Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current with an IC50 of 42.0 μM.
CAT No: R1330
Dynorphin A (1-10) TFA is a synthetic peptide fragment derived from the endogenous opioid peptide dynorphin A, corresponding to its N-terminal ten amino acids and presented as the trifluoroacetate salt. As a member of the opioid peptide family, it exhibits significant relevance in neurobiological and pharmacological research due to its ability to interact with opioid receptors, particularly the kappa opioid receptor (KOR). The truncated sequence preserves key residues essential for receptor binding and biological activity, making it a valuable tool for dissecting the structure-activity relationships and functional roles of dynorphin peptides in the central nervous system. Its defined sequence and physicochemical properties also support its use in a variety of experimental models aimed at elucidating the mechanisms of opioid signaling and peptide-mediated neuromodulation.
Receptor Binding Studies: Dynorphin A (1-10) TFA is widely utilized in receptor pharmacology to investigate the binding affinities and selectivity profiles of opioid receptor subtypes, especially KOR. By employing this peptide in radioligand binding assays or competition studies, researchers can delineate the contributions of the N-terminal region to receptor interaction, compare its potency to full-length dynorphin A, and map critical residues responsible for receptor activation or antagonism. These insights are fundamental for advancing the understanding of opioid receptor pharmacodynamics and for guiding the design of next-generation receptor ligands.
Neuroscience Research: The peptide serves as a model compound for probing the physiological and pathophysiological roles of endogenous opioid systems in the brain and spinal cord. Experimental use in electrophysiological recordings, neurotransmitter release assays, and behavioral paradigms allows for detailed examination of its effects on synaptic transmission, neuronal excitability, and neuroplasticity. The fragment's activity profile is particularly relevant for exploring the mechanisms underlying pain modulation, stress responses, and the regulation of emotional and cognitive processes mediated by KOR signaling.
Peptide Structure-Activity Relationship (SAR) Analysis: Researchers leverage Dynorphin A (1-10) TFA in systematic SAR studies to dissect how specific amino acid sequences and modifications influence opioid peptide function. By comparing the biological activities of truncated, mutated, or chemically modified analogs, investigators can identify structural determinants of receptor affinity, selectivity, and efficacy. These findings not only elucidate the molecular basis of dynorphin receptor interactions but also inform the development of novel peptide-based probes and therapeutic leads.
Peptide Synthesis and Analytical Standards: As a well-characterized synthetic fragment, this peptide is frequently used as a reference material in peptide synthesis workflows and analytical method development. Its defined sequence and established chromatographic behavior make it suitable for calibrating analytical instruments such as HPLC or mass spectrometry, validating peptide purification protocols, and benchmarking the quality of custom-synthesized opioid peptides. Such applications are essential for ensuring reproducibility and accuracy in peptide research and production environments.
Intracellular Signaling Investigations: The ability of Dynorphin A (1-10) TFA to activate KOR and modulate downstream signaling cascades makes it a valuable reagent for studying intracellular pathways linked to opioid receptor activation. Use in cell-based assays enables the assessment of G-protein coupling, second messenger modulation, and kinase activation in response to peptide stimulation. These studies provide crucial insights into the cellular mechanisms by which opioid peptides influence physiological and pathophysiological processes, supporting broader research into signal transduction and neuropharmacology.
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