This is a working overview of MC4R, written for readers who want more than a one-paragraph summary but less than a textbook.
This page was last updated on 2025-11-18 and is reviewed periodically as new material appears.
Bremelanotide is a synthetic cyclic heptapeptide developed as an analogue of alpha-melanocyte-stimulating hormone, a naturally occurring peptide involved in pigmentation and appetite signalling. Its structure contains seven amino acid residues joined by a lactam bridge that closes the ring between two side chains. The molecular formula is C50H68N14O10 and the nominal molecular mass is near 1025 daltons. Much of the early laboratory literature refers to the same molecule by the development code PT-141.
The compound emerged from a research programme examining melanocortin analogues for effects on skin pigmentation. During early human studies, participants reported spontaneous erections as an unexpected side effect, which redirected development toward sexual function rather than tanning. An intranasal formulation was investigated in clinical trials but did not reach market approval. A subcutaneous injectable version later completed the regulatory process, and the nasal route does not appear in approved labelling.
Approved use is narrow and jurisdiction-specific. In the United States, the injectable product is authorised for premenopausal women with acquired, generalised hypoactive sexual desire disorder, a diagnosis that requires documented distress. It is not approved for men, for postmenopausal women, or for use alongside hormonal contraceptives under the approved labelling. Outside regulated markets, the same peptide is frequently sold as a research chemical, where identity, purity, and sterility are not independently verified.
Receptor activation in hypothalamic and limbic circuits is the mechanism most often cited for the observed effects on sexual desire. Signalling through MC4R couples to Gs proteins and raises intracellular cyclic AMP, which in turn modulates dopaminergic tone in reward-related pathways. Because the peptide reaches the central nervous system after subcutaneous administration, peripheral vascular changes are regarded as secondary rather than primary. The precise neural circuits that translate receptor occupancy into behavioural change remain incompletely mapped, and published accounts describe the pathway in general terms rather than as a fully resolved sequence.
Development began with intranasal formulations investigated for erectile dysfunction, but blood pressure elevation limited that route and prompted a switch to subcutaneous delivery. Clinical testing then shifted toward hypoactive sexual desire disorder in premenopausal women, and a subcutaneous product received United States approval in 2019. Later trials examined other populations with mixed results, and questions about effect size, durability and patient selection remain open in the peer-reviewed literature. Research interest continues in parallel with the broader melanocortin field, where several synthetic analogues are studied together.
| Property | Value | Notes |
|---|---|---|
| Molecular formula | C50H68N14O10 | Cyclic heptapeptide backbone |
| Molecular mass | Approximately 1025 Da | Nominal mass of the free peptide |
| Appearance | White to off-white lyophilised powder | Typical for purified synthetic peptides |
| Solubility class | Freely soluble in water | Organic solubility is limited |
| Typical storage temperature | −20 °C or below | Protect from moisture and light |
Published discussion sits at the intersection of peptide chemistry, neuroendocrinology and sexual medicine. Trial reports emphasise change scores on validated instruments, while mechanistic papers focus on hypothalamic circuits and receptor selectivity. Because placebo response in this field is large, effect sizes are usually reported with confidence intervals rather than as isolated averages. Reviews note that female and male data sets are not interchangeable and should be read separately. Diagnostic terminology has been revised over time, which complicates comparison between older and newer studies.
Bremelanotide is a synthetic cyclic heptapeptide that acts on a family of G-protein-coupled receptors. It was designed as a structural analogue of alpha-melanocyte-stimulating hormone, the endogenous peptide associated with pigmentation and several central signalling pathways. A lactam bridge constrains the ring and slows enzymatic breakdown, which distinguishes it from the linear parent molecule. Research interest moved over time from pigment biology toward central nervous system effects, particularly circuits connected to sexual desire. Parenteral delivery is used because oral bioavailability is poor.
