PT-141: a melanocortin agonist for the treatment of sexual dysfunction.
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.
Molinoff
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Palatin Technologies, Inc, Cranbury, New Jersey 08512, USA.
Shadiack
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Earle
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Diamond
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Quon
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D000281:Administration, Intranasal; D000818:Animals; D002460:Cell Line; D018592:Cross-Over Studies; D004311:Double-Blind Method; D007172:Erectile Dysfunction / Q000188:drug therapy*; D016762:Genes, fos; D006801:Humans; D008297:Male; D009474:Neurons / Q000166:cytology / Q000378:metabolism; D010286:Paraventricular Hypothalamic Nucleus / Q000166:cytology / Q000378:metabolism; D010410:Penile Erection; D010456:Peptides, Cyclic / Q000378:metabolism / Q000627:therapeutic use*; D010775:Photic Stimulation; D010919:Placebos; D051381:Rats; D017207:Rats, Sprague-Dawley; D044104:Receptor, Melanocortin, Type 3; D044105:Receptor, Melanocortin, Type 4; D018043:Receptors, Corticotropin / Q000235:genetics / Q000378:metabolism; D000521:alpha-MSH / Q000031:analogs & derivatives* / Q000378:metabolism / Q000627:therapeutic use*
D010456:Peptides, Cyclic; D010919:Placebos; D044104:Receptor, Melanocortin, Type 3; D044105:Receptor, Melanocortin, Type 4; D018043:Receptors, Corticotropin; D000521:alpha-MSH; C476721:bremelanotide