PT-141 (Bremelanotide) 10mg

PT-141 (Bremelanotide) 10mg is a synthetic research compound intended for use in in vitro laboratory experiments only. PT-141 is a heptamer (containing 7 amino acids). PT-141, also known as Bremelanotide, acts as an agonist for melanocortin receptors, triggering the signals. PT-141 mimics alpha-melanocyte-stimulating hormone (α-MSH). Different cell lines are being tested to see the effect of PT-141 on cell functions. The half-life of the peptide is a few minutes; nevertheless, once engaging with the cells, the peptide has shown its effects for up to 72 minutes.

Following subcutaneous or intracerebroventricular (ICV) administration in rats, PT-141 selectively increases measures of solicitation. ⁽¹⁾ Importantly, the peptide did not cause any changes in the locomotion of animals, indicating its specificity. The peptide acts as an agonist at melanocortin-1 and 4 receptors (MC1R and MC4R). MCR4s are found to be associated with the modulation of sexual function. ⁽²⁾ PT-141 has been tested for its stimulant effect on female sexual desire as well as male erectile dysfunction. ^(2,3)  Studies have shown that a subcutaneous injection of PT-141 45 minutes before sexual activity improves sexual desire and reduces sexual stress. ⁽³⁾ According to one study, co-administration of PT-141 with stimulants like sildenafil or MCR agonists improved erectile response in men, compared to control groups receiving vehicle or monotherapy. ⁽⁴⁾The mechanism associated with PT-141’s effect on erectile function is nitric oxide generation. ⁽⁵⁾

Some studies have shown that PT-141 may cause liver toxicity, indicated by a marked rise in blood aminotransferase levels, a small increase in alkaline phosphatase, and mild jaundice. ⁽³⁾ However, there have not been any acute or chronic liver failures attributed to PT-141 so far. PT-141 can be used for in vitro experiments with its specific effects on MCRs.

The peptide comes as a lyophilized white powder in a vial with a concentration of 10 mg/vial.

References: 1. Pfaus J, Giuliano F, Gelez H. J Sex Med. Bremelanotide: an overview of preclinical CNS effects on female sexual function. 2007;4 Suppl 4:269-79. 2.  Hedlund P. PT-141 Palatin. Curr Opin Investig Drugs. 2004;5(4):456-62. 3. LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. 4.Diamond LE, Earle DC, Garcia WD, Spana C. Co-administration of low doses of intranasal PT-141, a melanocortin receptor agonist, and sildenafil to men with erectile dysfunction results in an enhanced erectile response.Urology. 2005;65(4):755-9. 5. Molinoff PB, Shadiack AM, Earle D, Diamond LE, Quon CY. PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Ann N Y Acad Sci. 2003;994:96-102.