Early clinical work used an intranasal formulation, and later programmes switched to subcutaneous delivery for more consistent absorption. A subcutaneous product received regulatory approval in the United States in 2019 for premenopausal women with acquired, generalised hypoactive sexual desire disorder. Approval followed phase 3 trials in which active treatment separated from placebo on desire and distress measures, though the average difference was modest. Labeling carries a caution about transient blood pressure elevation, so cardiovascular history is assessed before prescribing. Questions about durability of benefit beyond several months remain open.
Identity and purity are established with orthogonal methods rather than a single test. Reverse-phase high-performance liquid chromatography with ultraviolet detection gives a purity figure by area normalization, while mass spectrometry confirms the expected molecular ion. Amino acid analysis or peptide mapping can detect sequence errors that a mass value alone would miss, and residual counterion content is sometimes measured separately. Common impurities include truncated sequences, oxidized residues, and deamidated products; reporting them individually is more informative than a single composite purity number.
Lyophilized peptide arrives as a white to off-white cake or powder and is normally held at minus twenty degrees Celsius or colder for extended periods. Short-term bench work at ambient temperature is tolerable for minutes, not hours, because the solid is hygroscopic and picks up moisture that promotes hydrolysis. Vials should stay in a desiccator or a sealed bag with desiccant, protected from light, since aromatic residues in the sequence are susceptible to photo-oxidation. Inventory records that note arrival date and storage location reduce the chance of using degraded material.
The molecular backbone consists of seven amino acid residues joined into a ring through a disulfide bridge. This cyclic conformation is critical for receptor binding. The sequence includes an acetylated N-terminus and an amidated C-terminus, modifications that improve resistance to enzymatic breakdown. One residue is in the D-configuration, a feature that further stabilizes the peptide against protease activity. Together, the ring structure and specific stereochemistry determine selectivity among melanocortin receptor subtypes.
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.
Apart from negative affectivity and disinhibition, research has found "substantial but mixed" associations with the other trait domains, indicating the heterogeneity of the diagnosis, which aligns with the view of BPD as an "index of global personality pathology and severity, which aligns with the original metaphorical use of the term 'borderline' or 'borderland'". It is suggested that it "therefore seems reasonable if the borderline pattern serves as a transitional specifier that eventually is phased out in the coming era".
After the defeat of Prussia by Napoleon and the subsequent reorganisation of the Prussian state, the academy was merged on 3 August 1811 with the Protestant Viadrina University, previously located in Frankfurt (Oder), and re-established in Breslau as the Königliche Universität zu Breslau – Universitas litterarum Vratislaviensis (in 1911 named the Schlesische Friedrich-Wilhelms-Universität zu Breslau, to honour the founder Frederick William III of Prussia). At first, the conjoint academy had five faculties: philosophy, medicine, law, Protestant theology, and Catholic theology. Connected with the university were three theological seminars, a philological seminar, a seminar for German Philology, another seminar for Romanic and English philology, an historical seminar, a mathematical-physical one, a legal state seminar, and a scientific seminar. From 1842, the university also had a chair of Slavic Studies. The university had twelve different scientific institutes, six clinical centers, and three collections. An agricultural institute with ten teachers and forty-four students, comprising a chemical veterinary institute, a veterinary institute, and a technological institute, was added to the university in 1881. In 1884, the university had 1,481 students in attendance, with a faculty numbering 131.
=== Sequestrate species === The description of Russula was changed in 2007 when molecular analysis revealed that several sequestrate species formerly classified in Macowanites (syn. Elasmomyces) were shown to lie within Russula. The type species of Macowanites, Macowanites agaricinus, was transferred and several new species were added: Russula albidoflava, R. albobrunnea, R. brunneonigra, R. galbana, R. pumicoidea, R. reddellii, R. sinuata, and R. variispora. The genus names Gymnomyces and Martellia, formerly used for sequestrate species, are now accepted synonyms of Russula, The genus Cystangium is also probably a synonym of Russula but is still in use.
