the 50th birthday of HM King Carl XVI Gustaf, Kingdom of Sweden Jubilee medal on the occasion of the 70th birthday of HM King Carl XVI Gustaf, Kingdom of Sweden

The second type of browning, non-enzymatic browning, is a process that also produces the brown pigmentation in foods but without the activity of enzymes. The two main forms of non-enzymatic browning are caramelization and the Maillard reaction. Both vary in the reaction rate as a function of water activity (in food chemistry, the standard state of water activity is most often defined as the partial vapor pressure of pure water at the same temperature). Caramelization is a process involving the pyrolysis of sugar. It is used extensively in cooking for the desired nutty flavor and brown color. As the process occurs, volatile chemicals are released, producing the characteristic caramel flavor.

Sources: en.wikipedia.org

Related pages on this site

Background from the literature

===== Treatment ===== Because there are no medications with an approved indication for cocaine use disorder, psychosocial treatments are the current standard. Effective approaches include group and individual counseling, cognitive behavioral therapy (CBT), and motivational interviewing (MI). Contingency management (CM)—which rewards patients with vouchers for meeting treatment goals—has proven especially effective, particularly for helping patients achieve initial abstinence from cocaine.

== Products and services == Eurogentec has developed three interrelated business units, Life Science Research Products and Services, In Vitro Diagnostics Manufacturing Solutions, and GMP Biomanufacturing.

It has been suggested that the same may have been true for clomipramine and other TCAs. Nonetheless, there is little doubt that many may, indeed, benefit from much higher doses. 250 mg/d, as mentioned elsewhere, is the typical maximum recommended dose but some people may need as much as 300 mg/d or more to benefit from all clomipramine has to offer beyond its potent SNRI capacity alone.

Certain drugs that have been introduced for uses other than analgesics are also used in pain management. Both first-generation (such as amitriptyline) and newer antidepressants (such as duloxetine) are used alongside NSAIDs and opioids for pain involving nerve damage and similar problems. Other agents directly potentiate the effects of analgesics, such as using hydroxyzine, promethazine, carisoprodol, or tripelennamine to increase the pain-killing ability of a given dose of opioid analgesic. Adjuvant analgesics, also called atypical analgesics, include orphenadrine, mexiletine, pregabalin, gabapentin, cyclobenzaprine, hyoscine (scopolamine), and other drugs possessing anticonvulsant, anticholinergic, and/or antispasmodic properties, as well as many other drugs with CNS actions. These drugs are used along with analgesics to modulate and/or modify the action of opioids when used against pain, especially of neuropathic origin. Dextromethorphan has been noted to slow the development of and reverse tolerance to opioids, as well as to exert additional analgesia by acting upon NMDA receptors, as does ketamine. Some analgesics such as methadone and ketobemidone and perhaps piritramide have intrinsic NMDA action. The anticonvulsant carbamazepine is used to treat neuropathic pain. Similarly, the gabapentinoids gabapentin and pregabalin are prescribed for neuropathic pain, and phenibut is available without prescription. Gabapentinoids work as α2δ-subunit blockers of voltage-gated calcium channels, and tend to have other mechanisms of action as well.

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 II identical to alpha-melanocyte-stimulating hormone?

No. It is a synthetic analogue carrying four amino acid changes, a lactam ring and an amidated C-terminus. The natural hormone is a linear thirteen-amino-acid peptide processed from proopiomelanocortin.

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