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Chemical Identity Of Bremelanotide — Reference Sheet

By Editorial Desk · published 2026-04-20 · last reviewed 2026-05-29 · News

A practical reference on cyclic heptapeptide: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.

Reviewed 2026-05-29. 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.

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.

Receptor Pharmacology And Signalling

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.

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

Analytical Characterisation and Storage Practice

Published studies differ in design, population and endpoint definition, so results are not always directly comparable across reports. Some trials used patient-reported measures of desire and distress, while others tracked physiological or behavioural outcomes. Questions that remain open include the durability of effects beyond short follow-up periods, the frequency of transient blood pressure elevation observed after administration, and whether a subtype-selective analogue could separate central effects from pigmentation-related activity. These points are usually framed as unresolved rather than settled in review literature.

Routine characterisation of bremelanotide relies on reversed-phase high-performance liquid chromatography with ultraviolet detection near 214 nm, where the peptide backbone absorbs. Mass spectrometry, typically in tandem mode with electrospray ionisation, confirms identity and supports quantification in biological matrices. Additional checks include amino acid analysis, peptide mapping after enzymatic digestion, and confirmation of the lactam bridge, since incomplete cyclisation produces a mass-shifted by-product. Purity values above 95 percent are common in reference-grade material, though reports vary in how strictly related substances are resolved from the parent peak.

Related pages on this site

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.

Peptide Handling and Storage Practice

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.

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.

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.

Further detail

Mizell won his first start of 1953, coming within an out of throwing a complete game on April 22 against Cincinnati in an 8–3 victory. On April 28, he held the Phillies to one run for five innings in a tie, as rain forced the game to be called and it was never resumed. His most notable game of the season came on May 4, when he gave up just two hits in a shutout of the Pirates. Mizell had a 2.83 ERA before the All-Star Break, but he had a 4.14 ERA in the second half of the season. On August 7, he held the New York Giants to one run in a complete game, 2–1 triumph. Exactly one week later, he held Cincinnati to one run over nine innings, but the Cardinals only scored one for him. After throwing a scoreless 10th, Mizell took the loss in the 11th when Roy McMillan had an RBI single against him. His 11 strikeouts in that contest were a season-high, and he also had five games in which he had nine, including each of his last two starts. In 33 starts, he had a 13–11 record. For the second year in a row, he led the NL in strikeouts per 9 innings pitched (6.9), and he finished third in the league with 173 strikeouts this time, behind Roberts's 198 and Carl Erskine's 187. His 3.49 ERA was the ninth-best mark in the league, but his 114 walks trailed only Johnny Lindell's 139 for the league lead.

==== Mental health ==== Layard and others show that the most important influence on happiness is mental health. L.M. Keyes and Shane Lopez illustrate the four typologies of mental health functioning: flourishing, struggling, floundering and languishing. However, complete mental health is a combination of high emotional well-being, high psychological well-being, and high social well-being, along with low mental illness. Although health is part of well-being, some people are able to maintain satisfactory wellbeing despite the presence of psychological symptoms.

Plants communicate with each other through both airborne and below-ground chemical cues. For example, when damaged by an herbivore, many plants emit an altered bouquet of volatile organic compounds (VOCs). Various C6 fatty acids and alcohols (sometimes known as green leaf volatiles) are often emitted from damaged leaves, since they are break-down products of plant cell membranes. These compounds (familiar to many as the smell of freshly mown grass) can be perceived by neighboring plants where they may trigger the induction of plant defenses. It is debated to what extent this communication reflects a history of active selection due to mutual benefit as opposed to "eavesdropping" on cues unintentionally emitted by neighboring plants.

== Pathophysiology == The thyroid gland is responsible for regulating whole-body metabolism through the production of two major hormones: thyroxine (T4) and triiodothyronine (T3). Of the metabolically active thyroid hormones, 93% is T4 and 7% is T3. T3 is four times more potent than T4 and most T4 is converted to T3 in the tissues. Iodine is necessary for adequate hormone production. Thyroid-stimulating hormone (TSH) is a circulating or serum hormone from the pituitary gland that stimulates the thyroid gland to produce T3 and T4. Hypothyroidism occurs when the thyroid gland does not produce enough T3 and T4. The most common cause of hypothyroidism worldwide is too little dietary iodine. Hashimoto's thyroiditis is the most common cause of hypothyroidism in countries with sufficient dietary iodine. With the cessation of the production of thyroid hormone, the thyroid gland contains enough reserve T3 and T4 to last 2 to 3 months. The thyroid hormones T3 and T4 influence the production by virtually all cells in the body of hundreds of new intracellular proteins and enzymes. This influence includes the expression of the calcium ATPase, regulation of ion channels, oxidative phosphorylation, increased Na-K-ATPase activity, increased carbohydrate metabolism, increased free fatty acids, increased vitamin requirements, and increased overall metabolism.