{\displaystyle \sigma _{11}=\left(\lambda ^{2}-{\cfrac {1}{\lambda ^{2}}}\right)\left({\cfrac {\mu J_{m}}{J_{m}-I_{1}+3}}\right)~;~~\sigma _{22}=0~;~~\sigma _{33}=\left(1-{\cfrac {1}{\lambda ^{2}}}\right)\left({\cfrac {\mu J_{m}}{J_{m}-I_{1}+3}}\right)~.}
Sources: en.wikipedia.org
Some software packages such as Markerview include multivariate statistical analysis (for example, principal component analysis) and these will be helpful for the identification of correlations in lipid metabolites that are associated with a physiological phenotype, in particular for the development of lipid-based biomarkers. Another objective of the information technology side of lipidomics involves the construction of metabolic maps from data on lipid structures and lipid-related protein and genes. Some of these lipid pathways are extremely complex, for example the mammalian glycosphingolipid pathway. The establishment of searchable and interactive databases of lipids and lipid-related genes/proteins is also an extremely important resource as a reference for the lipidomics community. Integration of these databases with MS and other experimental data, as well as with metabolic networks offers an opportunity to devise therapeutic strategies to prevent or reverse these pathological states involving dysfunction of lipid-related processes.
== Commemorative address on the 50th anniversary of the reopening of the Vienna Burgtheater (2005) == At the gala evening marking the 50th anniversary of the reopening of the Vienna Burgtheater following its destruction in World War II, Kermani criticized Europe as a community of values, calling into question the EU's very refugee and asylum policies. After all, Kermani reminded his audience, poets have been dreaming of a Europe without borders and without nationalism for centuries.
=== Key market drivers === Consumer empowerment: Growing interest in preventive healthcare and personal health optimization has driven demand for accessible testing options. Technological advances: Innovations in sample collection (including at-home blood collection with minimal blood volume requirements) and point-of-care testing have made DTC testing more convenient and accessible. Chronic disease prevalence: Rising rates of diabetes (affecting 37.3 million Americans according to the CDC), cardiovascular disease, and other chronic conditions have increased demand for regular monitoring. Cost transparency: DTC services often provide upfront pricing, contrasting with the often opaque costs of traditional healthcare-ordered testing.
== Research == Along with the clinical trials in obesity that generated the data submitted to regulatory authorities, rimonabant was also studied in clinical trials for diabetes, atherosclerosis, and smoking cessation.
Metofoline (INN), also known as methofoline (USAN), is an opioid analgesic drug discovered in the 1950s by a team of Swiss researchers at Hoffmann-La Roche. Methopholine is an isoquinoline derivative which is not structurally related to most other opioids. However, its structural similarity to the non-opioid alkaloid papaverine is notable. Metofoline has around the same efficacy as an analgesic as codeine, and was evaluated for the treatment of postoperative pain. Metofoline tablets were marketed in the United States under the brand name of Versidyne, but the drug was withdrawn from the market in 1965 due to the occurrence of ophthalmic side-effects alongside the discovery that the drug could produce cataracts in dogs. Metofoline has two enantiomers, with the levo (R) enantiomer being the active form, around 3x the potency of codeine, and the (S) enantiomer being inactive. Analogs where the 4'-chloro group has been replaced by other electron withdrawing groups have also been tested, the fluoro derivative being slightly more potent than chloro, and the nitro derivative being most potent of all, with the racemic 4'-nitromethopholine being around 20x the potency of codeine. Later research was carried out by Bristol-Myer in the 1960s and animal studies suggested derivatives with significantly increased analgesic activity of over x50 codeine.
Sources: en.wikipedia.org
A multiaxial joint (polyaxial joint or triaxial joint) is a synovial joint that allows for several directions of movement. In the human body, the shoulder and hip joints are multiaxial joints. They allow the upper or lower limb to move in an anterior-posterior direction and a medial-lateral direction. In addition, the limb can also be rotated around its long axis. This third movement results in rotation of the limb so that its anterior surface is moved either toward or away from the midline of the body.
Alex Wayman has argued that the ideas found in the dependent origination doctrine may precede the birth of the Buddha, noting that the first four causal links starting with avidya in the Twelve Nidānas are found in the cosmic development theory of the Brihadaranyaka Upanishad and other older Vedic texts. According to Kalupahana, the concept of causality and causal efficacy where a cause "produces an effect because a property or svadha (energy) is inherent in something" along with alternative ideas of causality, appear extensively in the Vedic literature of the 2nd millennium BCE, such as the 10th mandala of the Rigveda and the Brahmanas layer of the Vedas.
