If you have been reading about MC4 receptor and want a single page that covers the useful parts, this is it: definitions, context, how it is studied, and the questions that come up repeatedly.
Last reviewed on 2026-05-24. Where a claim depends on a specific study, the study is described rather than over-claimed.
Development of the peptide passed through several delivery formats, including an intranasal version tested in early trials and an injectable version that entered later clinical study. Regulatory approval for a subcutaneous product in the United States was granted in 2019 after review of controlled trials in premenopausal women. Outside the clinic, the compound circulates in research and non-pharmaceutical markets under its code name, where identity and purity vary considerably between suppliers. Synonyms appearing across technical literature include bremelanotide, PT-141, and Palatin 141.
PT-141 is the research designation for bremelanotide, a synthetic cyclic heptapeptide developed as a melanocortin receptor agonist. The peptide contains seven amino acids with an internal lactam bridge that constrains the backbone into a stable ring. Cyclisation of this kind improves resistance to enzymatic degradation relative to linear analogues. The compound was first explored for effects on melanin production, because several melanocortin receptors influence pigmentation. Its later association with sexual desire emerged from observations made during that early work, and the molecule became the subject of a separate development programme.
Clinical development of bremelanotide proceeded through several reformulation attempts. An early intranasal version was discontinued, and a subcutaneous auto-injector formulation later received approval for hypoactive sexual desire disorder in premenopausal women. Approval decisions have varied by country and over time, and the product has not been universally adopted. Blood pressure elevation is a documented effect, which is why some jurisdictions require monitoring after administration. The clinical evidence base continues to evolve as additional studies are published.
Bremelanotide is a cyclic heptapeptide that acts as an agonist at melanocortin receptors. It binds MC1R, MC3R, MC4R, and MC5R, with MC4R activation considered most relevant to sexual desire pathways in the central nervous system. The molecule is a synthetic analog of alpha-melanocyte-stimulating hormone, a naturally occurring peptide involved in pigmentation and energy regulation. Early research explored its use in tanning before attention shifted toward sexual dysfunction applications. Receptor binding affinity varies across these subtypes.
Activation of MC4R in the hypothalamus is thought to influence dopaminergic signaling, which in turn affects arousal and desire. This mechanism differs from that of phosphodiesterase type 5 inhibitors, which act primarily on vascular smooth muscle in the genital region. Because the pathway is central rather than peripheral, effects are not strictly dependent on local blood flow. The precise downstream cascade linking receptor binding to behavioral outcomes remains an area of ongoing investigation.
| Property | Value | Notes |
|---|---|---|
| Chemical class | Cyclic heptapeptide | Synthetic melanocortin analogue |
| Molecular formula | C50H68N14O10 | Corresponds to a mass near 1025 daltons |
| Appearance | White to off-white powder | Lyophilised solid before reconstitution |
| Solubility | Soluble in water and polar solvents | Poor solubility in nonpolar media |
| Common synonyms | Bremelanotide, PT-141 | Code name and international name used interchangeably |
Whether the behavioral effect originates centrally, peripherally, or through both remains an active question. Animal experiments using receptor antagonists and site-specific injections point toward hypothalamic melanocortin circuits as a key locus, but translating those findings to humans is not straightforward. Blood pressure changes observed in trials suggest a vascular component that may be peripherally mediated. The relationship between receptor occupancy and reported effect has not been mapped in humans, and no validated biomarker predicts response. This gap makes it difficult to explain individual variability on pharmacological grounds alone.
Bremelanotide acts as an agonist at melanocortin receptors, a family of five G-protein-coupled receptors labeled MC1 through MC5. Binding studies indicate activity at several of these subtypes rather than strict selectivity for one. Signalling proceeds mainly through Gs-mediated activation of adenylyl cyclase, raising intracellular cyclic AMP. The MC4 receptor, expressed in hypothalamic and limbic circuits, is widely regarded as the subtype most relevant to sexual response. Because the molecule is not subtype-selective, effects at other melanocortin receptors are expected and are used to explain some observed side effects.
The peptide contains seven amino acids arranged in a ring, closed by a lactam bridge between a side-chain acid and an amine. This cyclic constraint holds the backbone in a defined conformation and increases resistance to enzymatic breakdown relative to linear analogs. N-terminal acetylation and a C-terminal amide further protect the molecule from exopeptidases. The result is a compound with a comparatively long circulation time for a small peptide. Structural modification of the bridge alters receptor affinity, which is one reason analogs in this family differ in their subtype preferences.
The lactam ring that closes the peptide backbone improves resistance to exopeptidase attack, but the molecule stays susceptible to hydrolysis and oxidation once dissolved. Degradation accelerates with temperature, extreme pH, and light exposure, and repeated freeze-thaw cycles promote aggregation and material loss. Lyophilized powder held desiccated at or below minus twenty degrees Celsius is the common way to keep reference material. Reconstituted solutions are generally kept cold and used within a short window because their stability is far lower than that of the dry solid.
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.
