en · de · es · fr · pt
liraglutide-notes.peptides1004.com › Data › Chemical Identity Of Bremelanotide — Explained

Chemical Identity Of Bremelanotide — Explained

By Editorial Desk · published 2026-02-06 · last reviewed 2026-02-21 · Data

certificate of analysis comes up often in conversation and rarely with the context attached. Here we lay out the basics in order, then work through the practical considerations.

Updated 2026-02-21. Numbers and descriptions here follow the published literature rather than marketing material.

Chemical Identity of Bremelanotide

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.

Melanocortin Receptor Agonist Pharmacology

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.

Pt-141 at a glance

PropertyValueNotes
Chemical classCyclic peptideMelanocortin receptor agonist family
Molecular weightApproximately 1025 DaFree base form
AppearanceWhite to off-white powderLyophilized product
SolubilitySoluble in waterAlso dissolves in polar organic solvents
Storage temperature-20 degrees CelsiusDry and protected from light

Melanocortin Receptor Pharmacology

Compared with melanotan II, bremelanotide is a smaller cyclic peptide with a more constrained backbone, which affects receptor selectivity and metabolic stability. Published descriptions give a plasma half-life on the order of a few hours after subcutaneous administration, with elimination through hepatic and renal routes and limited plasma protein binding. Central access is inferred from effects observed in animal models, although direct measurement in humans is limited. Handling and storage requirements follow from the peptide backbone, which is susceptible to hydrolysis and oxidation.

The melanocortin system comprises five G protein-coupled receptors, designated MC1 through MC5, that signal mainly through cyclic AMP accumulation. MC1R and MC2R are associated with pigmentation and adrenal steroid production, while MC3R and MC4R are expressed in the central nervous system and influence energy balance and behavior. MC5R appears in exocrine tissues. Natural agonists include alpha-melanocyte-stimulating hormone and adrenocorticotropic hormone, and endogenous antagonists such as agouti-related protein modulate the same sites. This receptor family provides the framework within which bremelanotide activity is described.

Related pages on this site

Bremelanotide Background and Receptor Pharmacology

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.

PT-141 is the research code for bremelanotide, a cyclic heptapeptide derived from alpha-melanocyte-stimulating hormone. The molecule belongs to the melanocortin receptor agonist family and shows highest affinity for the MC4 receptor subtype, with weaker activity at MC1, MC3 and MC5. Its structure retains the core His-Phe-Arg-Trp sequence that defines melanocortin recognition, while cyclization and terminal modifications improve metabolic stability relative to the parent hormone. Early work classified the compound as a centrally acting agent rather than a peripherally acting vasodilator, which shaped subsequent development priorities.

Melanocortin Receptor Signaling Mechanism

PT-141 initiates cellular signaling by binding to specific subtypes within the melanocortin receptor family. These receptors belong to the G protein-coupled receptor superfamily, and activation raises intracellular cyclic adenosine monophosphate levels. This cascade ultimately influences neuronal circuits in the central nervous system that are associated with sexual desire and arousal. Research indicates the compound's action concentrates in hypothalamic regions rather than peripheral tissues, which helps explain some observed pharmacological features. The selectivity of receptor binding underlies its functional differences.

Compared with the related compound melanotan II, PT-141 shows markedly weaker activation of receptors tied to pigmentation. This difference stems from subtle structural variations that alter affinity distribution across receptor subtypes. Investigators propose that such selectivity produces a different side effect profile in specific applications. However, downstream consequences of prolonged receptor activation remain uncertain in the literature. Published studies do not fully agree on the duration of signaling pathway activity and the mechanisms of desensitization.

Peptide Handling and Storage Practice

Lyophilized peptide material is generally stored at -20 °C or below to limit degradation, while reconstituted solutions are less stable and are typically kept refrigerated and protected from light. Repeated freeze-thaw cycles can accelerate aggregation and should be minimized. Stability for any specific lot depends on purity, moisture content, and packaging. Handling in a temperature-controlled environment reduces variability across replicates, and exposure to ambient humidity during weighing can introduce error. Aliquotting reduces the number of times a stock container is opened.

Reverse-phase high-performance liquid chromatography is the standard method for assessing purity. Mass spectrometry confirms molecular identity and detects sequence variants or truncation products. Ultraviolet absorbance at 214 or 280 nm is used for quantification, with the choice depending on the peptide sequence. Method validation typically addresses linearity, limit of detection, and precision across a defined concentration range. Impurity profiling may also employ ion-exchange or size-exclusion chromatography, and these techniques complement one another.

Certificate of analysis documents usually report purity percentage, molecular weight, and appearance. Researchers verify identity by comparing observed and theoretical mass values. Chain-of-custody records and batch numbers help trace material from source to experiment. Independent verification of supplier claims is considered good practice when material identity is critical to a study. Records should include the storage history of each aliquot, and unexpected deviations in appearance or solubility warrant re-testing before use.

