PT-141 - 10mg

SPECIFICATIONS

Product Code: PT1410

Sequence: Ac-Nle-cyclo(-Asp-His-D-Phe-Arg-Trp-Lys)-OH

Molecular Formula: C50H68N14O10

Molecular Weight: 1024.54 g/mol

CAS: 189691-06-3

Purity: Technical / Research Grade 99%

Other details: No TFA Salt

Form: Lyophilized powder

Color: White

Storage temperature: -20°C

Source: Synthetic

Safety classification: Standard handling

DESCRIPTION

Bremelanotide (PT-141) is a synthetic peptide structurally related to the naturally occurring human hormone alpha-melanocyte–stimulating hormone (α-MSH). This compound was originally investigated for its potential applications in both men and women and has since attracted particular scientific interest in the context of female sexual health, especially in premenopausal women. Unlike many other agents studied for sexual function, PT-141 acts primarily through central nervous system pathways rather than through direct vascular mechanisms.

PT-141 functions as an agonist of melanocortin receptors, a family of receptors involved in the regulation of multiple physiological processes, including appetite, energy balance, immune modulation, mood, and sexual behavior. Early experimental research demonstrated that melanocortin signaling plays a key role in behavioral and neuroendocrine responses. When α-MSH–related peptides were administered in animal models, an increase in sexual motivation and performance was observed, suggesting a central mechanism of action.

Subsequent studies identified PT-141 as having strong agonistic activity at melanocortin-3 (MC3R) and melanocortin-4 (MC4R) receptors. These receptors are widely expressed in regions of the brain involved in autonomic regulation, motivation, and sexual behavior, particularly within the hypothalamus. Activation of MC3R and MC4R has been shown in experimental models to increase neuronal firing and immunoreactivity in hypothalamic nuclei associated with sexual arousal and behavioral response.

Neurobiological investigations indicate that, after binding to melanocortin receptors, PT-141 activates hypothalamic neurons and modulates downstream neural circuits within the central nervous system. This cascade appears to stimulate surrounding neuronal networks involved in arousal and motivational behavior. Importantly, this mechanism does not rely on peripheral blood flow alone, distinguishing PT-141 from phosphodiesterase-5 inhibitors and other vasodilatory approaches.

Erectile dysfunction (ED) is a multifactorial condition that may arise from vascular, neurogenic, hormonal, or psychogenic causes. Epidemiological data indicate that tens of millions of men worldwide are affected by ED, making it a significant public health concern. Conventional therapies are not effective in all patients, particularly in cases where neural signaling rather than vascular insufficiency is the primary contributor.

Female sexual dysfunction has also been recognized as a clinically relevant condition. The American Sexual Health Association defines hypoactive sexual desire disorder (HSDD) as a persistent lack of sexual thoughts, fantasies, or desire for sexual activity that leads to personal distress or interpersonal difficulty. This condition may have both psychological and physiological components and can significantly affect quality of life.

Early human studies investigating PT-141 explored its effects on sexual arousal in healthy volunteers. In a phase I randomized, double-blind, placebo-controlled study conducted in 2003 involving healthy male participants without erectile dysfunction, intranasal administration of PT-141 was associated with a marked increase in the duration of rigid erections compared with placebo. Follow-up studies conducted in 2004, involving several hundred participants, reported that relatively low doses of PT-141 were associated with statistically significant erectile responses.

These findings led to phase II investigations focusing on individuals with erectile dysfunction. In these studies, administration of PT-141 was associated with notable improvements in erectile function scores, including increased rigidity and duration. Importantly, responses were observed even in some individuals who did not respond adequately to standard treatments, suggesting a distinct and complementary mechanism of action.

Research has also demonstrated that PT-141 may increase sexual desire and arousal in both men and women, even in the absence of direct sexual stimulation. This observation supports the hypothesis that melanocortin receptor activation influences central motivational pathways rather than acting solely at the level of peripheral sexual organs.

Beyond sexual arousal, melanocortin signaling has been implicated in energy balance and mood regulation. As a result, PT-141 has also been associated in research settings with subjective increases in alertness and perceived energy levels, although these effects remain secondary to its primary area of investigation.

Reported adverse effects in clinical and experimental studies have generally been mild to moderate. The most commonly reported effect is nausea, particularly at higher doses. Other reported effects include flushing and headache. Early intranasal formulations were associated with transient increases in blood pressure; however, subsequent studies using subcutaneous administration demonstrated a substantially lower incidence of this effect.

Overall, PT-141 represents a well-studied melanocortin receptor agonist with a unique central mechanism of action. Its ability to modulate hypothalamic pathways involved in sexual motivation and arousal has positioned it as a molecule of significant interest in research related to sexual health, neuroendocrinology, and behavioral biology.

All information provided above is derived from scientific literature, experimental models, and clinical research contexts and is intended exclusively for educational and research purposes.

REFERENCES

All information presented above is derived from in vitro experiments, animal studies, and other preclinical research models. These data are intended solely for basic scientific investigation of biological mechanisms and do not imply any therapeutic, diagnostic, preventive, or clinical use in humans or animals.

S.A. Kingsberg et al., "Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder: Two Randomized Phase 3 Trials" [PubMed]

J.G. Pfaus et al., "The neurobiology of bremelanotide for the treatment of hypoactive sexual desire disorder in premenopausal women" [PubMed]

A.H. Clayton et al., "Bremelanotide for female sexual dysfunctions in premenopausal women: a randomized, placebo-controlled dose-finding trial" [PubMed]

D. Mayer et al., "Bremelanotide: New Drug Approved for Treating Hypoactive Sexual Desire Disorder" [PubMed]

S. Cipriani et al., "An evaluation of bremelanotide injection for the treatment of hypoactive sexual desire disorder" [PubMed]

S. Dhillon et al., "Bremelanotide: First Approval" [PubMed]

J. Pfaus et al., "Bremelanotide: an overview of preclinical CNS effects on female sexual function" [PubMed]

B. Mintzes et al., "Bremelanotide and flibanserin for low sexual desire in women: the fallacy of regulatory precedent" [PubMed]

A.N. Edinoff et al., "Bremelanotide for Treatment of Female Hypoactive Sexual Desire" [PubMed]

M.R. Safarinejad et al., "Salvage of sildenafil failures with bremelanotide: a randomized, double-blind, placebo controlled study" [PubMed]

L.E. Diamond et al., "Co-administration of low doses of intranasal PT-141, a melanocortin receptor agonist, and sildenafil to men with erectile dysfunction results in an enhanced erectile response" [PubMed]

A.M. Shadiack et al., "Melanocortins in the treatment of male and female sexual dysfunction" [PubMed]

R. Kumar et al., "Central nervous system agents and erectile dysfunction" [PubMed]

L.E. Diamond et al., "Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction" [PubMed]

S. Kim et al., "Novel Emerging Therapies for Erectile Dysfunction" [PubMed]

P.B. Molinoff et al., "PT-141: a melanocortin agonist for the treatment of sexual dysfunction" [PubMed]

DISCLAIMER

This product is intendend for lab research and development use only. These studies are performed outside of the body. This product is not medicines or drugs and has not been approved by the FDA or EMA to prevent, treat or cure any medical condition, ailment or disease. Bodily introduction of any kind into humans or animals is strictly forbidden by law. This product should only be handled by licensed, qualified professionals.

All product information provided on this website is for informational and educational purposes only.

INDEPENDENT THIRD-PARTY CERTIFICATE OF ANALYSIS SHOWN FORREFERENCE PURPOSES. ANALYTICAL RESULTS MAY VARY SLIGHTLY BETWEEN BATCHES.