PT-141
From PeptidePlaza, the free peptide reference · Entry #010 · Nootropic · Hand-curated entry · Editorial standards
PT-141 (also known as Bremelanotide, Vyleesi, Melanotan II metabolite) is a nootropic research peptide. A cyclic heptapeptide melanocortin receptor agonist and active metabolite of Melanotan II. Unlike peripheral vasodilators, PT-141 acts centrally via the CNS to modulate arousal and food intake pathways.
PT-141 (Bremelanotide) is a cyclic heptapeptide and metabolite of Melanotan II, acting as a non-selective melanocortin receptor agonist (MC1R, MC3R, MC4R, MC5R). Uniquely, it acts via the CNS rather than peripheral vasodilation — specifically through MC4R in the hypothalamus and limbic system to mediate arousal pathways. FDA-approved (2019) as Vyleesi for hypoactive sexual desire disorder (HSDD) in premenopausal women. Also studied for its role in appetite suppression via MC3R/MC4R, and tanning via MC1R.
1 Mechanism of action
Non-selective MC receptor agonism. MC4R activation in hypothalamus mediates arousal and appetite suppression; MC1R mediates melanogenesis; MC3R modulates energy balance and feeding behavior.
Primary targets: MC1R · MC3R · MC4R · MC5R
2 Reported effects
Effects below are those reported in the published literature cited on this page. They are not claims of clinical benefit and not medical advice.
2.1 Reported benefits
- FDA-approved for hypoactive sexual desire disorder in women
- CNS-mediated arousal pathway independent of vascular mechanisms
- Appetite suppression effects via MC4R activation
2.2 Side effects
- Nausea (reported in ~40% of patients in trials)
- Flushing and injection site reactions
- Transient increase in blood pressure
3 Chemical and physical properties
| CAS number | 189691-06-3 |
|---|---|
| Molar mass | 1025.18 g/mol |
| Purity (typical) | >99.2% |
| Half-life | ~2.7 hours |
| Storage | −20 °C, lyophilised powder, desiccated |
| Solubility | Sterile water / bacteriostatic water |
| Receptors / targets | MC1R, MC3R, MC4R, MC5R |
3.1 Amino acid sequence
Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH
4 Research dosages
1.75 mg SC as needed (FDA-approved); research protocols explore 0.75–2.5 mg dose range.
5 Research studies (8)
- Bremelanotide for Hypoactive Sexual Desire Disorder (RECONNECT Study)
Obstetrics & Gynecology (2019) · RCT · N=1,247Phase 3 RCT supporting FDA approval. Bremelanotide SC improved FSDS-DAO score and satisfying sexual events vs placebo in premenopausal HSDD.Key finding: Bremelanotide significantly increased sexual desire scores and satisfying sexual events — led to FDA approval for HSDD. - Central Nervous System Mechanisms of Melanocortin-Mediated Sexual Function
Journal of Sexual Medicine (2007) · Review · N/A (review)Review of MC4R role in CNS-mediated arousal; pharmacological rationale for bremelanotide vs peripheral mechanisms.Key finding: MC4R activation in the hypothalamus directly mediates sexual arousal via distinct CNS pathways independent of vascular mechanisms. - Comprehensive characterization of bremelanotide acetate and its degradants by LC-HRMS/MS and predicting epimerization through computational modelling
Analytical methods : advancing methods and applications (2026) · PreclinicalOverall, this study provides valuable insights into BRM stability behavior and supports peptide API/formulation development, impurity profiling, and quality control. - Should Bremelanotide Be Considered for the Treatment of Sexual Arousal and Desire Disorders in Men?
