This is a working overview of MC4R agonist, written for readers who want more than a one-paragraph summary but less than a textbook.
This page was last updated on 2026-04-30 and is reviewed periodically as new material appears.
Across literature and commercial listings, the substance appears under several names, including bremelanotide, PT-141, and various brand designations. A CAS registry number provides a unique identifier for the compound, aiding retrieval from chemical databases. Synonym lists may also contain early development codes and descriptive chemical names. When consulting sources, researchers need to confirm that the cited names refer to the same molecular structure to avoid confusion. Naming consistency matters especially when comparing analytical data across publications.
PT-141 is a synthetic cyclic heptapeptide whose development code is bremelanotide. It belongs to the class of melanocortin receptor agonists and acts by mimicking endogenous peptide hormones. The compound originated from research on melanotan II, where investigators exploring derivatives found distinct pharmacological features. Unlike the parent compound, PT-141 showed effects on pathways related to sexual desire and function in early studies, prompting its development as a separate candidate. Its molecular design aimed to separate receptor activity from pigmentary effects.
How receptor activation translates into a change in desire is not established in detail. Proposed steps include modulation of dopaminergic signalling in reward circuits and downstream effects on autonomic tone. Human data consist mainly of clinical trials measuring self-reported outcomes rather than direct measurements of brain activity or transmitter release. The transient rise in blood pressure sometimes observed after administration is likewise reported consistently but explained only partly by known melanocortin pathways.
Melanocortin receptors form a family of five G-protein-coupled proteins, labelled MC1R through MC5R, that respond to peptides derived from pro-opiomelanocortin. Alpha-melanocyte-stimulating hormone and adrenocorticotropic hormone are the best-known endogenous ligands. The receptors are distributed differently across tissues, so a single agonist can produce effects in the brain, skin, adrenal gland and vasculature. This distribution explains why one peptide can influence both pigmentation and motivated behaviour.
Bremelanotide is a cyclic heptapeptide that binds several melanocortin receptors rather than one. In vitro assays report agonist activity at MC1R, MC3R, MC4R and MC5R, with MC4R generally treated as the subtype most relevant to sexual effects. MC4R is expressed in hypothalamic nuclei involved in appetite, energy balance and motivated behaviour, which provides a plausible route for central action. Selective MC4R agonists studied in animals produce comparable behavioural changes, supporting that interpretation.
| Property | Value | Notes |
|---|---|---|
| Chemical class | Cyclic peptide | Melanocortin receptor agonist family |
| Molecular weight | Approximately 1025 Da | Free base form |
| Appearance | White to off-white powder | Lyophilized product |
| Solubility | Soluble in water | Also dissolves in polar organic solvents |
| Storage temperature | -20 degrees Celsius | Dry and protected from light |
After subcutaneous administration, plasma concentrations rise within roughly thirty minutes and the elimination half-life is short, on the order of two to three hours. Reported physiological responses include transient increases in blood pressure and nausea, which tended to diminish with repeated dosing in trial settings. Because the peptide clears quickly, effects are not expected to persist long after a dose. Absorption from non-injected routes is poorly characterised, and nasal delivery produced variable plasma levels in older work.
Clinical research typically uses randomised, double-blind, placebo-controlled designs. The most common primary endpoint is the desire domain score of the Female Sexual Function Index, sometimes paired with a distress measure. Secondary outcomes include arousal, satisfaction, and event-based counts of satisfying sexual episodes. Across trials, average improvements are modest and individual responses vary widely. Whether benefits persist beyond a few months, and whether they depend on baseline hormone status, remain open questions rather than settled findings.
Melanocortin receptors form a family of five G-protein-coupled receptors designated MC1 through MC5. Bremelanotide binds most strongly at MC4R and MC1R, with weaker activity reported at MC3R and MC5R. MC4R is expressed in hypothalamic nuclei that coordinate energy balance and aspects of sexual behaviour. The prevailing interpretation is that central MC4R activation, rather than peripheral vascular effects alone, drives the reported changes in desire. This account remains partly inferential, since direct receptor-level measurement in living humans is not practical.
Handling procedures emphasize minimizing moisture uptake, since the dried solid is hygroscopic and can draw water when warmed to room temperature before a vial is opened. Laboratories record lot number, purity, counter-ion content, and residual solvent data supplied by the producer. Impurity profiles are compared run to run, and any shift in retention time or peak shape prompts re-verification against a reference standard. Certificates of analysis are treated as claims to be checked rather than accepted at face value.
