PT-141

PT-141 or Bremelanotide is the generic term for a research peptide being studied for its possible use in helping to improve sexual dysfunction in both men (erectile dysfunction or impotence) and women (sexual arousal disorder). PT-141 was developed from the tanning peptide Melanotan 2, which is a synthetically produced variant of a peptide hormone naturally produced in the body that stimulates melanogenesis which is known as alpha-Melanocyte stimulating hormone.

MSH activates certain melanocortin receptors in the process of exerting its effects. Indeed, MSH also exerts a potent influence on lipid metabolism, appetite, and sexual libido.

Resultantly, PT-141 has been shown in studies to exhibit libido-enhancing effects by activating the melanocortin receptors MC1R and MC4R, but not skin tanning. Melanotan 1 and Melanotan 2 have been researched for their use in protecting against the harmful effects of ultraviolet radiation from sunlight due to their melanogenesis-stimulating properties.

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.

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