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

Ann N Y Acad Sci. 2003 Jun;994:96-102. doi: 10.1111/j.1749-6632.2003.tb03167.x.

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.

Publication types

  • Clinical Trial

MeSH terms

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

Substances

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