PT-141: Melanocortin Receptor Agonist Research Overview
PT-141 (also known as Bremelanotide) is a synthetic cyclic heptapeptide developed as a melanocortin receptor agonist. The compound has been studied across two related research lines: as a derivative of melanotan-class peptides exploring melanocortin receptor pharmacology, and as a research tool for central nervous system sexual response signaling pathways. This page summarizes the published preclinical research.
Background
PT-141 was originally developed as a sun-tanning research compound, derived from the melanotan-class of synthetic alpha-melanocyte stimulating hormone (alpha-MSH) analogs. During early preclinical investigations, researchers observed effects on sexual response signaling in animal models that were not accounted for by skin melanogenesis, prompting a redirection of research focus to those pathways.[1]
The compound is a derivative of Melanotan II — a cyclic alpha-MSH analog with activity at multiple melanocortin receptors (MC1R, MC3R, MC4R, MC5R). PT-141 differs structurally from MT-II and shows a different selectivity profile, with research interest focused particularly on its MC4R activity.[2]
PT-141 is studied as a research reference compound. While clinical formulations exist with approved indications in specific therapeutic contexts, research-grade material supplied for laboratory use is intended exclusively for in vitro research.
Chemistry & Structure
PT-141 structural features:
- Sequence: cyclic heptapeptide based on the alpha-MSH active core (His-Phe-Arg-Trp)
- Cyclization: lactam bridge providing conformational restriction
- Length: 7 amino acids
- Molecular formula: C₅₀H₆₈N₁₄O₁₀
- Molecular weight: approximately 1,025 Da
- C-terminus: free acid
Comparison to Melanotan II
Both Melanotan II and PT-141 are cyclic heptapeptide analogs of the alpha-MSH active core. They differ in C-terminal chemistry — MT-II has an amide C-terminus, while PT-141 has a free carboxylic acid. This single structural difference affects melanocortin receptor selectivity, particularly the relative activity at MC1R (which drives melanogenesis) vs MC4R (where the sexual response signaling localizes).[2]
The cyclization in both peptides imposes a defined backbone geometry that mimics the active conformation of the alpha-MSH His-Phe-Arg-Trp motif, providing receptor agonist activity in a compact molecule.
Receptor Pharmacology
PT-141 binds and activates multiple melanocortin receptor subtypes.
Melanocortin receptor subtypes
The melanocortin receptor family includes five subtypes (MC1R through MC5R), each with distinct tissue distribution and signaling consequences. PT-141 shows agonist activity at MC1R, MC3R, MC4R, and MC5R with varying potency. MC4R activity is the primary focus of central sexual response research.[3]
MC4R signaling pathways
MC4R is expressed predominantly in the central nervous system, including hypothalamic nuclei involved in appetite, autonomic regulation, and sexual response circuits. MC4R agonist activity triggers Gs-coupled cAMP signaling, with downstream consequences including modulation of pro-opiomelanocortin (POMC) neuron activity.[4]
Documented Preclinical Research Areas
PT-141 research spans several preclinical domains.
Central sexual response signaling
The largest body of PT-141 preclinical literature examines central nervous system pathways involved in sexual response. Rodent models with standardized behavioral endpoints have been the principal substrate. The signaling is mediated through MC4R-expressing neurons in specific hypothalamic nuclei.[5]
Melanocortin receptor pharmacology
PT-141 is used as a tool compound in studies characterizing the broader melanocortin receptor family. Comparative studies pair PT-141 with subtype-selective agonists and antagonists to dissect MC1R-vs-MC4R contributions to various pathway readouts.[3]
Central appetite signaling
Because MC4R is centrally involved in appetite regulation, melanocortin agonists including PT-141 have been studied in rodent models of food intake and body weight. These studies are distinct from the sexual response research line but use overlapping receptor biology.[4]
Stability & Handling
PT-141 is a small cyclic heptapeptide. The cyclization provides structural stability, and the compound is generally robust under standard handling conditions.
Storage
Lyophilized PT-141 is stored at minus 20 degrees Celsius for long-term preservation. Refrigerated storage at 4 degrees Celsius is acceptable short-term.
Reconstitution
Bacteriostatic water or sterile water are standard reconstitution solvents. The cyclic structure dissolves cleanly in aqueous solvents.
Quality verification
HPLC for purity (≥99%), mass spectrometry for identity confirmation, and verification of intact cyclization. Each batch of Instant Peptides PT-141 ships with a full Certificate of Analysis.
Available Research Material
Instant Peptides supplies PT-141 as a synthetic lyophilized reference compound. Material is supplied to qualified research professionals. Not for human or animal consumption.
View the product page for current pricing and the Certificate of Analysis for the active batch.
Available Research Material
PT-141
Lyophilized synthetic reference compound. Independently tested for purity by HPLC and mass spectrometry. Full Certificate of Analysis included.
View product detailsReferences
- 1.Molinoff PB, Shadiack AM, Earle D, et al. PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Annals of the New York Academy of Sciences. 2003. PMID: 12846982
- 2.Hadley ME, Hruby VJ, Blanchard J, et al. Discovery and development of novel melanogenic drugs. Pharmaceutical Biotechnology. 1998. PMID: 9504951
- 3.Schiöth HB, Muceniece R, Wikberg JE. Characterisation of the melanocortin 4 receptor by radioligand binding. Pharmacology & Toxicology. 1996. PMID: 9036304
- 4.Cone RD. Anatomy and regulation of the central melanocortin system. Nature Neuroscience. 2005. PMID: 15856065
- 5.Pfaus J, Giuliano F, Gelez H. Bremelanotide: an overview of preclinical CNS effects on female sexual function. Journal of Sexual Medicine. 2007. PMID: 17970980