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Bremelanotide · melanocortin agonist heptapeptide
Bremelanotide. A synthetic cyclic heptapeptide analog of alpha-melanocyte-stimulating hormone. Supplied as a lyophilized powder for research purposes only.
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Valtrax Research supplies materials strictly for in-vitro laboratory research. They are not drugs, supplements, cosmetics, or medical devices, and are not intended for human or animal use, ingestion, or administration. By ordering, you confirm you are a qualified researcher purchasing for lawful research use, in accordance with all applicable Canadian laws and regulations.
PT-141 — bremelanotide in the journals — is the active metabolite that survived when Melanotan II was put through metabolism. Strip the C-terminal amide and what remains is a cyclic heptapeptide that drops MT-II’s pigment-driving baggage and keeps the central melanocortin activity, with MC4R the receptor of interest.
That narrowing is the point. Rather than the broad tanning response of its parent, PT-141 reads through the hypothalamic melanocortin circuitry, which is the lane essentially all of its study sits in.
The work splits cleanly: receptor pharmacology on one side — how the heptapeptide engages MC4R and the other melanocortin subtypes — and behavioral/clinical endpoints on the other, where its central (not vascular) mode of action is the recurring contrast. The bremelanotide trial set supplies most of the human data.
Mechanistically PT-141 is a non-selective melanocortin agonist that matters mainly at MC4R, the receptor sitting in the hypothalamic pathways tied to sexual arousal. Unlike PDE5-type approaches, its activity is central rather than vascular, which is the distinction the literature returns to again and again.
The clinical record runs from Diamond’s early intranasal pharmacology through Clayton’s dose-finding to the Kingsberg Phase 3 program that anchored the bremelanotide approval. Borland’s 2025 hamster work adds the preclinical behavioral angle, keeping the molecule grounded in the melanocortin circuitry it was narrowed down to hit.
PT-141 is a deliberate offshoot of Melanotan II. When MT-II was studied for pigmentation, an unexpected arousal signal turned up; chemists chased that effect, deamidated the parent, and arrived at a heptapeptide that kept the central activity while shedding the tanning response.
From there it moved into its own development line under the name bremelanotide — first explored by an intranasal route, later reformulated and carried through controlled trials as a melanocortin-targeted agent.
Kingsberg, S.A. et al. (2019). Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder: Two Randomized Phase 3 Trials. Obstet Gynecol 134(5):899–908.
PubMedClayton, A.H. et al. (2016). Bremelanotide for female sexual dysfunctions in premenopausal women: a randomized, placebo-controlled dose-finding trial. Womens Health (Lond) 12(3):325–337.
PubMedDiamond, L.E. et al. (2004). Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction. Int J Impot Res 16(1):51–59.
PubMedBorland, J.M. et al. (2025). Female Syrian hamster analyses of bremelanotide, a US FDA approved drug for the treatment of female hypoactive sexual desire disorder.
PubMedThird-party tested for purity, identity, quantity.
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