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Bremelanotide

CAT#
10-101-112
Synonyms/Alias
(Ac-Nle4, Asp5, D-Phe7, Lys10)-cyclo-α-MSH (4-10); PT-141
CAS No.
189691-06-3
Sequence
Ac-Nle-cyclo(-Asp-His-D-Phe-Arg-Trp-Lys-OH)
M.W/Mr.
1025.18
Molecular Formula
C50H68N14O10
Source
Synthetic
Long-term Storage Conditions
−20°C
Application
Erectile dysfunction & Female sexual dysfunction & Hemorrhagic shock & Reperfusion injury
Description
Bremelanotide, formerly known as PT-141, is a peptide drug. Similarly to its analogues α-MSH and melanotan II, bremelanotide acts as a non-selective agonist of all of the melanocortin receptors except MC2.
Areas of Interest
Diseases

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PT-141, also called as Bremelanotide, is a derivative for Melanotan 2 (M2). Unlike M2, PT-141 lacks C-terminal amide molecules. PT-141, a synthetic cyclic hepta-peptide lactam derivative of alpha-Melanocyte-stimulating hormone (alpha-MSH), is an agonist at melanocortin receptors including the MC3R and MC4R, which are expressed primarily in the central nervous system. Melanocortin receptors are members of the rhodopsin family of 7-transmembrane G protein-coupled receptors. There are five known members of the melanocortin receptor system each with differing specificities for melanocortins: MC1R; MC2R; MC3R; MC4R; MC5R.  >> Read More

Bremelanotide is an analogue of the naturally occurring peptide alpha-melanocyte-stimulating hormone (alpha-MSH). It stimulates erection in men and male rats, and is currently in clinical trials for the treatment of erectile dysfunction.

Pfaus J, Giuliano F, Gelez H. Bremelanotide: an overview of preclinical CNS effects on female sexual function[J]. The journal of sexual medicine, 2007, 4(s4): 269-279.

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 P B, Shadiack A M, Earle D, et al. PT‐141: a melanocortin agonist for the treatment of sexual dysfunction[J]. Annals of the New York Academy of Sciences, 2003, 994(1): 96-102.

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