Everything below concerns afamelanotide. We keep the language plain, cite what the science says, and separate well-supported claims from open questions.
Last reviewed on 2025-08-01. Where a claim depends on a specific study, the study is described rather than over-claimed.
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.
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.
| Property | Value | Notes |
|---|---|---|
| Molecular formula | C50H69N15O9 | Cyclic heptapeptide, C-terminally amidated |
| Approximate molecular mass | 1024 Da | Monoisotopic mass of the free peptide |
| Appearance | White to off-white powder | Typically supplied as a lyophilised solid |
| Solubility class | Soluble in water and polar solvents | Also dissolves in neutral aqueous buffer |
| Common synonyms | Melanotan II, MT-II, MT-2 | Described as a melanocortin agonist in early literature |
== External links == Overview of all the structural information available in the PDB for UniProt: P06241 (Human Tyrosine-protein kinase Fyn) at the PDBe-KB. Overview of all the structural information available in the PDB for UniProt: P39688 (Mouse Tyrosine-protein kinase Fyn) at the PDBe-KB.
Radium has 33 known isotopes with mass numbers from 202 to 234, all of which are radioactive. Four of these – 223Ra (half-life 11.4 days), 224Ra (3.64 days), 226Ra (1600 years), and 228Ra (5.75 years) – occur naturally in the decay chains of primordial thorium-232, uranium-235, and uranium-238 (223Ra from uranium-235, 226Ra from uranium-238, and the other two from thorium-232). These isotopes nevertheless still have half-lives too short to be primordial radionuclides, and only exist in nature from these decay chains. Together with the mostly artificial 225Ra (15 d), which occurs in nature only as a decay product of minute traces of neptunium-237, these are the five most stable isotopes of radium. All other 27 known radium isotopes have half-lives under two hours, and the majority have half-lives under a minute. Of these, 221Ra (half-life 28 s) also occurs as a 237Np daughter, and 220Ra and 222Ra would be produced by the still-unobserved double beta decay of natural radon isotopes. At least 12 nuclear isomers have been reported, the most stable of which is radium-205m with a half-life between 130~230 milliseconds; this is still shorter than twenty-four ground-state radium isotopes. 226Ra is the most stable isotope of radium and is the last isotope in the (4n + 2) decay chain of uranium-238 with a half-life of over a millennium; it makes up almost all of natural radium. Its immediate decay product is the dense radioactive noble gas radon (specifically the isotope 222Rn), which is responsible for much of the danger of environmental radium.
== Definition == Stimulant is an overarching term that covers many drugs including those that increase the activity of the central nervous system and the body, drugs that are pleasurable and invigorating, or drugs that have sympathomimetic effects. Sympathomimetic effects are those effects that mimic or copy the actions of the sympathetic nervous system. The sympathetic nervous system is a part of the nervous system that prepares the body for action, such as increasing the heart rate, blood pressure, and breathing rate. Stimulants can activate the same receptors as the natural chemicals released by the sympathetic nervous system (namely epinephrine and norepinephrine) and cause similar effects. Psychostimulant refers to a subset of substances within the stimulant drug class that act at the dopamine transporter (DAT), a protein that normally clears dopamine from the synaptic cleft. Amphetamine, methylphenidate, cocaine, and modafinil are examples of psychostimulants that promote arousal and affect task performance in a dose-dependent manner. Psychostimulants act at DAT by inhibiting dopamine reuptake or by initiating transporter-mediated dopamine efflux (i.e., reverse transport), thereby producing indirect dopamine agonist effects in the central nervous system. The DAT-mediated actions of psychostimulants contrast with other central nervous system stimulants that can overlap in behavioural effects, such as caffeine, a drug that promotes wakefulness primarily through antagonism of adenosine receptors.
