PT-141 is a synthetic α-MSH derivative that activates central melanocortin receptors (MC4R/MC1R) to enhance libido and arousal via neural signaling. FDA-approved for HSDD in women; acts on CNS rather than vascular pathways.
PT-141
Also known as: Bremelanotide; Vyleesi™; Rekynda
Overview
Benefits
- Improves libido
- Enhances sexual function
- Neuroprotection
- May increase pigmentation
Consider This Peptide If You Want To
- Enhance libido and arousal
- Support CNS-based sexual function
Dosage & Administration
Dosage Guidelines
Recommended Dosage
• Amount:1 mg
• Frequency:weekly
• Duration:4 weeks
• Rest Period:
• Time of Day:morning
• Ingestion:subcutaneous
Administration Routes:Subcutaneous
Research Findings on Dosage:
• Subcutaneous Injection:
◦ Commonly Reported Dosage: 1--2 mg (0.1-0.2 mL)
◦ Timing: Administer 45 minutes to 1 hour before anticipated sexual activity.
▪ Recommended Use: No more than one dose per 24 hour period and no more than twice weekly to reduce side effects and receptor desensitization
• Notes:
◦ Duration of effects can last 24-72 hours
◦ Recommended to inject 1 mg (0.1 mL) as a test dose. If well tolerated, inject an additional 1 mg (0.1 mL) more than 30 minutes later
◦ Avoid using a PDE5 inhibitor while using PT-141
Mechanism of Action
Mechanism of Action
How this peptide works in the body
Melanocortin Receptor Activation:
PT-141 binds to melanocortin receptors MC4R and MC3R in the hypothalamus, activating Gs protein-coupled receptors that stimulate adenylyl cyclase, increasing cyclic AMP (cAMP) levels. This cascade enhances dopaminergic activity in the medial preoptic area (mPOA) and paraventricular nucleus (PVN), key regions regulating sexual arousal and desire. Unlike PDE5 inhibitors, PT-141 bypasses peripheral vascular pathways, directly modulating central arousal mechanisms.
Central Nervous System Stimulation:
PT-141 activates pro-opiomelanocortin (POMC) neurons in the arcuate nucleus of the hypothalamus, leading to increased release of α-melanocyte-stimulating hormone (α-MSH). This stimulates neuronal circuits responsible for libido and sexual motivation, amplifying behavioral and physiological responses to sexual stimuli, even in the absence of external sensory input.
Neurotransmitter Regulation:
PT-141 enhances dopamine (DA) release by stimulating MC4R in presynaptic neurons, promoting activation of dopaminergic projections to the nucleus accumbens, reinforcing sexual motivation and reward perception. Simultaneously, it increases norepinephrine (NE) levels in the locus coeruleus, heightening sympathetic nervous system activity, which contributes to physical arousal, elevated heart rate, and enhanced genital blood flow.
Consider Stacking With
- Any GHRP
- Any GHRH
- Oxytocin
- Kisspeptin-10
- VIP
Side Effects & Cautions
Common Side Effects
- Nausea (40%)
- Flushing (20%)
- Headache (11%)
- Injection site reactions (13%)
Cautions
- Avoid with uncontrolled hypertension or CVD
- Do not combine with PDE5 inhibitors
Rare Side Effects
- Hypertension
- Hyperpigmentation (with long use)
- Rare priapism
Research & References
Research Highlights
Clinical Trials for HSDD:
Phase III studies demonstrated increased SSEs and reduced distress in women with HSDD after 24 weeks of treatment. Common side effects included nausea and flushing.
Studies on Erectile Dysfunction:
PT-141 restored erectile function in men unresponsive to sildenafil, with a rapid onset of action (30--60 minutes).
Neurological Implications:
Research indicates modulation of dopaminergic pathways enhances reward-based neuropharmacology.
References
Diamond, L. E., et al. (2004). "Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141." J Sex Med
King, S. H., et al. (2019). "Melanocortin receptor agonists for the treatment of sexual dysfunction." Neuroendocrinology
Palatin Technologies. (2019). Vyleesi™ FDA approval monograph
Safarinejad, M. R., & Hosseini, S. Y. (2008). "Salvage of sildenafil failures with bremelanotide: A randomized, double-blind study." J Urol