PT-141 (Bremelanotide) (Research Overview)
PT-141 (Bremelanotide) is a synthetic cyclic heptapeptide analog of α-melanocyte-stimulating hormone (α-MSH). It is used in research as a melanocortin receptor agonist with activity at MC3R and MC4R.
Mechanism of Action
Bremelanotide has the structure Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH. The lactam-cyclized core preserves the His-Phe-Arg-Trp pharmacophore shared with α-MSH, and the D-Phe and norleucine substitutions are described in the literature as improving stability and receptor selectivity.
It acts on G-protein-coupled melanocortin receptors, raising intracellular cAMP in receptor-expressing cells. Pharmacology studies compare its affinity and efficacy across MC1R, MC3R, MC4R and MC5R and relate those profiles to central signaling pathways in the hypothalamus.
Research Areas
Published preclinical research has used PT-141 to study melanocortin receptor pharmacology, including receptor binding, cAMP signaling, and receptor-subtype selectivity in cell systems.
Neuroscience groups have also used it as a tool compound in animal models of central melanocortin signaling, to map hypothalamic and limbic circuits that express MC3R and MC4R.
Findings from animal or in-vitro systems do not establish safety or efficacy for any indication and should not be interpreted as medical claims.
Specification summary
PT-141 (Bremelanotide)
Stated purity ≥99%. For laboratory research use only.
Related materials
References
- Sawyer TK, Sanfilippo PJ, Hruby VJ, Engel MH, Heward CB, Burnett JB, et al. 4-Norleucine, 7-D-phenylalanine-alpha-melanocyte-stimulating hormone: a highly potent alpha-melanotropin with ultralong biological activity. Proc Natl Acad Sci U S A. 1980;77(10):5754-8. PMID 6777774 · DOI
- Voisey J, Carroll L, van Daal A. Melanocortins and their receptors and antagonists. Curr Drug Targets. 2003;4(7):586-97. PMID 14535656 · DOI
- Yuan XC, Tao YX. Ligands for Melanocortin Receptors: Beyond Melanocyte-Stimulating Hormones and Adrenocorticotropin. Biomolecules. 2022;12(10). PMID 36291616 · DOI
- Molden BM, Cooney KA, West K, Van Der Ploeg LH, Baldini G. Temporal cAMP Signaling Selectivity by Natural and Synthetic MC4R Agonists. Mol Endocrinol. 2015;29(11):1619-33. PMID 26418335 · DOI
- Ellacott KL, Cone RD. The central melanocortin system and the integration of short- and long-term regulators of energy homeostasis. Recent Prog Horm Res. 2004;59:395-408. PMID 14749511 · DOI
Cited literature is provided for scientific context only and does not describe or endorse any use of these products.
For laboratory research use only. Not for human or veterinary use. Not intended to diagnose, treat, cure, or prevent any disease.