=== Glycogen synthesis === The phosphorylation of glucose to glucose 6-phosphate has role in regulating glycogen synthase. Glucose is phosphorylated to glucose 6-phosphate to allow its transport across the membrane by ATP-D-glucose 6-phosphotransferase and non-specific hexokinase (ATP-D-hexose 6-phosphotransferase). Liver cells are freely permeable to glucose, and the initial rate of phosphorylation of glucose is the rate-limiting step in glucose metabolism by the liver. The liver's crucial role in controlling blood sugar concentrations by breaking down glucose into carbon dioxide and glycogen is characterized by the negative Gibbs free energy (ΔG) value, which indicates that this is a point of regulation with. The hexokinase enzyme has a low Michaelis constant (Km), indicating a high affinity for glucose, so this initial phosphorylation can proceed even when glucose levels at nanoscopic scale within the blood. The phosphorylation of glucose can be enhanced by the binding of fructose 6-phosphate (F6P), and lessened by the binding fructose 1-phosphate (F1P). Fructose consumed in the diet is converted to F1P in the liver. This negates the action of F6P on glucokinase, which ultimately favors the forward reaction. The capacity of liver cells to phosphorylate fructose exceeds capacity to metabolize fructose-1-phosphate. Consuming excess fructose ultimately results in an imbalance in liver metabolism, which indirectly exhausts the liver cell's supply of ATP.
== Cross-linking with hemoglobin-albumin == Disuccinimidyl suberate's reactivity toward primary amines allows it to serve as a cross-linking agent for proteins, without toxic side-products and forming peptide bonds with the lysine residues in a single step. In a study on blood substitutes, DSS was shown to cross-link Hemoglobin intramolecularly, yielding a relatively stable protein (polymerized Hb or polyHb), whose oxygen affinity was almost halved compared to that of native Hb. This was shown to be reversed when Hemoglobin was copolymerized with bovine serum albumin (BSA), showing very little change in auto-oxidation and oxygen affinity compared to the native Hb.
Sources: en.wikipedia.org
== Contraindications == Levothyroxine is contraindicated in people with hypersensitivity to levothyroxine sodium or any component of the formulation, people with acute myocardial infarction, and people with thyrotoxicosis of any etiology. Levothyroxine is also contraindicated for people with uncorrected adrenal insufficiency, as thyroid hormones may cause an acute adrenal crisis by increasing the metabolic clearance of glucocorticoids. For oral tablets, the inability to swallow capsules is an additional contraindication.
On February 9, 1909, the Smoking Opium Exclusion Act, "to prohibit the importation and use of opium for other than medicinal purposes", became the first US federal law to ban the non-medical use of a substance. This was soon followed by the Harrison Narcotics Tax Act of 1914, that regulated and taxed the production, importation, and distribution of opiates and coca products. Amending the Smoking Opium Exclusion Act, the Anti-Heroin Act of 1924 specifically outlawed the manufacture, importation and sale of heroin. During World War I (1914–1918), soldiers were commonly treated with morphine, giving rise to addiction among veterans. An international wartime focus on military use of opiates and cocaine for medical treatment and performance enhancement, and concern over potential abuse, led to the global adoption of the International Opium Convention, through its incorporation into the Treaty of Versailles in 1919, with administration by the newly established League of Nations. The treaty, originally formulated in 1912 but not widely implemented, became the basis of current international drug control policy. It was initially concerned with regulating the free trade of drugs, without affecting production or use, and in 1920, it established the Opium Advisory Committee (OAC). The US, one of the most prohibitionist countries, felt these provisions did not go far enough in restricting drugs. In 1919, the 18th Amendment to the US Constitution was ratified, prohibiting the manufacture, sale and transportation of "intoxicating liquors", with exceptions for religious and medical use.
==== IR spectroscopy ==== One case study investigated the formation of gaseous intermediates in the decomposition of CCl4 in the presence of steam over La2O3 using Fourier-transform infrared spectroscopy. This experiment produced useful information about the reaction mechanism, active site orientation, and about which species compete for the active site.
