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(Ac-Nle4, Asp5, D-Phe7, Lys10)-cyclo-α-MSH (4-10); PT-141
Molecular Formula
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Erectile dysfunction & Female sexual dysfunction & Hemorrhagic shock & Reperfusion injury
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.
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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

CAS: 138890-62-7
Sequence: ---
M.W: 383.51
Molecular Formula: C12H21N3O5S3
CAS: 47931-85-1 (net)
Sequence: H-Cys-Ser-Asn-Leu-Ser-Thr-Cys-Val-Leu-Gly-Lys-Leu-Ser-Gln-Glu-Leu-His-Lys-Leu-Gln-Thr-Tyr-Pro-Arg-Thr-Asn-Thr-Gly-Ser-Gly-Thr-Pro-NH2 acetate salt (Disulfide bond)
M.W: 3431.9
Molecular Formula: C145H240N44O48S2
CAS: 37025-55-1
Sequence: Butyryl-Tyr(Me)-Ile-Gln-Asn-Cys-Pro-Leu-Gly-NH2(Disulfide bond)
M.W: 988.2
Molecular Formula: C45H69N11O12S
CAS: 38821-49-7
Sequence: ---
M.W: 244.24
Molecular Formula: C10H16N2O5
CAS: 638-23-3
Sequence: H-Cys(carboxymethyl)-OH
M.W: 179.19
Molecular Formula: C5H9NO4S

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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