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Chemical Identity Of Bremelanotide — Evidence Review

By Editorial Desk · published 2025-06-29 · last reviewed 2025-07-13 · Wiki

This is a working overview of melanocortin receptor, written for readers who want more than a one-paragraph summary but less than a textbook.

Reviewed 2025-07-13. Anything still debated is marked as such rather than presented as settled.

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.

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

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.

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Background and Receptor Pharmacology

Early research on PT-141 grew out of work on melanotan II, a related cyclic peptide studied for pigmentation. Investigators observed that centrally acting melanocortin agonists also influenced sexual behaviour in animal models, and the programme shifted toward that endpoint. A nasal formulation was evaluated in clinical trials but showed inconsistent absorption, and later studies used subcutaneous administration instead. Regulatory approval in the United States followed in 2019 for a defined population of premenopausal women with acquired, generalised hypoactive sexual desire disorder. That approval was specific to that group rather than a broad indication.

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

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.

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.

Notes from published material

Only one Ambrosiella (A. cleistominuta from the xyleborine ambrosia beetle Anisandrus maiche) has ever been reported to produce sexual structures, and the rest (including A. roeperi) have been assumed to undergo exclusively clonal reproduction. All Ambrosiella produce translucent, flask-shaped conidiogenous cells (phialides) borne on non-fertile sporodochia (minute, dense cushions of nonreproductive hyphae holding up the fertile tissue). Conidia may arise from these phialides as chains – i.e., new spores are successively pushed out, with the newest growth closest to the original conidiogenous cell – or singly, as an aleurioconidium that ruptures the membrane of the mother cell and then remains a unique, differentiated terminal unit without any subsequent neighbors produced from the phialide. A. roeperi operates only through the latter mechanism, which is distinct from what is reported in A. beaveri, A. trypodendri, and A. hartigii (suggested to use the former, chain-like method).

Based on the size and histological staining characteristics of the fibrils, it is likely that at least in part they are composed of type III collagen (reticulin). An in vitro study with native collagen demonstrated that fibronectin binds to type III collagen rather than other types.

Health Canada followed with similar label updates in 2021, and Australia's Therapeutic Goods Administration aligned all SSRI and SNRI product information in 2024, noting that venlafaxine already carried a warning about persistent sexual dysfunction.

== External links == Clinical trial number NCT00001262 for "Copper Histidine Therapy for Menkes Diseases" at ClinicalTrials.gov Clinical trial number NCT00811785 for "Molecular Bases of Response to Copper Treatment in Menkes Disease, Related Phenotypes, and Unexplained Copper Deficiency" at ClinicalTrials.gov

Agustín Edwards Mac Clure, a person with marked anti-Peruvian sentiments, who from the beginning of his administration came to intensify Chile's "strong hand" policy in Tacna and Arica, renewing the Peruvian protests. The anti-Peruvian riots and attacks, as well as their anti-Chilean counterparts, constantly harassed the diplomatic missions of the countries, which is why several cities in Chile began to rearticulate the patriotic leagues, nationalist organizations responsible for much of the xenophobic violence that was unleashed against Peruvians and Bolivians residing in the country in the country that had annexed the provinces where they lived. According to Arnold McKay, former US consul in Antofagasta, Chile activated three strategies to achieve that objective. He founded Ligas Patrioticas, clandestine organizations inspired by the Ku Klux Klan, which expelled prosperous and influential Peruvians and Bolivians. He maintained strict censorship of Peruvian newspapers. Since 1918, he prescribed the appearance of resident or passing foreigners to register their fingerprints and show their nationality cards to the police. This measure arose to exclude extremists from the country, but in fact it served to find out how many Peruvians and Bolivians were in the area. From 1918 to 1922, the Chilean State and population were exposed to a real and fictitious "danger from the North". The nationalist feeling of the leagues was mainly marked by a fundamental anti-Peruvianism.