Selenium disulfide has a composition that approximates to SeS2 and is sometimes called selenium sulfide. However, as used in proprietary formulations, it is not a pure chemical compound but a mixture of eight-membered-ring compounds where the overall Se:S ratio is 1:2. The specific chemicals contain a variable number of S and Se atoms, SenS8−n. Many selenium sulfides are known, as indicated by 77Se-NMR spectroscopy.
Sources: en.wikipedia.org
== Associations with national cuisines == In the United States, fried ice cream has been associated with Asian cuisine, appearing in reviews of Chinese, Japanese, and Polynesian restaurants in the "Dining Out" section of the New York Times in the 1970s.
== The TRAIL receptors as a drug target == In clinical trials only a small proportion of cancer patients responded to various drugs that targeted TRAIL death receptors. Many cancer cell lines develop resistance to TRAIL and limits the efficacy of TRAIL-based therapies.
In 1924, Louis de Broglie proposed that all particles—particularly subatomic particles such as electrons—have an associated wave. Erwin Schrödinger, fascinated by this idea, developed an equation that describes an electron as a wave function instead of a point. This approach predicted many of the spectral phenomena that Bohr's model failed to explain, but it was difficult to visualize, and faced opposition. One of its critics, Max Born, proposed instead that Schrödinger's wave function did not describe the physical extent of an electron (like a charge distribution in classical electromagnetism), but rather gave the probability that an electron would, when measured, be found at a particular point. This reconciled the ideas of wave-like and particle-like electrons: the behavior of an electron, or of any other subatomic entity, has both wave-like and particle-like aspects, and whether one aspect or the other is observed depend upon the experiment. Schrödinger's wave model for hydrogen replaced Bohr's circular orbits with atomic orbitals giving only the probability of finding an electron at positions around the nucleus. The orbitals come in a variety of shapes depending on their energy level and angular momentum. The shapes of atomic orbitals are found by solving the Schrödinger equation. Analytic solutions of the Schrödinger equation are known for the hydrogen atom and hydrogen-like atoms such as the hydrogen molecular ion. Beginning with the helium atom—which contains just two electrons—numerical methods are used to solve the Schrödinger equation.
Amines, alkyl and aryl alike, are organized into three subcategories (see table) based on the number of carbon atoms adjacent to the nitrogen (how many hydrogen atoms of the ammonia molecule are replaced by hydrocarbon groups): Primary (1°) amines—Primary amines arise when one of three hydrogen atoms in ammonia is replaced by an alkyl or aromatic group. Important primary alkyl amines include methylamine, most amino acids, and the buffering agent tris, while primary aromatic amines include aniline. Secondary (2°) amines—Secondary amines have two organic substituents (alkyl, aryl or both) bound to the nitrogen together with one hydrogen. Important representatives include dimethylamine, while an example of an aromatic amine would be diphenylamine. Tertiary (3°) amines—In tertiary amines, nitrogen has three organic substituents. Examples include trimethylamine, which has a distinctively fishy smell, and EDTA. A fourth subcategory is determined by the connectivity of the substituents attached to the nitrogen:
== Method translation == Faster GC methods have shorter times but Kovats indices of the compounds may be conserved if proper method translation is applied. Temperatures of the temperature program stay the same, but ramps and times change when using a smaller column or faster carrier gas. If column dimensions Length×diameter×film are divided by 2 and gas velocity is doubled by using H2 in place of Helium, the hold times must be divided by 4 and the ramps must be multiplied by 4 to keep the same index and the same retention temperature for the same compound analyzed. Method translation rules are incorporated in some chromatography data systems.
Sources: en.wikipedia.org
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.
Afamelanotide is the linear analogue [Nle4-D-Phe7]-alpha-MSH, sometimes called melanotan I, while melanotan II is cyclic and carries three further substitutions. The two are distinct molecules and are not interchangeable in analytical testing.
Binding to the four melanocortin receptor subtypes is well documented in vitro. The relative contribution of each subtype to whole-body effects in humans is far less certain.
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.