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PT-141 (Bremelanotide): A Technical Reference for Laboratory Investigation

PEPTIDE RESEARCH PT-141 (Bremelanotide): A Technical Reference for Laboratory Investigation PT-141 is a synthetic cyclic heptapeptide analog of the alpha-melanocyte-stimulating hormone (α-MSH) utilized in laboratory settings to investigate the activation of melanocortin receptors.

Overview and Classification

PT-141, also known as bremelanotide, is classified as a cyclic heptapeptide lactam. It is a structural derivative of the endogenous neuropeptide alpha-melanocyte-stimulating hormone (α-MSH). Unlike its precursor, which is a linear peptide, the cyclic structure of PT-141 is engineered to alter its binding affinity and stability within experimental models. The molecular structure and specific physical characteristics of this compound, including precise molecular weight and CAS identification, are subject to batch-specific variance. Researchers are directed to consult the provided Certificate of Analysis (COA) or the PubChem database for verified technical specifications regarding the specific lot under investigation. • Molecular Class: Cyclic heptapeptide analog. • Origin: Derived from the melanocortin receptor agonist core. • Research Application: Tool compound for receptor-ligand interaction studies.

Molecular Target and Mechanism

In laboratory research, PT-141 is identified as a non-selective agonist of the melanocortin receptor (MCR) family. Specifically, research models utilize this compound to probe the activation pathways associated with the MC3R and MC4R subtypes located within the central nervous system. The mechanism of action involves the binding of the peptide to these G-protein-coupled receptors (GPCRs). Upon binding, the compound is reported in literature to initiate intracellular signaling cascades, typically involving the modulation of cyclic adenosine monophosphate (cAMP) levels. Laboratory studies focus on the binding kinetics and the subsequent intracellular conformational changes triggered by this ligand-receptor interaction.

Why Researchers Use It

PT-141 is employed as a pharmacological tool to investigate the physiological role of the melanocortin system. Because the endogenous ligand (α-MSH) is susceptible to rapid enzymatic degradation, researchers utilize the synthetic stability of PT-141 to observe receptor signaling over extended durations in vitro. By utilizing this compound, investigators can systematically map the distribution and functional responsiveness of melanocortin receptors in various tissue cultures and neural cell lines. It serves as a probe to determine how receptor activation influences downstream signaling pathways, providing data on the sensitivity and selectivity of MCRs under controlled experimental conditions.

Research Context

The primary context for PT-141 research involves the study of the hypothalamic-pituitary axis and the broader melanocortin signaling network. Laboratory investigations often focus on how melanocortin receptor activation modulates neurotransmitter release and intracellular signaling in neural models. Current research efforts are directed toward characterizing the differences between various melanocortin receptor agonists. By comparing the binding affinity and signaling duration of PT-141 against other synthetic analogs, researchers aim to refine the understanding of how receptor-ligand topography affects signal transduction efficiency in isolated cellular environments.

Handling, Stability, and Storage for Laboratory Use

For laboratory applications, PT-141 is typically supplied as a lyophilized powder. To maintain structural integrity, the peptide should be stored in a desiccated environment at -20°C for long-term stability. Short-term storage (up to one month) may be maintained at 4°C, provided the compound is protected from light and moisture. When preparing stock solutions for in-vitro assays, researchers typically reconstitute the peptide using high-purity solvents such as sterile deionized water or an appropriate buffer solution (e.g., PBS) compatible with the specific cell line under study. If solubility requires, a minimal volume of dimethyl sulfoxide (DMSO) may be utilized as a solvent, provided that the final concentration of the vehicle does not interfere with the experimental assay. Once reconstituted, stock solutions should be aliquoted and stored at -80°C to prevent freeze-thaw degradation.

Purity and Analytical Verification

The integrity of experimental data is contingent upon the purity of the research compound. Analytical verification of PT-141 is conducted through High-Performance Liquid Chromatography (HPLC) to determine chemical purity and Mass Spectrometry (MS) to confirm molecular identity. Researchers should verify that the purity level meets the requirements of their specific assay, typically aiming for >98% purity as confirmed by HPLC. A batch-specific Certificate of Analysis (COA) is essential for any laboratory study, as it provides the necessary documentation for the specific lot’s analytical profile, including residual solvent content and peptide content analysis.

How It Relates to Other Compounds in Its Research Class

PT-141 is part of a broader class of melanocortin receptor ligands. It is frequently compared to other synthetic analogs, such as Melanotan II, which also acts on the MCR family but exhibits different receptor selectivity profiles. In research models, these compounds are distinguished by their binding affinities for the five known melanocortin receptor subtypes (MC1R through MC5R). While some analogs are engineered for higher selectivity toward specific receptor subtypes to isolate signaling pathways, PT-141 is studied for its broad-spectrum agonist activity across the central melanocortin receptors. Understanding the relative potency and selectivity of these compounds allows researchers to isolate specific signaling nodes within the melanocortin network.

Frequently Asked Research Questions

What is the primary role of PT-141 in an in-vitro assay? PT-141 is used as a tool to activate melanocortin receptors (MC3R/MC4R) to observe the resulting intracellular signaling pathways, specifically the modulation of cAMP levels and secondary messenger activation. How does the cyclic structure affect the peptide's stability? The cyclic lactam structure is designed to constrain the peptide backbone, which is reported to increase resistance to enzymatic proteolysis compared to linear peptides, thereby allowing for more consistent signaling in laboratory models. Is PT-141 selective for a single melanocortin receptor subtype? No, PT-141 is generally characterized as a non-selective melanocortin receptor agonist, meaning it interacts with multiple MCR subtypes within the neural signaling pathways being studied. What is the recommended solvent for stock preparation? Standard laboratory practice involves reconstitution in deionized water or a phosphate-buffered saline (PBS) solution. DMSO may be used as a co-solvent if necessary for solubilization, provided it is validated for the specific experimental system. Research use only — no structure/function or human-use claims are made. This information is intended for professional researchers and laboratory use only.

References

  1. National Center for Biotechnology Information — Peptides (StatPearls)
  2. NCBI Bookshelf — Molecular Biology of the Cell

Authoritative sources cited for research context. Research use only — not medical advice.