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. Image File history File links PT-141_chemical_structure_lo_res. ... Image File history File links PT-141_chemical_structure_lo_res. ... A medication is a licenced drug taken to cure or reduce symptoms of an illness or medical condition. ... Sexual problems, also called sexual dysfunction or sexual malfunction, are defined as difficulty during any stage of the sexual act (which includes desire, arousal, orgasm, and resolution) that prevents the individual or couple from enjoying sexual activity. ... Erectile dysfunction, also known as impotence, is a sexual dysfunction characterized by the inability to develop or maintain an erection of the penis for satisfactory sexual intercourse regardless of the capability of ejaculation. ... Impotence or, more clinically, erectile dysfunction is the inability to develop or maintain an erection of the penis for satisfactory sexual intercourse regardless of the capability of ejaculation. ... Sexual arousal disorder, a condition found in the DSM-IV, is generally defined as the inability to attain or maintain typical responses to sexual arousal. ... An aphrodisiac is an agent which acts on the mind and causes the arousal of the mood of sexual desire. ... Sildenafil citrate, sold under the name Viagra, is a drug used to treat male erectile dysfunction (impotence), developed by the pharmaceutical company Pfizer. ...

Originally, the compound Melanotan II that bremelanotide was developed from was tested as a sunless tanning agent. In intial 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. Melanotan and melanotan II, are analogs of the peptide hormone alpha-melanocyte stimulating hormone (α-MSH) that tend to induce skin tanning and, in the case of melanotan II, increase libido. ...

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. Peptides (from the Greek πεπτος, digestible), are the family of short molecules formed from the linking, in a defined order, of various α-amino acids. ... A lactam (the noun is a grammatical blend from lactone + amide) is a cyclic amide. ... Melanocyte-stimulating hormone (MSH) is a peptide hormone produced by cells in the intermediate lobe of the pituitary gland. ... Melanocortins are a group of pituitary peptide hormones that include adrenocorticotropin (ACTH) and the alpha, beta and gamma melanocyte stimulating hormones (MSH). ... In biochemistry, a receptor is a protein on the cell membrane or within the cytoplasm or cell nucleus that binds to a specific molecule (a ligand), such as a neurotransmitter, hormone, or other substance, and initiates the cellular response to the ligand. ... A diagram showing the CNS: 1. ... Peptide sequence or amino acid sequence is the order in which amino acid residues, connected by peptide bonds, lie in the chain. ... A metabolite is the product of metabolism. ... Melanotan and melanotan II, are analogs of the peptide hormone alpha-melanocyte stimulating hormone (α-MSH) that tend to induce skin tanning and, in the case of melanotan II, increase libido. ... The C-terminal end refers to the extremity of a protein or polypeptide terminated by an amino acid with a free carboxyl group (COOH). ... In chemistry, an amide is either the organic functional group characterized by a carbonyl group linked to a nitrogen atom, a compound that contains this functional group, or a particular inorganic anion. ... In organic chemistry functional groups are specific groups of atoms within molecules, that are responsible for the characteristic chemical reactions of those molecules. ...

In the United States it is currently in a Phase III clinical trial. In medicine, a clinical trial (synonyms: clinical studies, research protocols, medical research) is a research study. ...

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
• [1] Norman Levine, MD; researcher on Melanotan at University of Arizona Dermatology