Background from the literature

Blood alcohol content (BAC), also known as blood alcohol concentration or blood alcohol level, is the concentration of alcohol in a person's blood, measured for legal or medical purposes. BAC is expressed as the mass of alcohol per unit volume of blood. In the United States and many other countries, it is commonly reported as a percentage, such as 0.08% (equivalent to 0.8 g/L). Legal limits for driving vary by country, ranging from zero tolerance policies to 0.08%. Levels above 0.40% (4 g/L) may be fatal.

Alexander Butlerov showed in 1861 that the formose reaction created sugars including tetroses, pentoses, and hexoses when formaldehyde is heated under basic conditions with divalent metal ions like calcium. R. Breslow proposed that the reaction was autocatalytic in 1959.

=== DNA damage === Aging is the most important risk factor for cardiovascular problems. The causative basis by which aging mediates its impact, independently of other recognized risk factors, remains to be determined. Evidence has been reviewed for the key role of DNA damage in vascular aging. 8-oxoG, a common type of oxidative damage in DNA, is found to accumulate in plaque vascular smooth muscle cells, macrophages and endothelial cells, thus linking DNA damage to plaque formation. DNA strand breaks also increased in atherosclerotic plaques. Werner syndrome (WS) is a premature aging condition in humans. WS is caused by a genetic defect in a RecQ helicase that is employed in several repair processes that remove damage from DNA. WS patients develop a considerable burden of atherosclerotic plaques in their coronary arteries and aorta: calcification of the aortic valve is also frequently observed. These findings link excessive unrepaired DNA damage to premature aging and early atherosclerotic plaque development (see DNA damage theory of aging).

Properties also decrease with the age of the fiber. Younger fibers tend to be stronger and more elastic than older ones. Many natural fibers exhibit strain rate sensitivity due to their viscoelastic nature. Bone contains collagen and exhibits strain rate sensitivity in that the stiffness increases with strain rate, also known as strain hardening. Spider silk has hard and elastic regions that together contribute to its strain rate sensitivity, these cause the silk to exhibit strain hardening as well. Properties of natural fibers are also dependent on the moisture content in the fiber.

Curium pnictides show ferromagnetic transitions upon cooling: 244CmN and 244CmAs at 109 K, 248CmP at 73 K and 248CmSb at 162 K. The lanthanide analog of curium, gadolinium, and its pnictides, also show magnetic transitions upon cooling, but the transition character is somewhat different: Gd and GdN become ferromagnetic, and GdP, GdAs and GdSb show antiferromagnetic ordering. In accordance with magnetic data, electrical resistivity of curium increases with temperature – about twice between 4 and 60 K – and then is nearly constant up to room temperature. There is a significant increase in resistivity over time (~10 μΩ·cm/h) due to self-damage of the crystal lattice by alpha decay. This makes uncertain the true resistivity of curium (~125 μΩ·cm). Curium's resistivity is similar to that of gadolinium, and the actinides plutonium and neptunium, but significantly higher than that of americium, uranium, polonium and thorium. Under ultraviolet illumination, curium(III) ions show strong and stable yellow-orange fluorescence with a maximum in the range of 590–640 nm depending on their environment. The fluorescence originates from the transitions from the first excited state 6D7/2 and the ground state 8S7/2. Analysis of this fluorescence allows monitoring interactions between Cm(III) ions in organic and inorganic complexes.

Sources: en.wikipedia.org

Further detail

== History == Ziprasidone is chemically similar to risperidone, of which it is a structural analogue. It was first synthesized in 1987 at the Pfizer central research campus in Groton, Connecticut. Phase I trials started in 1995. In 1998 ziprasidone was approved in Sweden. After the FDA raised concerns about long QT syndrome, more clinical trials were conducted and submitted to the FDA, which approved the drug on February 5, 2001.

There are several Akabori amino acid reactions, which are named after Shirō Akabori (Japanese: 赤堀 四郎) (1900–1992), a Japanese chemist. In the first reaction, an α-amino acid is oxidised and undergoes decarboxylation to give an aldehyde at the former α position by heating with oxygen in the presence of a reducing sugar. This reaction is useful for preparing dichlorophthalimido derivatives of peptides for mass spectral analysis.

=== Affinity Chromatography === Affinity chromatography exploits the specific interactions between proteins and their ligands. A target protein is captured on a column containing a ligand that specifically binds to it, such as an antibody, enzyme substrate, or metal ion. After washing away non-specifically bound proteins, the target protein is eluted using a solution that disrupts the protein-ligand interaction. This method provides high specificity and is often used for purifying recombinant proteins that have affinity tags.

