Bremelanotide

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Chemical structure of Bremelanotide (formerly PT-141)

Bremelanotide (formerly PT-141) is the generic term for a new medication for use in treating sexual dysfunction in men (erectile dysfunction or impotence) as well as sexual dysfunction in women (sexual arousal disorder). It seems to be the first real aphrodisiac. Unlike Viagra and other related medications, it does not act upon the vascular system, but directly increases sexual desire. Bremelanotide is a spray introduced nasally.

Originally, the peptide Melanotan II that bremelanotide was developed from was tested as a sunless tanning agent. In initial testing, Melanotan II did induce tanning but additionally caused sexual arousal and spontaneous erections as unexpected side effects in eight out of the ten original male volunteer test subjects. In clinical studies, bremelanotide has been shown to be effective in treating male sexual and erectile dysfunction as well as female sexual dysfunction. It is currently being tested by Palatin Technologies.

Bremelanotide is a cyclic hepta-peptide lactam analog of alpha-melanocyte-stimulating hormone (alpha-MSH) that activates the melanocortin receptors MC3-R and MC4-R in the central nervous system. It has the amino acid sequence Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH or cyclo-[Nle⁴, Asp⁵, D-Phe⁷, Lys¹⁰]alpha-MSH-(4-10). PT-141 is a metabolite of Melanotan II that lacks the C-terminal amide function. Its molecular forumla is C₅₀H₆₈N₁₄O₁₀ with a molecular weight of 1025.2.

In the United States it is currently in a Phase IIb clinical trial.

External links

[Palatin Technologies] The company that has developed bremelanotide.
[US 6,794,489] bremelanotide (PT-141) patent (Appl. No.:040547)
[US 6,579,968] bremelanotide (PT-141) patent (Appl. No.:066501)
[Melanotan.org]
[Proc. Nat. Acad. Sci 101: 10201 (2004)] A scientific study with female rats.
[Review article] (in German).
[New York Magazine article]
[link] Norman Levine, MD; researcher on Melanotan at University of Arizona Dermatology

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