PT-141 10mg

Compound Name: PT-141

Synonyms: Bremelanotide

CAS Number: 189691-06-3

Molecular Formula: C₅₀H₆₈N₁₄O₁₀

Molecular Weight: ~1025.2 g/mol

Structure: Cyclic heptapeptide analog

Peptide Sequence: Ac-Nle-c[Asp-His-D-Phe-Arg-Trp-Lys]-OH

Chemical Structure:

Source: PubChem

Mechanism of Action: PT-141 exerts its effects by acting as a potent agonist at melanocortin receptors MC3 and MC4, primarily in the central nervous system. Activation of these GPCRs results in increased cAMP signaling, modulating neural pathways involved in sexual arousal and desire. Unlike PDE5 inhibitors, PT-141 does not rely on peripheral vascular changes, but instead enhances sexual motivation centrally. Its selectivity for central melanocortin receptors underlies its prosexual effects without altering hormone levels^1-4.

Biological Activity: PT-141 centrally facilitates sexual arousal and desire in both sexes. In preclinical models, it increases solicitous and proceptive behaviors; in clinical studies, it enhances sexual function and satisfaction in individuals with hypoactive sexual desire disorder and certain types of erectile dysfunction. It does not significantly influence skin pigmentation or systemic endocrine function at therapeutic doses^1-4.

Storage: Store lyophilized peptide at -20°C; reconstituted solutions should be aliquoted and stored at -20°C. Avoid repeated freeze-thaw cycles.

Drug Categories: Melanocortin receptor agonist, sexual function research tool, peptide research reagent.

Additional Notes:

• Does not act as a vasodilator or influence nitric oxide.
• Limited peripheral melanogenic effects compared to related peptides.
• Approved as bremelanotide for clinical use in selected jurisdictions for hypoactive sexual desire disorder (HSDD) in premenopausal women

Summary Table:

Disclaimer: For Research Use Only. Not intended for human or veterinary use. This compound is supplied solely for laboratory and R&D purposes.

Detailed Product Description

PT-141 (bremelanotide) is a synthetic cyclic peptide and potent agonist of central melanocortin receptors MC3R and MC4R. It is structurally derived from Melanotan-II, but features a modified C-terminal hydroxyl group, enhancing its selectivity for CNS targets and significantly reducing activity at MC1R^1-3. Unlike traditional erectile dysfunction agents, PT-141 works through the central melanocortin pathway rather than vascular smooth muscle, making it unique for investigating sexual response and psychogenic arousal^2,4. The compound induces erections and proceptive sexual behaviors in animal models and has demonstrated efficacy in clinical studies for hypoactive sexual desire disorder and sexual arousal disorders, particularly when administered intranasally or subcutaneously. PT-141 does not cause skin pigmentation or tanning. It is an invaluable research tool for probing neurobehavioral effects of melanocortin signaling and for the development of novel therapies in sexual medicine and behavioral pharmacology.

Research Highlights

• Stimulates sexual arousal and erectile responses via MC3R/MC4R activation¹.
• Effective in both male and female animal models for proceptive sexual behaviors^2,4.
• Demonstrates CNS selectivity with minimal peripheral and tanning activity^1-4.
• Clinical studies show activity in patients with sexual arousal and desire disorders³.

• Structurally related to Melanotan-II but optimized for central, not peripheral, effects^1,2.

Mechanism of Action

MC3 (Melanocortin 3) Receptor Agonism

• Regulates sexual behavior (CNS): Promotes neural activity in hypothalamic and limbic circuits that modulate sexual motivation and arousal^1-3.
• Enhances proceptive behaviors and mating responses, especially in females².
• Contributes to central integration of sexual cues and behavioral output⁴.

MC4 (Melanocortin 4) Receptor Agonism

• Potently induces penile erection and sexual desire by engaging spinal and supraspinal networks^1-3.
• Increases cAMP signaling in CNS pathways, leading to rapid and reversible erectile response^1-4.

• Bypasses peripheral vasodilator pathways, making its effect independent of endothelial function³.

Pharmacokinetic Profile:

• Route of Administration: Subcutaneous injection or intranasal spray
• Dosing Frequency: On demand
• Half-Life: 2.5 – 4 hours

Formulation & Handling

• Lyophilized powder, reconstituted in sterile saline.
• Store lyophilized powder at –20 °C.

Selected Clinical Trial Activity

References

¹Diamond, L. E., Earle, D. C., Rosen, R. C., Willett, M. S. & Molinoff, P. B. 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. Int. J. Impot. Res. 16, 51–59 (2004).

²Pfaus, J. G. et al. Selective facilitation of sexual solicitation in the female rat by a melanocortin receptor agonist. Proc. Natl Acad. Sci. USA 101, 10201–10204 (2004).

³Diamond, L. E. et al. An effect on the subjective sexual response in premenopausal women with sexual arousal disorder by bremelanotide (PT-141), a melanocortin receptor agonist. J. Sex. Med. 3, 628–638 (2006).

⁴Giuliano, F., Rossler, A. S., Clement, P., Droupy, S. & Alexandre, L. The use of telemetry technology to test the proerectile effect of Melanotan-II (MT-II) in conscious rats. Eur. Urol. 48, 145–152 (2005).