PT-141 (Bremelanotide) 10mg

1. What is PT-141?

PT-141, also known as Bremelanotide, is a synthetic peptide derived from the melanocortin peptide family. It is primarily used for the treatment of sexual dysfunction, including erectile dysfunction (ED) in men and sexual arousal disorder in women. PT-141 works by activating melanocortin receptors (MC1, MC3, MC4, MC5) in the brain, which helps enhance libido and sexual desire. Unlike traditional erectile dysfunction drugs, PT-141 acts through the central nervous system, rather than directly affecting blood flow.

2. PT-141 Structure

【pictures linking，https://pubchem.ncbi.nlm.nih.gov/compound/9941379】

Sequence:Ac-Nle-Asp(1)-His-D-Phe-Arg-Trp-Lys(1)

Molecular Formula: C50H68N14O10

Molecular Weight: 1025.16 g/mol

PubChem ClD: 9941379

CAS Number:189691-06-3

3. PT-141 Research

PT141, later named Bremelanotide, is a cyclic heptapeptide analogue of α-MSH, acting primarily as a central melanocortin receptor (MC3R/MC4R) agonist. Unlike PDE5 inhibitors (e.g., Viagra), PT141 operates centrally to enhance libido and arousal by targeting neural circuits linked to sexual motivation and reward.

Preclinical & early human data:

In rats and nonhuman primates, PT141 induced penile erections and activated hypothalamic neurons relevant to sexual behavior 【https://pubmed.ncbi.nlm.nih.gov/12851303/】.

A Phase I/II trial (intranasal) in healthy males confirmed safety and an approximate 30-minute onset, with notable intensity and duration of rigidity .

Even men unresponsive to sildenafil achieved significant erection improvement (IIEF scores improved markedly) 【https://wjmh.org/DOIx.php?id=10.5534%2Fwjmh.200007&utm_source=chatgpt.com】.

Mechanistic differentiation:

Works via MC4R pathway in the CNS, promoting erection, desire, and sexual motivation, not vascular mechanisms 【https://pubmed.ncbi.nlm.nih.gov/12851303/】.

Women’s HSDD trials:

Registered as Vyleesi, 1.75 mg subcutaneous dosing ~45 minutes before sexual activity, leading to improved FSFI-Desire and orgasm scores 【https://pmc.ncbi.nlm.nih.gov/articles/PMC8788464/?utm_source=chatgpt.com】.

In a 52-week open-label study, sustained sexual desire benefits and tolerability were confirmed; common side effects included nausea (~40%) and flushing (~20%)【https://pmc.ncbi.nlm.nih.gov/articles/PMC6819023/?utm_source=chatgpt.com】.

✅ Why Consider PT141?

🌐 Acts at the level of the brain, enhancing sexual desire and arousal rather than solely blood flow.

🚀 Rapid onset (~30–45 min) and on-demand dosing, granting greater spontaneity compared to daily pills.

🗣 Effective in PDE5 non-responders for erectile dysfunction, offering new options .

👩‍⚕️ FDA-approved for premenopausal women with HSDD (brand name Vyleesi) since 2019 【https://en.wikipedia.org/wiki/Bremelanotide?utm_source=chatgpt.com】.

👥 Synergistic potential: reported enhanced effects when combined with sildenafil; additive value in desire and performance .

🛡 Fewer vascular contraindications: unlike PDE5 inhibitors, PT141 doesn’t interact adversely with nitrates .

4. Future PT-141 Research

Selective MC4R Analogues (PL6983):

Designed to reduce blood pressure side effects seen with PT141, while maintaining sexual efficacy 【https://en.wikipedia.org/wiki/PL-6983?utm_source=chatgpt.com】.

Alternative Delivery Formats:

Research continues into optimized nasal sprays, subcutaneous options, and potential oral peptide delivery systems.

Expanded Populations:

Testing in diabetic men, other male dysfunction cohorts, and co-use with PDE5 inhibitors; early evidence shows synergistic benefit .

Women’s Sexual Dysfunction:

Exploring extended use, combination with therapies like kisspeptin, oxytocin, and broader sexual health outcomes .

Neurobiological Mechanisms:

Advanced imaging (fMRI), biomarker mapping, neuroendocrine assessments to define PT141’s action on desire and reward pathways.

Safety and Real-world Usage:

Longterm open-label data over 1 year (RECONNECT), with monitoring for blood pressure, pigmentation changes, and treatment adherence 【https://en.wikipedia.org/wiki/Bremelanotide?utm_source=chatgpt.com】【https://pmc.ncbi.nlm.nih.gov/articles/PMC6819023/?utm_source=chatgpt.com】.

5.Application Areas

Erectile Dysfunction: As a central-onset treatment for men, especially when PDE5 inhibitors are ineffective or contraindicated.

Hypoactive Sexual Desire Disorder (HSDD) in women: Ondemand treatment with demonstrated clinical benefits.

Performance anxiety: Central delivery may ease psychological barriers to arousal 【https://en.wikipedia.org/wiki/Bremelanotide?utm_source=chatgpt.com】.

Combination therapies: Co-administration with PDE5 inhibitors or other neuromodulators for multilayered sexual support.

Off-label potential: Includes use in male libido concerns, premature ejaculation, and psychosexual therapy adjunct.

✅ Summary

PT141 (Bremelanotide) offers a novel, central approach to sexual dysfunction by targeting MC4 receptors in the CNS, enhancing desire, arousal, and performance. With rapid on-demand onset (~30–45 minutes) and approval for female HSDD, it fills critical gaps left by PDE5 treatments. Ongoing innovations—like MC4R-selective analogs and new delivery systems—promise enhanced safety and broader applicability across genders, metabolic profiles, and psycho-sexual health contexts.

ALL ARTICLES AND PRODUCT INFORMATION PROVIDED ON THIS WEBSITE ARE FOR INFORMATONAL AND EDUCATIONAL PURPOSES ONLY.

The products offered on this website are furnished for in-vitro studies only. In-vitro studies(Latin: in glass) are performed outside of the body. These products are not medicines or drugs and have not been approved by the FDA 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.