PT-141

Receptor Agonist
Chemical Profile
Molecular Formula
C50H68N14O10
Molar Mass
1,025.18 g/mol
CAS Number
189691-06-3
Purity Standard
99%+ (HPLC Verified)
Amino Acid Sequence
Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH

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Overview

PT-141 (Bremelanotide) is a cyclic heptapeptide that acts as a melanocortin receptor agonist, with particular affinity for the MC3 and MC4 receptor subtypes. It was originally developed from the linear alpha-melanocyte-stimulating hormone (alpha-MSH) peptide Melanotan II, with structural modifications that enhance its selectivity for central nervous system melanocortin receptors.

Unlike compounds that act on peripheral vascular mechanisms, PT-141 works through direct activation of CNS melanocortin pathways, making it a unique tool for researchers studying the neurological basis of sexual function and arousal. This central mechanism of action has made it one of the most interesting peptides in neuroendocrine research.

PT-141's cyclic structure confers enhanced enzymatic stability compared to linear peptide analogs, and its melanocortin receptor selectivity profile provides researchers with a relatively targeted tool for investigating MC3R/MC4R-mediated signaling pathways.

The compound has been extensively studied in both animal models and clinical research settings, contributing significantly to our understanding of melanocortin system involvement in sexual function, energy balance, and social behavior.

Synthesis Overview

PT-141 (Bremelanotide) is synthesized using a combination of solid-phase peptide synthesis and selective cyclization chemistry. The linear precursor is assembled on a solid support using Fmoc-SPPS, incorporating the unnatural amino acids norleucine (Nle) and D-phenylalanine (D-Phe). Following cleavage from the resin, the side-chain cyclization between aspartic acid and lysine residues is performed in solution phase. The resulting cyclic peptide is purified via reverse-phase HPLC and lyophilized to a stable powder.

Research Applications

  • Melanocortin receptor (MC3R/MC4R) binding and activation studies
  • Central nervous system signaling pathway research
  • Melanocortin system role in sexual function investigation
  • Appetite and energy homeostasis modulation research
  • Blood-brain barrier penetration studies
  • Comparative melanocortin receptor selectivity analysis

Related Compounds