The Centre Party, whose pragmatic principles generally left it open to supporting either a monarchical or republican form of government, proved one of the mainstays of the Weimar Republic, continuing the cooperation with SPD and DDP in the Weimar Coalition. This combination, however, lost its majority in the 1920 elections. The formation of the new Christian People's Party in Rhineland (May 1920) caused considerable concern among the Centre leadership. Seeing the exodus of conservative Catholics caused by a sharp left turn of the Centre at the end of war, Adam Stegerwald proposed his "Essen program" (September 1920) that promised Germany to become "Christian, democratic, German, and social" and a plan to form a broad-based Christian party. The party was an ideologically diverse coalition of Catholic politicians, comprising republicans like Matthias Erzberger and Joseph Wirth as well as right-wingers like Franz von Papen. As a result of the party's flexibility, it participated in every government between 1919 and 1932, both with parties to their left and to their right. The Centre mainly provided the ministers for finance and labour and, on four occasions, the Chancellor. However, this also damaged the party's prospects because it was increasingly associated with all of the conflicts, problems, and failures of the Republic.

Sources: en.wikipedia.org

Background from the literature

== Properties == Flavin adenine dinucleotide consists of two portions: the adenine nucleotide (adenosine monophosphate) and the flavin mononucleotide (FMN) bridged together through their phosphate groups. Adenine is bound to a cyclic ribose at the 1' carbon, while phosphate is bound to the ribose at the 5' carbon to form the adenine nucleotide. Riboflavin is formed by a carbon-nitrogen (C-N) bond between the isoalloxazine and the ribitol. The phosphate group is then bound to the terminal ribose carbon, forming a FMN. Because the bond between the isoalloxazine and the ribitol is not considered to be a glycosidic bond, the flavin mononucleotide is not truly a nucleotide. This makes the dinucleotide name misleading; however, the flavin mononucleotide group is still very close to a nucleotide in its structure and chemical properties.

In humans, the only post-synaptic receptor at which amphetamine is known to bind is the 5-HT1A receptor, where it acts as an agonist with low micromolar affinity. The full profile of amphetamine's short-term drug effects in humans is mostly derived through increased cellular communication or neurotransmission of dopamine, serotonin, norepinephrine, epinephrine, histamine, CART peptides, endogenous opioids, adrenocorticotropic hormone, corticosteroids, and glutamate, which it affects through interactions with CART, 5-HT1A, EAAT3, TAAR1, VMAT1, VMAT2, and possibly other biological targets. Amphetamine also activates seven human carbonic anhydrase enzymes, several of which are expressed in the human brain. Dextroamphetamine displays higher binding affinity for DAT than levoamphetamine, whereas both enantiomers share comparable affinity at NET; Consequently, dextroamphetamine produces greater CNS stimulation than levoamphetamine, roughly three to four times more, but levoamphetamine has slightly stronger cardiovascular and peripheral effects. Dextroamphetamine is also a more potent agonist of TAAR1 than levoamphetamine.

== Development and social impact == John Rolfe of Virginia used this species of tobacco to break the Spanish monopoly on tobacco in 1612. He did so by obtaining Nicotiana tabacum - the coveted plant he had designs to replace Nicotiana rustica with. Up until 1612, Nicotiana rustica was Virginia's only tobacco crop, and was found by Englishmen to be too bitter for enjoyment. Rolfe, by successfully planting, maintaining, and curing Nicotiana tabacum until sale (by removing all superfluous leaves and applying as little water as possible during curing), made Virginia a potential competitor with Spain's colonies. This transitioned the colony to a cash-crop focused one, monocropping tobacco by 1613, the year the first shipment (of 4 barrels) arrived in London. By 1617, the quality of Virginia tobacco had made it the gold standard in European markets, which have become insatiable- 20,000lbs of tobacco was exported there that year. These exports grew exponentially, doubling to 40,000lbs the following year (the year the first enslaved Africans arrive in America), and reaching 60,000lbs by 1620. The money obtained from tobacco exports was used, in turn, to fund the purchasing of more European indentured servants and especially enslaved Africans to fulfill the rising labor demand. In the 17th century, 75% of all colonists in Virginia had come as servants, indentured (with a term of 4 to 7 years of service) or Africans in perpetuity (for life), the latter being preferred as they were cheaper sources of labor:

=== Other uses === Risperidone has demonstrated clinical benefit as an augmentation agent in the management of (unipolar) non-psychotic treatment-resistant depression alongside antidepressant treatment. Atypical antipsychotics, such as risperidone, are among the most common augments for antidepressant therapy. Such usage occurs off-label in most jurisdictions and the risk of adverse effects (e.g., weight gain, movement disorders) must be carefully weighed against the clinical benefit. Risperidone has shown promise in treating therapy-resistant obsessive–compulsive disorder, when serotonin reuptake inhibitors alone are not sufficient. Risperidone has proven to be effective in treatment of aggression associated with attention deficit hyperactivity disorder (ADHD), or with another mental condition. Risperidone has not demonstrated a benefit in the treatment of eating disorders or personality disorders, except for limited evidence in schizotypal personality disorder.