Journal of clinical psychopharmacology (2026) · ReviewDepartments of Psychiatry and Behavioral Neurosciences, and Anesthesiology, Wayne State University School of Medicine, Detroit, MI. - Bremelanotide
(2006) · ReviewUntil more data become available, bremelanotide should be used with caution during breastfeeding, especially while nursing a newborn or preterm infant. - Female Syrian hamster analyses of bremelanotide, a US FDA approved drug for the treatment of female hypoactive sexual desire disorder
Neuropharmacology (2025) · PreclinicalIf there are other authors, they declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. - Melanocortin Receptor Agonist Bremelanotide Induces Cell Death and Growth Inhibition in Glioblastoma Cells via Suppression of Survivin Expression
Anticancer research (2024) · PreclinicalThe present results identified melanocortin receptors 3 and 4 as novel and viable therapeutic targets for glioblastoma. - Small Effects, Questionable Outcomes: Bremelanotide for Hypoactive Sexual Desire Disorder
Journal of sex research (2024) · PreclinicalAcross RECONNECT trial data from two prior publications and the current study, bremelanotide's benefits are statistically modest and limited to outcomes for which scant evidence of validity among women with HSDD exists.
6 Safety and risk profile
6.1 Regulatory status
PT-141 is currently classified as FDA approved. Approval applies to specific clinical indications and dosing; research-grade material is not the approved product.
Safety score: 75/100 — low concern. Derived from clinical data volume, known risks and regulatory status.
6.2 Contraindications
Conditions and populations in which use is contraindicated:
- Uncontrolled hypertension (SBP >160 mmHg)
- Cardiovascular disease with recent MI or stroke
- Severe hepatic impairment
- Pregnancy
6.3 Drug interactions
| Drug or class | Interaction | Risk |
|---|---|---|
| Antihypertensives | Transient BP increases of 6 mmHg SBP / 3 mmHg DBP — may counteract antihypertensives. | Moderate |
| Oral naltrexone | Naltrexone-containing products reduce bremelanotide Cmax by 30–40%. | Moderate |
6.4 Long-term risks
- Skin hyperpigmentation with chronic use (MC1R agonism)
- Blood pressure effects with frequent repeated dosing
- Nevus/melanocyte changes with prolonged MC1R stimulation
6.5 Research best practices
- Store at room temperature; lyophilized at −20 °C
- Maximum frequency: 8 doses per month (per FDA labeling)
- Administer 45 minutes before anticipated effect
- Monitor blood pressure in hypertensive subjects
7 Frequently asked questions
- How does PT-141 work differently from other compounds?
- Unlike peripheral vasodilators that work via blood flow, PT-141 acts directly on the central nervous system through melanocortin receptors in the hypothalamus — the part of the brain that regulates arousal and desire. It does not require visual or physical stimulation to be effective.
- What is the FDA status of PT-141?
- PT-141 (Bremelanotide) is FDA-approved under the brand name Vyleesi for hypoactive sexual desire disorder (HSDD) in premenopausal women. It is administered as a subcutaneous injection 45 minutes before anticipated activity.
8 References
- Comprehensive characterization of bremelanotide acetate and its degradants by LC-HRMS/MS and predicting epimerization through computational modelling PubMed (2026). Yuvaraaj VK, et al.. View source
- Should Bremelanotide Be Considered for the Treatment of Sexual Arousal and Desire Disorders in Men? PubMed (2026). Pfaus JG, et al.. View source
- Bremelanotide PubMed (2006). View source
- Female Syrian hamster analyses of bremelanotide, a US FDA approved drug for the treatment of female hypoactive sexual desire disorder PubMed (2025). Borland JM, et al.. View source
Related compounds
Entries that share a target, a mechanism, or a research area with PT-141.
Also targets MC1R
A potent cyclic analog of α-MSH that activates melanocortin receptors broadly. Studied for UV-independent melanogenesis, appetite suppression, and as the parent compound of PT-141 (Bremelanotide).
Also targets MC4R
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Shares activation and hypothalamus pharmacology
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Shares mc4r and hypothalamus pharmacology
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Shares agonism and energy pharmacology
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Shares modulates and balance pharmacology
A synthetic analog of the endogenous tetrapeptide Tuftsin. Developed by the Russian Institute of Molecular Genetics. Studied for anxiolytic, nootropic, and immunomodulatory effects without sedation or dependence.
9 See also
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