On inhalation and exhalation air moves through the airways in the same direction, thus creating a unidirectional airflow through the lungs. A similar system is found in birds, monitor lizards and iguanas. Most reptiles lack a secondary palate, meaning that they must hold their breath while swallowing. Crocodilians have evolved a bony secondary palate that allows them to continue breathing while remaining submerged (and protect their brains against damage by struggling prey). Skinks (family Scincidae) also have evolved a bony secondary palate, to varying degrees. Snakes took a different approach and extended their trachea instead. Their tracheal extension sticks out like a fleshy straw, and allows these animals to swallow large prey without suffering from asphyxiation.

Individuals whose willingness to volunteer in a clinical trial may be unduly influenced by the expectation, whether justified or not, of benefits associated with participation, or of a retaliatory response from senior members of a hierarchy in case of refusal to participate. Examples are members of a group with a hierarchical structure, such as medical, pharmacy, dental, and nursing students, subordinate hospital and laboratory personnel, employees of the pharmaceutical industry, members of the armed forces, and persons kept in detention. Other vulnerable subjects include patients with incurable diseases, persons in nursing homes, unemployed or impoverished persons, patients in emergency situations, ethnic minority groups, homeless persons, nomads, refugees, minors, and those incapable of giving consent. (ICH E6)

Sources: en.wikipedia.org

Background from the literature

Soy flour refers to soybeans ground finely enough to pass through a 100-mesh or smaller screen where special care was taken during desolventizing (not toasted) to minimize denaturation of the protein to retain a high protein dispersibility index, for uses such as food extrusion of textured vegetable protein. It is the starting material for soy concentrate and protein isolate production. Soy flour can also be made by roasting the soybean, removing the coat (hull), and grinding it into flour. Soy flour is manufactured with different fat levels. Alternatively, raw soy flour omits the roasting step.

chromatography Any of a variety of laboratory methods designed to separate a heterogeneous mixture into its component chemical species by first dissolving the mixture in a gas or liquid solvent called the mobile phase and then passing it through a system such as a chromatography column or a capillary tube upon which a material called the stationary phase is fixed. The different species present in the mixture have different affinities for and retention times upon the stationary phase, causing them to separate from the rest of the species in the moving fluid at characteristic rates. This phenomenon is exploited both to detect or measure the relative proportions of analytes present in a mixture, and to purify specific compounds.

== Multi-substrate reactions == Multi-substrate reactions follow complex rate equations that describe how the substrates bind and in what sequence. The analysis of these reactions is much simpler if the concentration of substrate A is kept constant and substrate B varied. Under these conditions, the enzyme behaves just like a single-substrate enzyme, and a plot of v by [S] gives apparent KM and Vmax constants for substrate B. If a set of these measurements is performed at different fixed concentrations of A, these data can be used to work out what the mechanism of the reaction is. For an enzyme that takes two substrates A and B and turns them into two products P and Q, there are two types of mechanism: ternary complex and substituted-enzyme mechanisms. Ternary-complex mechanisms

When the university partially reopened, Cremer was still temporarily banned from work due to her German citizenship and would secretly visit the university in a delivery truck to continue research. Cremer was allowed to return to her work in late 1945. Prior completed the research demonstrating a novel method for measurements and qualitative and quantitative analysis in 1947. Another student of Cremer's, Roland Müller wrote his dissertation on the analytical possibilities of the gas chromatograph. Cremer was appointed director of the Physical Chemistry Institute at Innsbruck and was made a professor in 1951. Cremer began presenting Prior and Müller's work in 1947 at various scientific meetings. In 1951, three papers on Cremer's work were published in Zeitschrift für Elektrochemie, a lesser known German scientific journal. The scientific community responded to presentations and papers either negatively or not at all. Many believed that older methods were sufficient. In 1952, the British Anthony Trafford James and Archer Porter Martin and in 1953, the Czech J. Janak published reports claiming the invention of gas chromatography. Martin and his partner Richard Laurence Millington Synge won the Nobel Prize for partition chromatography, which is often credited for introducing the use of gas as a mobile phase, in 1952. All were completely ignorant of Cremer's early work. This has been attributed to the fact that Cremer spoke to the wrong people in the wrong places. Austrian analytical and micro chemists did not focus on gases, so the idea did not gain interest.

Sources: en.wikipedia.org

Frequently asked questions

What class of compound is PT-141?

It belongs to the melanocortin receptor agonist family of peptides. Its cyclic structure distinguishes it from linear peptides and shapes its receptor binding profile.

How was the compound originally identified?

It emerged from research on melanotan II. Investigators exploring derivatives observed distinct pharmacological features related to sexual function.

Which synonyms appear for PT-141?

Common names include bremelanotide and PT-141. Chemical databases may also list early development codes and descriptive names.

What is PT-141?

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.

Network