PT-141: a melanocortin agonist for the treatment of sexual dysfunction.

Abstract

PT-141, a synthetic peptide analogue of alpha-MSH, is an agonist at melanocortin receptors including the MC3R and MC4R, which are expressed primarily in the central nervous system. Administration of PT-141 to rats and nonhuman primates results in penile erections. Systemic administration of PT-141 to rats activates neurons in the hypothalamus as shown by an increase in c-Fos immunoreactivity. Neurons in the same region of the central nervous system take up pseudorabies virus injected into the corpus cavernosum of the rat penis. Administration of PT-141 to normal men and to patients with erectile dysfunction resulted in a rapid dose-dependent increase in erectile activity. The results suggest that PT-141 holds promise as a new treatment for sexual dysfunction.

• Authors: P B Molinoff, A M Shadiack, D Earle, L E Diamond, C Y Quon
• Journal: Annals of the New York Academy of Sciences (Ann N Y Acad Sci) Vol. 994 Pg. 96-102 (Jun 2003) ISSN: 0077-8923 [Print] United States
• PMID: 12851303 (Publication Type: Clinical Trial, Journal Article)

Chemical References

• Peptides, Cyclic
• Placebos
• Receptor, Melanocortin, Type 3
• Receptor, Melanocortin, Type 4
• Receptors, Corticotropin
• alpha-MSH
• bremelanotide

Topics

• Administration, Intranasal
• Animals
• Cell Line
• Cross-Over Studies
• Double-Blind Method
• Erectile Dysfunction (drug therapy)
• Genes, fos
• Humans
• Male
• Neurons (cytology, metabolism)
• Paraventricular Hypothalamic Nucleus (cytology, metabolism)
• Penile Erection
• Peptides, Cyclic (metabolism, therapeutic use)
• Photic Stimulation
• Placebos
• Rats
• Rats, Sprague-Dawley
• Receptor, Melanocortin, Type 3
• Receptor, Melanocortin, Type 4
• Receptors, Corticotropin (genetics, metabolism)
• alpha-MSH (analogs & derivatives, metabolism, therapeutic use)