Regulatory status varies by jurisdiction, where approved prescription products, compounded preparations and research-grade material are treated as distinct categories with different documentation requirements. Suppliers of research material commonly issue a certificate of analysis listing purity, identity and sometimes endotoxin content. Independent verification by a third-party laboratory is often recommended because self-reported figures are difficult to check. Literature discussions usually state the source, purity and storage conditions of the material used, since these details affect reproducibility. Analysts note that a reported purity figure does not by itself describe biological activity.
Lyophilised peptide is generally held below minus twenty degrees Celsius, protected from light and moisture, because hydrolysis and oxidation accumulate faster at ambient temperature. Once reconstituted, solutions are typically kept between two and eight degrees Celsius and used within a short window defined by the supplier. Repeated freeze-thaw cycles are avoided since they promote aggregation and loss of soluble material. Container material matters as well, because peptides adsorb to certain plastics and glass surfaces at low concentration. Stability figures supplied by a vendor apply only to the specific lot and buffer that were tested.
Hot cathode gauges are accurate from 10−3 torr to 10−10 torr. The principle behind cold cathode version is the same, except that electrons are produced in a discharge created by a high voltage electrical discharge. Cold cathode gauges are accurate from 10−2 torr to 10−9 torr. Ionization gauge calibration is very sensitive to construction geometry, chemical composition of gases being measured, corrosion and surface deposits. Their calibration can be invalidated by activation at atmospheric pressure or low vacuum. The composition of gases at high vacuums will usually be unpredictable, so a mass spectrometer must be used in conjunction with the ionization gauge for accurate measurement.
Police Scotland arrest Scotland's former First Minister, Nicola Sturgeon, as part of their ongoing investigation into the SNP's finances. She is subsequently released without charge. 12 June Following a period of hot weather, thunderstorms and torrential rain bring flash flooding to parts of the UK. A mother-of-three is sentenced to 28 months in prison for inducing an abortion at home during 2020 with medication while she was 32–34 weeks pregnant. The medication was obtained following a remote consultation at which the woman misled doctors over the advancement of her pregnancy. 13 June 2023 Nottingham attacks: A major incident is declared in Nottingham, with much of the city centre cordoned off, following a vehicle-ramming and knife attack. A 31-year-old man is arrested on suspicion of multiple murders, following the deaths of three people including two university students, while three others are hospitalised. The first day of a public inquiry into the COVID-19 pandemic begins in central London. The inquiry's lead lawyer says "very little thought" was given about the impact of a national lockdown and that Brexit planning may have occupied too much of the government's time and resources, while a counsel for the Covid-19 Bereaved Families for Justice accuses the authorities of being "complacent". A heatwave is declared in several parts of the UK as temperatures reach 30 °C, and after exceeding 25 °C for three consecutive days; the UK's heat-health alert is also extended.
=== Protein sequencer === A protein sequenator is a machine that performs Edman degradation in an automated manner. A sample of the protein or peptide is immobilized in the reaction vessel of the protein sequenator and the Edman degradation is performed. Each cycle releases and derivatises one amino acid from the protein or peptide's N-terminus and the released amino-acid derivative is then identified by HPLC. The sequencing process is done repetitively for the whole polypeptide until the entire measurable sequence is established or for a pre-determined number of cycles.
=== Studies of folding with high time resolution === The study of protein folding has been greatly advanced in recent years by the development of fast, time-resolved techniques. Experimenters rapidly trigger the folding of a sample of unfolded protein and observe the resulting dynamics. Fast techniques in use include ultrafast mixing of solutions, photochemical methods, and laser temperature jump spectroscopy. Among the many scientists who have contributed to the development of these techniques are Heinrich Roder, Terry Oas, Harry Gray, Martin Gruebele, Brian Dyer, William Eaton, Sheena Radford, Chris Dobson, Alan Fersht, Bengt Nölting and Lars Konermann.
Shotwell (1922–1998), organic chemist Jean'ne Shreeve (born 1933), American organic chemist Dorothy Martin Simon (1919–2016), American physical chemist Susan Solomon (born 1956), Atmospheric chemist JoAnne Stubbe (born 1946), American biochemist Ida Noddack Tacke (1896–1978), German chemist and physicist Tsippy Tamiri (1952-2017), Israeli chemist Giuliana Tesoro (1921–2002), Polymer chemist Margaret Thatcher (1925–2013), British chemist and Prime Minister Jean Thomas, British biochemist (chromatin) Martha J. B. Thomas (1926–2006), Analytical chemist and chemical engineer Ann E. Weber, American organic/medicinal chemist Karen Wetterhahn (1948–1997), American metal toxicologist Ruth R. Wexler (born 1955), American organic and medicinal chemist, discoverer of two marketed drugs M. Christina White (born 1970), American organometallic chemist Charlotte Williams, English inorganic chemist Angela K. Wilson, American computational, theoretical, and physical chemist Ruby K. Worner (1900–1995), American chemist and textiles expert Rosalyn Sussman Yalow (1921–2011), American biochemist Jenara Vicenta Arnal Yarza (1902–1960), Spanish chemist Jean Youatt (born 1925), Australian chemist, biochemist, and microbiologist Ada Yonath (born 1939), Israeli crystallographer, Nobel prize in chemistry 2009 Glaci Zancan (1935–2007), Brazilian biochemist, president of the Brazilian Society for the Progress of the Science (SBPC) from 1999 to 2003
Sources: en.wikipedia.org
The regulation of cell adhesion The regulation of glycoprotein synthesis The regulation of blood protein levels The binding of soluble extracellular and intercellular glycoproteins As a receptor on the surface of mammalian liver cells for the recognition of galactose residues, which results in removal of certain glycoproteins from the circulatory system As a receptor that recognizes hydrolytic enzymes containing mannose-6-phosphate, and targets these proteins for delivery to the lysosomes; I-cell disease is one type of defect in this particular system. Lectins are known to play important roles in the innate immune system. C-type lectins such as the mannose-binding lectin, help mediate the first-line defense against invading microorganisms. Other immune lectins play a role in self-nonself discrimination and they likely modulate inflammatory and autoreactive processes. Intelectins (X-type lectins) bind microbial glycans and may function in the innate immune system as well. Lectins may be involved in pattern recognition and pathogen elimination in the innate immunity of vertebrates including fishes.