Identity and purity testing for this peptide typically relies on reversed-phase high-performance liquid chromatography with ultraviolet detection, reported as area-percent purity. Mass spectrometry, usually in tandem mode, confirms molecular mass and supports quantification in biological matrices. Sequence confirmation may use peptide mapping after enzymatic digestion, while nuclear magnetic resonance and circular dichroism supply supplementary structural detail. No single technique establishes identity alone, so laboratories compare retention time, mass, and fragment pattern against a verified reference standard.
Bremelanotide acts as a non-selective agonist at melanocortin receptors, with reported activity at MC1R, MC3R, MC4R and MC5R. The proposed basis for its central effects is activation of MC4R populations in the hypothalamus, a region associated with appetite and reproductive signalling. Because the peptide carries a net positive charge and polar side chains, it does not cross biological membranes freely, which is one reason oral administration is not the standard route. Effects generally appear within an hour of parenteral administration and are described as centrally mediated rather than peripheral.
Bremelanotide, developed under the code PT-141, is a synthetic cyclic heptapeptide analogue of alpha-melanocyte-stimulating hormone. Its structure is Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH, with a lactam bridge joining the aspartate and lysine side chains. The molecule has the formula C50H68N14O10 and a monoisotopic mass near 1025 daltons. It is commonly prepared as the acetate salt and appears as a white to off-white lyophilised powder in solid form. The free acid is the pharmacologically relevant species, while the counter-ion improves handling and dissolution.
It is a bioactive sphingoid which derives from the sphinganine. It is formed by a sphingoid and an amino alcohol and it constitutes the conjugated base of 1-deoxymethylsphinganine (1+). Its role is accepting a hydron from a donor via its organic amino compound; it is a Brønsted base. It is also known as deoxymethyl-SA, (2R)-1-aminoheptadecan-2-ol and 1-desoxymethylsphinganine. The molecular weight of this compound is 271,48 g/mol and its molecular formula is C17H37NO, which means it has 17 carbons. In relation to its appearance, it has a powder form. Other physical and chemical properties are not certainly known.
42. Adv Gerontol. 2004;14:105-13. [The influence of substances revealing geroprotective of spontaneous carcinogenesis in mice]. [Article in Russian] Popovich IG. The review presents the results of experimental studies conducted by the author. CBA, SHR, HER-2/neu and SAM mice revealed inhibition of age-related alterations in estrus function and spontaneous tumour development and showed life span extension under the influence of the pineal gland hormone Melatonin, synthetic peptide bioregulator Epitalon, delta-sleep-inducing peptide Deltaran, enterosorbent Aqualen and succinic acid containing preparation Neuronol (Noogam). The observed effect depended on the dose and conditions of administration, as well as genetic predisposition of the particular mice strains to tumour development.
The period from 1958 to 1968 saw tremendous growth in aviation. Improvements in aviation safety and accident investigation procedures were rapidly advancing. In 1963, the Civil Aeronautics Board, under the leadership of then Deputy Director Bobbie R. Allen, established the National Aircraft Accident Investigation School in Oklahoma City. The ICAO's third accident investigation division meeting, held in Montreal, Canada, in January 1965, laid the foundation for accident investigations throughout the world. The proposals were presented by the Director of the Civil Aeronautics Board Bureau of Safety, Bobbie R. Allen, who headed the U.S. delegation. The U.S. formally adopted the proposals at the White House on December 1, 1965. The top 10 countries with the highest number of fatal civil airliner accidents from 1945 to 2021 are the United States, Russia, Canada, Brazil, Colombia, United Kingdom, France, Indonesia, Mexico, and India. The United Kingdom is noted to have the highest number of air crashes in Europe, with a total of 110 air crashes within the time period, and Indonesia is the highest in Asia at 104, followed by India at 95.
Patients with Type II diabetes will have elevated glucagon levels during a fast and after eating. These elevated glucagon levels over stimulate the liver to undergo gluconeogenesis, leading to elevated blood glucose levels. Consistently high blood glucose levels can lead to organ damage, neuropathy, blindness, cardiovascular issues and bone and joint problems. It is not entirely clear why glucagon levels are so high in patients with Type II diabetes. One theory is that the alpha cells have become resistant to the inhibitory effects of glucose and insulin and do not respond properly to them. Another theory is that nutrient stimulation of the gastrointestinal tract, thus the secretion of gastric inhibitory polypeptide and Glucagon-like peptide-1, is a very important factor in the elevated secretion of glucagon.
