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PT-141 is a synthetic analog of a natural, endogenous peptide known as alpha-MSH. As a result, it stimulates similar receptors and has similar results throughout the body. Alpha-MSH is a melanocortin, a set of hormones that regulate a large range of physical functions. Acting on the melanocortin 1 receptor produces the effects of PT-141, providing varying effects when interacting in different parts of the brain. They include sexual arousal and functioning, and appetite suppression.

Studies have been conducted on PT-141 since it was first synthesized in the 1960s. During routine studies, a researcher injected himself with twice the intended dose. He went on to experience an 8 hour erection.Later studies have shown potential efficacy in treating female sexual dysfunction.

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