14 March Members of the NASUWT narrowly vote to accept a pay offer, ending the prospect of further strike action in schools in Scotland. BBC Scotland hosts the final televised debate of the SNP leadership election. 16 March – Scientists identify a gene variant that is known to increases the risk of breast and ovarian cancer, and trace it to people with Orkney Island heritage, more specifically those with ancestry on the island of Westray. 18 March – Peter Murrell resigns as chief executive of the Scottish National Party amid a row over party membership. Mike Russell succeeds him as interim chief executive. 21 March – At 8pm, Times Radio airs a leadership debate from Edinburgh and featuring the three candidates in the Scottish National Party leadership election. 22 March First Minister Nicola Sturgeon issues a "sincere, heartfelt and unreserved" apology to people affected by the practice of forced adoption in Scotland during the 1950s, 1960s and 1970s. A major incident is declared, with 35 injuries reported, after the 76m-long RV Petrel research vessel tips over at a dock in Leith. 23 March Nicola Sturgeon attends her final First Minister's Questions as First Minister of Scotland. The TikTok app is banned on all Scottish Government phones and electronic devices. 24 March – Research led by the University of Edinburgh suggests one in 50 people in Scotland have had lasting ill-effects after contracting COVID-19. 25 March – HIV Scotland announces it will close due to issues with governance and financials.

Sources: en.wikipedia.org

Reference notes

=== Acoustic methods === Directed assembly using the acoustic methods manipulate waves in order to allow non-invasive assembling of micro and nano structures. Due to this, acoustics are especially widely used in the biomedical industry to manipulate droplets, cells and other molecules. Acoustic waves are generated by a piezoelectric transducer controlled from the pulse generator. These waves are able to then manipulate droplets of liquid and move them together, in order to form a packed assembly. Moreover, the frequency and amplitude of the waves can be modified in order to achieve a more accurate control of the particular behavior of the droplet or cell.

81.9% of voters decided for Baden to remain part of Baden-Württemberg, only 18.1% opted for the reconstitution of the old state of Baden. The referendums in Lower Saxony and Rhineland-Palatinate were held on 19 January 1975 (the percentages given are the percentages of those eligible who voted in favour):

== Screening == Because it can be difficult to measure weight-for-height Z scores (WHZ) frequently, screening is performed by physical exam, with careful examination of the child's feet to detect the presence of bilateral pitting edema. Screening for edema is essential for the diagnosis of kwashiorkor, since nearly two-thirds of kwashiorkor cases do not have evidence of acute wasting (i.e. mid-upper arm circumference (MUAC) < 125 mm, or WHZ < -2) when diagnosed with kwashiorkor.

Sodium oxybate has also been investigated and been of interest to improve sleep and associated symptoms in other conditions with sleep disruption, such as myalgic encephalomyelitis/chronic fatigue syndrome (ME/CFS) and long COVID, which also have high rates of non-restorative sleep. In addition, sodium oxybate was limitedly studied to improve insomnia in people with depression or bipolar disorder. However, it was reported to paradoxically disrupt sleep and induce narcolepsy-like changes in these individuals. Moreover, concerns about misuse have limited use of sodium oxybate for other medical conditions. GHB has also garnered a reputation as a date-rape drug, although the actual prevalence of this appears to be much lower than popular perception. The GABAB receptor agonist baclofen has also been more limitedly investigated for improvement of sleep and has been found to be effective in enhancing sleep similarly to sodium oxybate. However, in people with narcolepsy, baclofen and sodium oxybate both improved sleep but only sodium oxybate reduced daytime sleepiness. In any case, research in this area is limited, and there remains significant interest in baclofen in the potential treatment of sleeping problems. Unlike sodium oxybate, baclofen is not a controlled substance and has much less or no misuse potential. Baclofen and sodium oxybate have been found to activate the GABAB receptor differently, which is thought to underlie the differences in their effects.

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.

Is PT-141 selective for the MC4 receptor?

It is frequently described as an MC4 receptor agonist, but binding assays show activity at more than one melanocortin subtype. Selectivity is therefore relative rather than absolute. This matters when interpreting side effects tied to other receptor subtypes.

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