Proteins consist of chains of amino acids which spontaneously fold to form the three dimensional (3-D) structures of the proteins. The 3-D structure is necessary to understanding the biological function of the protein. Protein structures can be determined experimentally through techniques such as X-ray crystallography, cryo-electron microscopy and nuclear magnetic resonance (NMR), which are all expensive and time-consuming. Such efforts, using the experimental methods, have identified the structures of about 170,000 proteins over the last 60 years, while there are over 200 million known proteins across all life forms. Over the years, researchers have applied numerous computational methods to predict the 3D structures of proteins from their amino acid sequences, accuracy of such methods in best possible scenario is close to experimental techniques (NMR) by the use of homology modeling based on molecular evolution. CASP, which was launched in 1994 to challenge the scientific community to produce their best protein structure predictions, found that GDT scores of only about 40 out of 100 can be achieved for the most difficult proteins by 2016. AlphaFold started competing in the 2018 CASP using an artificial intelligence (AI) deep learning technique.
Sources: en.wikipedia.org
A chromogranin A-derived antifungal peptide (CGA 47–66, chromofungin) when embedded on a surface has been shown to have antifungal activity by interacting with the fungal membrane and thereby penetrating the cell. Additionally, in vitro studies have demonstrated that such an antifungal coating can inhibit the growth of yeast Candida albicans by 65% and completely stop the proliferation of filamentous fungus Neurospora crassa. Copper and copper alloy surfaces have demonstrated a die-off of Aspergillus spp., Fusarium spp., Penicillium chrysogenum, Aspergillus niger and Candida albicans fungal spores. Hence, the potential to help prevent the spread of fungi that cause human infections by using copper alloys (instead of non-antifungal metals) in air conditioning systems is worthy of further investigation. The physical topology of a surface will determine the viable environment for bacteria. It may affect a microbe's ability to adhere to its surface. Textile surfaces tend to be very easy for microbes to adhere to due to the abundance of interstitial spacing between fibers.
The structure of prolactin is similar to that of growth hormone and placental lactogen. The molecule is folded due to the activity of three disulfide bonds. Significant heterogeneity of the molecule has been described, thus bioassays and immunoassays can give different results due to differing glycosylation, phosphorylation and sulfation, as well as degradation. The non-glycosylated form of prolactin is the dominant form that is secreted by the pituitary gland. The three different sizes of prolactin are:
Individuals with 3-M syndrome have severe prenatal growth retardation due to growth delays during fetal development resulting in a low birth weight. Growth delays continue after birth throughout childhood and adolescence, ultimately leading to a short stature. Growth delays and immature bone development (growth retardation and delayed bone maturation) typically continue after birth (postnatally), leading to short stature (dwarfism) with proportional development of the arms and legs (as opposed to short stature with abnormally small arms and legs). In most cases, infants with 3M syndrome are unusually small and have a low birth weight despite being carried to term.
Dual-flow, also known as dual, countercurrent chromatography occurs when both phases are flowing in opposite directions inside the column. Instruments are available for dual-flow operation for both Hydrodynamic and hydrostatic CCC. Dual-flow countercurrent chromatography was first described by Yoichiro Ito in 1985 for foam CCC where gas-liquid separations were performed. Liquid–liquid separations soon followed. The countercurrent chromatography instrument must be modified so that both ends of the column have both inlet and outlet capabilities. This mode may accommodate continuous or sequential separations with the sample being introduced in the middle of the column or between two bobbins in a hydrodynamic instrument. A technique called intermittent countercurrent extraction (ICcE) is a quasi-continuous method where the flow of the phases is alternated "intermittently" between normal and reversed-phase elution so that the stationary phase also alternates.
Sources: en.wikipedia.org
It belongs to the melanocortin receptor agonist family of peptides. Its cyclic structure distinguishes it from linear peptides and shapes its receptor binding profile.
It emerged from research on melanotan II. Investigators exploring derivatives observed distinct pharmacological features related to sexual function.
Common names include bremelanotide and PT-141. Chemical databases may also list early development codes and descriptive names.
Bremelanotide binds several melanocortin receptors, and MC4R is the subtype most often cited as responsible for its behavioural effects. Activity at MC1R, MC3R and MC5R is also reported. Selectivity is therefore described as limited rather than precise.