Sources: en.wikipedia.org

Further detail

=== Specific risks/complications === Infection: About 0.9-2.5% of patients who undergo Mohs surgery will develop an infection. This is the most frequently documented adverse event with higher rates in patients who are immunosuppressed. To reduce this risk, antiseptics and antibiotics may be used, but the absolute benefit is modest. Impaired wound healing: Dehiscence (partial reopening of the wound) and necrosis (death of healthy tissue) rates are approximately 1-2%. Risk factors include larger excisions, flap/graft use, and immunosuppressed patients. Complication rates decrease when the wound heals with primary closure (using stitches after surgery) or secondary intention (the wound is left open to heal naturally). Hematoma formation and bleeding: This is most commonly seen in patients on antiplatelet or anticoagulant therapy and occurs in 0.9-1.5% of cases. Despite this, patients are not routinely asked to stop these medications, as most experience no complications, and withdrawal is generally not justified. Scarring: 5-7% of cases, especially larger tumors and complex repairs, result in hypertrophic scarring. Less commonly seen are postoperative swelling, rash, and disturbance of skin sensation. Pain is generally mild. Overall, Mohs surgery is generally safe, with risks/complications being minor and manageable.

==== Fabric properties ==== Should not cause damage through friction with the original fabric Be of similar or lighter weight than the original fabric. Match the original fabric with consideration of the loss of color or sheen Be of a tight enough weave to exclude dust if being used as a barrier

Data from the Moneyfacts Group suggests the average rate on a two-year fixed-term mortgage has fallen below 6% for the first time since June 2023. The Court of Session in Edinburgh rules that the UK government acted lawfully by blocking the Gender Recognition Reform (Scotland) Bill from becoming law, and rejects the Scottish Government's appeal against the decision. At the Old Bailey, Paul Bryan is sentenced to life imprisonment with a minimum of 24 years for the 1984 murder of Roman Szalajko at the victim's south London home. Bryan assumed the identity of a dead man with the same name, but was traced through a fingerprint match in 2022. After footballer Joey Barton suggests that women "should not be talking with any kind of authority" about men's football, Chelsea manager Emma Hayes says women are "routinely used to dealing with systemic misogyny and bullying" in football. Wham!'s Last Christmas tops the singles chart for the fourth time with Mariah Carey's All I Want For Christmas Is You taking the second spot. A week after the death of Shane MacGowan from The Pogues, Fairytale of New York rises to number four. 9 December Yellow weather warnings are in place for much of the UK as two successive storms, Elin and Fergus, reach the UK from the Atlantic, bringing high winds and heavy rain. The royal family reveal their Christmas card images with King Charles III choosing a photograph from his coronation earlier this year for his second Christmas as monarch.

1900 BCE: Aganice, also known as Athyrta, was an Egyptian princess during the Middle Kingdom (about 2000–1700 BCE) working on astronomy and natural philosophy. c. 1505–1458 BCE: Hatshepsut, also known as the Queen Doctor, promoted a botanical expedition searching for officinal plants. 1200 BCE: The Mesopotamian perfume-maker Tapputi-Belatekallim was referenced in the text of a cuneiform tablet. She is often considered the world's first recorded chemist. 500 BCE: Theano was a Pythagorean philosopher. c. 150 BCE: Aglaonice became the first female astronomer to be recorded in Ancient Greece. 1st century BCE: A woman known only as Fang became the earliest recorded Chinese female alchemist. She is credited with "the discovery of how to turn mercury into silver" – possibly the chemical process of boiling off mercury in order to extract pure silver residue from ores. 1st century CE: Mary the Jewess was among the world's first alchemists. 3rd century CE: Cleopatra the Alchemist, an early figure in chemistry and practical alchemy, is credited as inventing the alembic. c. 300–350 CE: Greek mathematician Pandrosion develops a numerical approximation for cube roots. c. 350–415 CE: Greek astronomer, mathematician and philosopher Hypatia became renowned as a respected academic teacher, commentator on mathematics, and head of her own science academy.

==== India ==== In India, glass noodles are called falooda (see falooda, the dessert dish), and are served on top of kulfi (a traditional ice cream). They are usually made from arrowroot starch using a traditional technique. The noodles have minimal flavor so they provide a nice contrast with the sweet kulfi. Kulfi and falooda can be bought from numerous food stalls throughout northern and southern parts of India.

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.

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