Bremelanotide: an overview of preclinical CNS effects on female sexual function.
Pfaus. James J; Giuliano. François F; Gelez. Hélène H
Key Findings
- Bremelanotide markedly increases sexual solicitation (desire) in female rats without affecting pacing or lordosis
- The effect occurs with peripheral (subcutaneous) dosing and when injected into the lateral ventricles or medial preoptic area, but not the ventromedial hypothalamus
- Peripheral dosing activates the medial preoptic area and other limbic/hypothalamic regions, likely via dopamine terminal activation
Practical Outcomes
- The study suggests bremelanotide could be a candidate for boosting female sexual desire, but because it’s only tested in rats, there’s no clear dosage or safety guidance for humans. Enthusiasts should wait for human trials before considering off‑label use, and monitor emerging research for dosing protocols and side‑effect data.
Summary
In rats, the peptide bremelanotide (pt‑141) boosts the female’s urge to mate—shown by more solicitation moves—when given under the skin or directly into a brain area called the medial preoptic area. It doesn’t change other sexual actions, and it seems to work by turning on dopamine signals in that brain region. While this points to a possible way to treat low sexual desire, the data are only from animal studies, so real‑world use in people is still uncertain.
Abstract
Bremelanotide is an analogue of the naturally occurring peptide alpha-melanocyte-stimulating hormone (alpha-MSH). It stimulates erection in men and male rats, and is currently in clinical trials for the treatment of erectile dysfunction. To review the effects of bremelanotide, an analogue of the naturally occurring peptide alpha-MSH, on the preclinical indices of sexual desire in female rats, and where in the brain these actions may occur. Appetitive sexual behaviors, such as solicitations, hops and darts, and pacing, were assessed along with consummatory behaviors such as lordosis. The involvement of brain regions was assessed following direct administration to the region, by the stimulation of molecular markers of neural activation, and using microdialysis to examine extracellular fluid for different neurotransmitters. Using a model that allows ovariectomized, hormone-primed female rats to control the timing of sexual encounters with males, we tested the ability of bremelanotide to increase appetitive (proceptive) and/or consummatory sexual behaviors. Bremelanotide dramatically and selectively increased measures of solicitation in female rats, without altering pacing or lordosis, following both peripheral (subcutaneous) administration or infusions directly into the lateral ventricles or medial preoptic area (mPOA), but not the ventromedial hypothalamus. The mPOA is critical for the display of appetitive sexual behaviors in females and males of a variety of species. Peripheral administration of bremelanotide activates the mPOA and other hypothalamic and limbic regions of the brain involved in sexual behavior, and may work by activating dopamine terminals in the mPOA. To the extent that solicitations indicate the desire of female rats to engage in sexual activity, bremelanotide appears to possess the behavioral, pharmacological, and neuroanatomical specificity required of a drug in the treatment of hypoactive sexual desire disorders.
Study Information
pubmed
2007
10.1111/j.1743-6109.2007.00610.x