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ClinicalCentral nervous system sexual desire activator

PT-141

Also indexed as Bremelanotide, Vyleesi

PT-141 (Bremelanotide) is a synthetic melanocortin receptor agonist originally derived from the tanning peptide Melanotan II. It is used to treat hypoactive sexual desire disorder (HSDD) and erectile dysfunction by acting centrally on the brain rather than peripherally on blood vessels. Unlike PDE5 inhibitors, PT-141 works through the central nervous system to increase sexual desire and arousal in both men and women.

Overview

Following subcutaneous administration, PT-141 achieves peak plasma concentrations (Tmax) at approximately 1 hour with a distribution half-life of ~1 hour and terminal half-life of approximately 120 hours due to peripheral tissue binding. It crosses the blood-brain barrier and demonstrates preferential accumulation in hypothalamic regions. The transient blood pressure elevation (mean systolic +6 mmHg, mean diastolic +3 mmHg) is believed to be mediated through peripheral MC1R and MC3R receptor engagement and resolves within 12 hours. Metabolized primarily via peptide hydrolysis.

Proposed mechanism

PT-141 acts as an agonist at melanocortin receptors MC3R and MC4R in the central nervous system, particularly in the hypothalamus and limbic system. Activation of these receptors triggers downstream dopaminergic and oxytocinergic signaling pathways that modulate sexual desire, arousal, and motivation. This central mechanism differentiates it from vasodilatory agents such as sildenafil, as PT-141 directly addresses the neurobiological component of sexual dysfunction.

What the evidence supports

Randomised controlled trial data in humans exists and supports use in specific contexts.

Graded Clinical

Findings supported by randomised, controlled trials in humans, with pre-registered endpoints and published results.

Key citations

Representative primary sources, including results that did not favour the compound.

  1. [1]

    Bremelanotide for Female Sexual Dysfunctions in Premenopausal Women: A Randomized, Placebo-Controlled Dose-Finding Trial (RECONNECT)

    · Obstetrics & Gynecology 134(5):899–908 · 2019

  2. [2]

    PT-141: A Melanocortin Agonist for the Treatment of Sexual Dysfunction

    · Annals of the New York Academy of Sciences 1035:330–41 · 2004

  3. [3]

    Safety and Efficacy of Bremelanotide for Hypoactive Sexual Desire Disorder: Two Randomized Phase 3 Trials

    · Obstetrics & Gynecology 134(5) · 2019

  4. [4]

    Melanocortin Receptors as Drug Targets for Disorders of Energy Homeostasis, Erectile Dysfunction, and Exocrine Gland Function

    · European Journal of Pharmacology 440(2–3):99–110 · 2003

Citation records in this build are illustrative placeholders for the design.

Reference information for research purposes. Not medical advice, and not a recommendation to use any compound. Many entries describe substances that are not approved for human use.

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