Astrochemistry – study of the abundance and reactions of chemical elements and molecules in the universe, and their interaction with radiation. Cosmochemistry – study of the chemical composition of matter in the universe and the processes that led to those compositions. Computational chemistry – is a branch of chemistry that uses computer simulations for solving chemical problems. Environmental chemistry – study of chemical and biochemical phenomena that occur diverse aspects of the environment such the air, soil, and water. It also studies the effects of human activity on the environment. Green chemistry is a philosophy of chemical research and engineering that encourages the design of products and processes that minimize the use and generation of hazardous substances. Supramolecular chemistry – refers to the domain of chemistry beyond that of molecules and focuses on the chemical systems made up of a discrete number of assembled molecular subunits or components. Theoretical chemistry – study of chemistry via fundamental theoretical reasoning (usually within mathematics or physics). In particular the application of quantum mechanics to chemistry is called quantum chemistry. Since the end of the Second World War, the development of computers has allowed a systematic development of computational chemistry, which is the art of developing and applying computer programs for solving chemical problems. Theoretical chemistry has large overlap with (theoretical and experimental) condensed matter physics and molecular physics.
Most cases of SCID are due to mutations in the IL2RG gene encoding the common gamma chain (γc) (CD132), a protein that is shared by the receptors for interleukins IL-2, IL-4, IL-7, IL-9, IL-15 and IL-21. These interleukins and their receptors are involved in the development and differentiation of T and B cells. Because the common gamma chain is shared by many interleukin receptors, mutations that result in a non-functional common gamma chain cause widespread defects in interleukin signalling. The result is a near complete failure of the immune system to develop and function, with low or absent T cells and NK cells and non-functional B cells.The common gamma chain is encoded by the gene IL-2 receptor gamma, or IL-2Rγ, which is located on the X-chromosome. For this reason, immunodeficiency caused by mutations in IL-2Rγ is known as X-linked severe combined immunodeficiency. The condition is inherited in an X-linked recessive pattern.
=== Academic service === Alongside her academic research, Franz is committed to mentoring early career researchers. She was awarded the Duke University Dean's Award for Excellence in Mentoring in 2016. In 2019 Franz was awarded the American Chemical Society Award for Encouraging Women into Careers in the Chemical Sciences. Franz co-edited the American Chemical Society Metals in Medicine Chemical Reviews. Franz was made the chair of the Gordon Research Conference on Metals in Medicine in 2013.
acid resin (6%), soluble in alcohol and having the formula C20H32O4 gum (similar to gum arabic) 30–36% 3-acetyl-beta-boswellic acid (Boswellia sacra) alpha-boswellic acid (Boswellia sacra) incensole acetate, C21H34O3 phellandrene olibanic acid Among various plants in the genus Boswellia, only Boswellia sacra, Boswellia serrata and Boswellia papyrifera have been confirmed to contain significant amounts of boswellic acids.
Sources: en.wikipedia.org
PT-141 is a laboratory code for bremelanotide, a synthetic peptide that activates melanocortin receptors. It has been developed both as an injectable pharmaceutical product and as a research chemical. The two contexts differ sharply in how identity, purity, and dosing are controlled.
It is neither a steroid nor a naturally occurring human hormone. Bremelanotide is a manufactured peptide that mimics part of the melanocortin signalling system by binding receptor proteins. Its effects come from receptor activation, not from replacing a circulating hormone.
The internal lactam bridge locks the peptide into a defined shape, which raises receptor affinity and slows enzymatic breakdown. Linear versions of the same sequence are less stable and bind more weakly. Ring geometry is therefore central to how the molecule behaves in the body.
PT-141 is the research code for bremelanotide, a cyclic peptide developed as a melanocortin receptor agonist. The code has appeared in literature and catalog listings since early development. Bremelanotide is the international nonproprietary name.