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