Study summary · research use only
Melanocortins in the treatment of male and female sexual dysfunction
Plain-language summary
Paraphrased from the published abstract below — not a verdict on whether anything works.
This review discusses melanocortinergic agents being investigated for male and female sexual dysfunction. The authors describe that systemic administration of the alpha-MSH analog MT-II was reported to cause penile erections across several species including humans, and that agents such as HP-228, THIQ, and bremelanotide (PT-141) show erectogenic properties attributed to central melanocortin receptor binding. They state bremelanotide, a nasally administered synthetic peptide, is the only such agent clinically studied in both males and females, with Phase II clinical trial data cited in support of melanocortin-based therapy for erectile dysfunction. Animal studies were reported to show pre-copulatory behaviors in female rats, and preliminary clinical data are said to suggest a role in sexual desire and arousal in women. The review characterizes the proposed central sites and mechanisms.
Abstract
Melanocortinergic agents are currently being investigated for a possible therapeutic role in male and female sexual dysfunction. These investigations were sparked by findings that systemic administration of a synthetic analog of alpha-MSH, MT-II, causes penile erections in a variety of species, including humans. Several other melanocortinergic agents including HP-228, THIQ, and bremelanotide (PT-141) have since been shown to have erectogenic properties thought to be due to binding to melanocortin receptors in the central nervous system, particularly the hypothalamus. Bremelanotide, a nasally administered synthetic peptide, is the only melanocortinergic agent that has been clinically studied in both males and females. Data from Phase II clinical trials of bremelanotide support the use of melanocortin-based therapy for erectile dysfunction. Studies using animal models have demonstrated that pre-copulatory behaviors in female rats analogous to sexual arousal are evoked, and preliminary clinical data also suggest a role in promoting sexual desire and arousal in women. Based on bremelanotide clinical experience, administration of a melanocortin agonist is well tolerated and not associated the hypotension observed with phosphodiesterase-5 inhibitors currently used to treat erectile dysfunction. This review discusses investigations of melanocortin agonists for the treatment of sexual dysfunction with emphasis on proposed sites and mechanisms of action in the central nervous system that appear to be involved in melanocortinergic modulation of sexual function. Current research validates use of melanocortinergic agents for the treatment of both male and female sexual dysfunction.
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