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

Chemical Identity Of Bremelanotide — Worked Examples

By Editorial Desk · published 2026-02-15 · last reviewed 2026-03-05 · Data

melanocortin receptor raises a handful of sensible questions. This page answers them in order, starting with the fundamentals and moving to applications.

Reviewed 2026-03-05. Anything still debated is marked as such rather than presented as settled.

Chemical Identity of Bremelanotide

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.

Bremelanotide Background and Receptor Pharmacology

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.

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

Identity and Chemical Background

Bremelanotide is a moderately large peptide with a molecular mass near 1025 daltons. In lyophilised form it appears as a white to off-white powder and is freely soluble in water and other polar solvents. The intact lactam ring is essential for receptor affinity, while linearised fragments bind far more weakly. Solutions are sensitive to extremes of pH and to prolonged exposure to light and heat, so handling typically involves buffered conditions and cold storage. Its short plasma half-life reflects rapid distribution and clearance rather than chemical breakdown inside the vial.

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.

Related pages on this site

Background and Receptor Pharmacology

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.

Analytical Methods and Storage Practice

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.

Receptor Pharmacology and Study Measures

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.

Reference notes

=== Mixed with polyketides === Due to the similarity with polyketide synthases (PKS), many secondary metabolites are, in fact, fusions of NRPs and polyketides. In essence, this occurs when PK modules follow NRP modules, and vice versa. This is possible because the carrier domains (PCP/ACP) are quite similar between each other and they use a similar "chain-flipping" action to access the growing substrate. Although there is high degree of similarity between the Carrier (PCP/ACP) domains of both types of synthetases, the mechanism of condensation is different from a chemical standpoint:

Histology image: 08008loa – Histology Learning System at Boston University Atlas image: eye_1 at the University of Michigan Health System—"Sagittal Section Through the Eyeball" MedlinePlus Encyclopedia: 002295

== Other uses == Operation Snowcap (1987-1994) a U.S. counter-narcotics trafficking program Snowcaps (song), a 1999 song by Unwed Sailor Snow Cap (story) by Matthew S. Armstrong from the graphic novel anthology Flight, see List of volumes of Flight

== Further reading == Bazell R (1998). Her-2: the making of Herceptin, a revolutionary treatment for breast cancer (1st ed.). New York: Random House. ISBN 0-679-45702-X. Boseley S (29 March 2006). "The selling of a wonder drug". The Guardian. Archived from the original on 13 December 2019. Retrieved 13 December 2019. Dent S, Verma S, Latreille J, Rayson D, Clemons M, Mackey J, et al. (August 2009). "The role of HER2-targeted therapies in women with HER2-overexpressing metastatic breast cancer". Current Oncology. 16 (4): 25–35. doi:10.3747/co.v16i4.469. PMC 2722050. PMID 19672422. Dean L (2015). "Trastuzumab (Herceptin) Therapy and ERBB2 (HER2) Genotype". In Pratt VM, McLeod HL, Rubinstein WS, et al. (eds.). Medical Genetics Summaries. National Center for Biotechnology Information (NCBI). PMID 28520362. Bookshelf ID: NBK310376. Archived from the original on 26 October 2020. Retrieved 5 February 2020.

There has been a tremendous advance in speed and cost reduction since the completion of the Human Genome Project, with some labs able to sequence over 100,000 billion bases each year, and a full genome can be sequenced for $1,000 or less. Computers became essential in molecular biology when protein sequences became available after Frederick Sanger determined the sequence of insulin in the early 1950s. Comparing multiple sequences manually turned out to be impractical. Margaret Oakley Dayhoff, a pioneer in the field, compiled one of the first protein sequence databases, initially published as books as well as methods of sequence alignment and molecular evolution. Another early contributor to bioinformatics was Elvin A. Kabat, who pioneered biological sequence analysis in 1970 with his comprehensive volumes of antibody sequences released online with Tai Te Wu between 1980 and 1991. In the 1970s, new techniques for sequencing DNA were applied to bacteriophage MS2 and øX174, and the extended nucleotide sequences were then parsed with informational and statistical algorithms. These studies showed that well-known features, such as coding segments and the triplet code, could be revealed in straightforward statistical analyses and were proof of the concept that bioinformatics would be insightful.

Sources: en.wikipedia.org

Reference notes

There are also the testimonies of Raymond Queneau (1903–1976), born in Le Havre, the city served as a framework for his novel Un rude hiver (A harsh winter) (1939). The plot of Une maison soufflée aux vents (A house blown to the winds) by Émile Danoën, winner of the Popular Novel Prize in 1951, and its sequel Idylle dans un quartier muré (Idyll in a walled neighbourhood) were located in Le Havre during the Second World War. Under the name Port de Brume Le Havre is the setting for three other novels by this author: Cerfs-volants (Kites), L'Aventure de Noël (The Adventure at Christmas), and La Queue à la pègre (Queue to the underworld). Michel Leiris wrote De la littérature considérée comme une tauromachie (Of literature considered like a bullfight) in December 1945. Diana Gabaldon set the second novel in her Outlander series, Dragonfly in Amber (1992), partly in Le Havre. Two mystery novels take place in Le Havre: Le Bilan Maletras (The Maletras Balance) by Georges Simenon and Le Crime de Rouletabille (Crime at the Roulette table) by Gaston Leroux. In Rouge Brésil (Red Brazil), winner of the Goncourt Prize in 2001, Jean-Christophe Rufin describes Le Havre in the 16th century as the port of departure of French expeditions to the New World: the hero Villegagnon leaves of the port to conquer new lands for the French crown which become Brazil. Martine–Marie Muller tells the saga of a clan of Stevedores from Le Havre in the 1950s to the 1970s in Quai des Amériques (Quay of the Americas).

== Specific examples == Using the bacterial one-hybrid system, one study has characterized 35 members of the Drosophila melanogaster segmentation network which includes representative members of all the major classes of DNA-binding domain proteins. Implications for medical research are evident from another study that used the B1H system to identify the DNA-binding specificity of a transcriptional regulator for a gene in Mycobacterium tuberculosis. The B1H system has also been used to identify an important turnover element in Escherichia coli.

Contamination has also been seen in water wells and other sources of drinking water. This contamination is seen in US, United Kingdom, Germany, Japan, and Canada, but information from most developing countries is nearly nonexistent. The lack of information on PFAS contamination in developing countries, especially those in Africa, are due to structural socioeconomic inequality and lack of access to the expensive laboratory capabilities required for PFAS quantification.

Russia launched an offensive in Kharkiv Oblast, pushing Ukrainian forces back one kilometer from the international border. Heavy shelling was reported in Vovchansk. Five villages (Strilecha, Krasne, Pylna, Borysivka and Ohirtseve) were reported to have been taken by Russia, while fighting was ongoing in the villages of Pletenivka and Hatyshche. At least two civilians were killed in Russian attacks. During a press conference with Slovak President Zuzana Čaputová, Zelenskyy acknowledged the Russian offensive, but said that "Ukraine met them there with our troops, brigades, and artillery." One person was killed by Russian shelling in Sumy Oblast. Two people were killed in separate Russian attacks in Donetsk Oblast. Russian-installed officials in Luhansk Oblast claimed that three people were killed and seven others injured in a drone strike on the Rovenky oil depot. Ukrainian media reported that the HUR carried out a drone strike on an oil refinery in Russia's Kaluga Oblast. Russian officials also claimed that drone strikes caused damage in Belgorod and Kursk Oblasts. The Czech Republic delivered an F-16 fighter jet simulator to Ukraine.

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 does the PT-141 code refer to?

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.

Network