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PT-141

Bremelanotide, Vyleesi

Quick Stats
Studies 74
Trials 10
Score 3
2017 pubmed 27 citations

Understanding the Role of Serotonin in Female Hypoactive Sexual Desire Disorder and Treatment Options.

Croft. Harry A HA

Key Findings

  • Serotonin overactivity is linked to reduced sexual desire (HSDD) in women.
  • Drugs that lower serotonin or increase dopamine (e.g., flibanserin, bupropion, bremelanotide) are being studied for HSDD.
  • Flibanserin is the only medication currently approved for female HSDD, acting as a serotonin 5‑HT1A agonist and 5‑HT2A antagonist.

Practical Outcomes

  • For biohackers, the take‑away is that targeting serotonin can help boost desire, but the evidence for PT‑141 specifically is limited in this review. If you’re considering PT‑141, treat it as one of several options that may work by reducing serotonin inhibition, and monitor how it interacts with dopamine‑enhancing strategies.

Summary

The review explains that too much serotonin in the brain can dampen sexual desire in women, while dopamine and other chemicals boost it. Most drugs that help with low desire work by lowering serotonin or raising dopamine, and the only approved pill right now is flibanserin. The peptide bremelanotide (PT‑141) is mentioned as one of several agents that target these pathways, but the paper doesn’t give new data on it.

Abstract

The neurobiology of sexual response is driven in part by dopamine and serotonin-the former modulating excitatory pathways and the latter regulating inhibitory pathways. Neurobiological underpinnings of hypoactive sexual desire disorder (HSDD) are seemingly related to overactive serotonin activity that results in underactive dopamine activity. As such, pharmacologic agents that decrease serotonin, increase dopamine, or some combination thereof, have therapeutic potential for HSDD. To review the role of serotonin in female sexual function and the effects of pharmacologic interventions that target the serotonin system in the treatment of HSDD. Searches of the Medline database for articles on serotonin and female sexual function. Relevant articles from the peer-reviewed literature were included. Female sexual response is regulated not only by the sex hormones but also by several neurotransmitters. It is postulated that dopamine, norepinephrine, oxytocin, and melanocortins serve as key neuromodulators for the excitatory pathways, whereas serotonin, opioids, and endocannabinoids serve as key neuromodulators for the inhibitory pathways. Serotonin appears to be a key inhibitory modulator of sexual desire, because it decreases the ability of excitatory systems to be activated by sexual cues. Centrally acting drugs that modulate the excitatory and inhibitory pathways involved in sexual desire (eg, bremelanotide, bupropion, buspirone, flibanserin) have been investigated as treatment options for HSDD. However, only flibanserin, a multifunctional serotonin agonist and antagonist (5-hydroxytryptamine [5-HT]<sub>1A</sub> receptor agonist and 5-HT<sub>2A</sub> receptor antagonist), is currently approved for the treatment of HSDD. The central serotonin system is 1 biochemical target for medications intended to treat HSDD. This narrative review integrates findings from preclinical studies and clinical trials to elucidate neurobiological underpinnings of HSDD but is limited to 1 neurotransmitter system (serotonin). Serotonin overactivity is a putative cause of sexual dysfunction in patients with HSDD. The unique pharmacologic profile of flibanserin tones down inhibitory serotonergic function and restores dopaminergic and noradrenergic function. Croft HA. Understanding the Role of Serotonin in Female Hypoactive Sexual Desire Disorder and Treatment Options. J Sex Med 2017;14:1575-1584.

Study Information

Provider

pubmed

Year

2017

Date

2017-12-01T00:00:00.000Z

DOI

10.1016/j.jsxm.2017.10.068

Citations

27

References

76