PT-141

PT-141 (Bremelanotide)

Primary Function: Libido enhancement, sexual arousal, CNS-based sexual response
Research Use: Sexual dysfunction, arousal disorders, melanocortin receptor studies
Molecular Formula: C50H68N14O10
CAS Number: 189691-06-3
Synonyms: Bremelanotide, MC-4R agonist, Melanotan derivative

Description:
PT-141 is a synthetic peptide analog of α-MSH (alpha-melanocyte-stimulating hormone) that acts as a potent agonist at melanocortin receptors, particularly MC-4R and MC-3R, which are involved in sexual desire and arousal. Unlike traditional treatments that act on vascular pathways (e.g., PDE5 inhibitors), PT-141 works centrally in the hypothalamus, targeting libido and arousal directly via the CNS. It is studied in both male and female sexual dysfunction models, including HSDD (Hypoactive Sexual Desire Disorder).

Mechanism of Action:

• Binds to MC-3R and MC-4R receptors in the brain
• Activates the hypothalamic arousal centers, enhancing sexual desire
• Does not affect blood pressure or vasodilation like PDE5 inhibitors
• Rapid onset of CNS-based arousal response

Key Research Areas:

• Female sexual arousal disorder and HSDD
• Erectile dysfunction in males (non-vascular origin)
• Libido modulation and CNS stimulation
• Melanocortin receptor pharmacology

History of Discovery:
PT-141 was developed by Palatin Technologies, originally derived from Melanotan II, a peptide known for its tanning and arousal side effects. Researchers isolated the pro-sexual effects of Melanotan II and refined the molecule to remove unwanted side effects like intense pigmentation. It was later approved by the FDA in 2019 under the name Vyleesi for the treatment of HSDD in premenopausal women.

Case Studies:

1. FDA Approval for HSDD (2019, J Sex Med): PT-141 demonstrated significant improvement in sexual desire and distress scores over placebo in a randomized, double-blind trial. [J Sex Med. 2019;16(9):1436–1444.]
2. Male Erectile Response (2004, Urology): PT-141 restored erectile function in men unresponsive to Viagra, indicating a CNS-mediated arousal benefit. [Urology. 2004;63(4):755–759.]
3. Safety and Tolerability (Phase III Trials): Most common side effects were transient nausea and flushing; no cardiovascular events reported. [Drug Des Devel Ther. 2016;10:2311–2319.]

Packaging Information:

• Form: Lyophilized powder
• Purity: ≥ 99%
• For research use only. Not for human or veterinary use.