PT-141: a melanocortin agonist for the treatment of sexual dysfunction.
Molinoff, P B, Shadiack, A M, Earle, D, Diamond, L E, Quon, C Y
PT‐141, a synthetic peptide analogue of α‐MSH, is an agonist at melanocortin receptors including the MC3R and MC4R, which are expressed primarily in the central nervous system, which suggests that PT‐141 holds promise as a new treatment for 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.
Annals of the New York Academy of Sciences (2003)
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