Come What(ever) May is the second studio album by American rock band Stone Sour, released on August 1, 2006, by Roadrunner Records. It was recorded and produced by Nick Raskulinecz and the band at Studio 606 in Los Angeles, California. Writing for the album began as early as 2003 when vocalist Corey Taylor and guitarist James Root were writing material for their other band, Slipknot. In January 2006, Stone Sour began recording their second album, during which time drummer Joel Ekman left the band because of family constraints. He was eventually replaced by ex-Soulfly drummer Roy Mayorga who played on all but two tracks on the album. Following the release of the album, Stone Sour promoted it for over a year, releasing five singles and touring in the United States, Canada, Japan and several countries in Europe. The album received generally positive reviews. It was praised for showing a progression in the band's songwriting ability and musical style. It was also certified Platinum in the United States and the single "30/30-150" was nominated for Best Metal Performance at the 49th Grammy Awards. On June 26, 2007, Stone Sour released a special edition version of the album; it included six previously unreleased tracks and a bonus DVD with three music videos and a complete live performance by the band in Moscow. It remains their best-selling album to date, mostly due to the success of the single "Through Glass". The album became their first to be certified Platinum by the RIAA which occurred on July 21, 2017.
P-glycoprotein (3.A.1.201.1) is a well-studied protein associated with multi-drug resistance. It belongs to the human ABCB (MDR/TAP) family and is also known as ABCB1 or MDR1 Pgp. MDR1 consists of a functional monomer with two transmembrane domains (TMD) and two nucleotide-binding domains (NBD). This protein can transport mainly cationic or electrically neutral substrates as well as a broad spectrum of amphiphilic substrates. The structure of the full-size ABCB1 monomer was obtained in the presence and absence of nucleotide using electron cryo crystallography. Without the nucleotide, the TMDs are approximately parallel and form a barrel surrounding a central pore, with the opening facing towards the extracellular side of the membrane and closed at the intracellular face. In the presence of the nonhydrolyzable ATP analog, AMP-PNP, the TMDs have a substantial reorganization with three clearly segregated domains. A central pore, which is enclosed between the TMDs, is slightly open towards the intracellular face with a gap between two domains allowing access of substrate from the lipid phase. Substantial repacking and possible rotation of the TM helices upon nucleotide binding suggests a helix rotation model for the transport mechanism.
The United States Environmental Protection Agency (EPA) maintains and approves test methods, which are approved procedures for measuring the presence and concentration of physical, chemical and biological contaminants; evaluating properties, such as toxic properties, of chemical substances; or measuring the effects of substances under various conditions. The methods in the Agency index are known as EPA Methods. There are other types of methods such as the ASTM and United States Pharmacopeia, but the EPA Methods are developed through a regulatory process involving public notice, comment and revision and are legally binding whereas ASTM methods are developed through a consensus process and compliance is voluntary. These methods are developed to help standardize and achieve the EPA mission to protect the environment and human health.
Sources: en.wikipedia.org
It is a synthetic cyclic peptide that acts as an agonist at melanocortin receptors. It is not a hormone replacement therapy and not a vasodilator in the usual clinical sense, although it does affect vascular tone. Chemically it belongs to the melanocortin analogue family.
PT-141 was the internal development code used during early research and it persists in older publications, conference abstracts, and informal listings. The code and the approved name refer to the same molecule. Its continued use reflects habit in the literature rather than any difference in substance.
No. The intranasal form was studied in trials but was never approved, and absorption through the nasal route varies considerably between individuals. Approved labelling covers a subcutaneous injection only. Any nasal product sold outside regulated channels falls outside verified manufacturing.
The code designates bremelanotide, a cyclic heptapeptide melanocortin receptor agonist. It served as an internal research identifier before the compound entered formal clinical development. The code and the generic name refer to the same molecule.