Dalargin (DALE) has originally been proposed as an antiulcer agent with cytoprotective properties; but it has been tested for other activities with promising results. Dalargin shows antioxidant; antiischemic; and wound-healing properties.
CAT No: HB00104
CAS No:81733-79-1
Synonyms/Alias:Dalargin;81733-79-1;Enkephalin-leu, ala(2)-arg(6)-;2-Ala-6-Arg-Leu-enkephalin;DALARGINE;(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid;UNII-V13505565P;DALARGIN [WHO-DD];BRN 4287455;Tyr-D-Ala-Gly-Phe-Leu-Arg;2-D-Alanine-1-6-beta-neoendorphin (human);DTXSID50231302;1-6-(D-ALA2)-DYNORPHIN;Tyrosyl-D-alanyl-glycyl-phenylalanyl-leucyl-arginine;tageflar;V13505565P;1-6-beta-Neoendorphin (human), 2-D-alanine-;N(sup 2)-(N-(N-(N-(L-Tyrosyl-D-alanyl)glycyl)-L-phenylalanyl)-L-leucyl)-L-arginine;1-6-.BETA.-NEOENDORPHIN (HUMAN), 2-D-ALANINE-;L-ARGININE, L-TYROSYL-D-ALANYLGLYCYL-L-PHENYLALANYL-L-LEUCYL-;L-Arginine, N(sup 2)-(N-(N-(N-(L-tyrosyl-D-alanyl)glycyl)-L-phenylalanyl)-L-leucyl)-;Tyr-Ala-Gly-Phe-Leu-Arg;Leu-enkephalin, Ala(2)-Arg(6)-;leucine-enkephalin, Ala(2)-Arg(6)-;enkephalin, Ala(2)-Leu(5)-Arg(6)-;enkephalin-Leu, alanyl(2)-arginine(6)-;(D-Ala2)-Leu-Enkephalin-Arg acetate salt;tyrosyl-alanyl-glycyl-phenylalanyl--leucyl-arginine;DTXCID10153793;EX-A5715;H-Tyr-D-Ala-Gly-Phe-Leu-Arg-OH;HY-P4053;FA108952;CS-0635584;Q27291394;(2S,5S,8S,14R,17S)-17-amino-8-benzyl-2-(3-guanidinopropyl)-18-(4-hydroxyphenyl)-5-isobutyl-14-methyl-4,7,10,13,16-pentaoxo-3,6,9,12,15-pentaazaoctadecan-1-oic acid;
DALARGIN is a synthetic hexapeptide belonging to the class of opioid peptides, structurally related to enkephalins and endorphins. As a biologically active peptide, it interacts primarily with opioid receptors in the central nervous system, exhibiting notable affinity for the delta and mu subtypes. Its unique sequence and receptor selectivity have made it a valuable tool in neuropharmacological research, particularly for probing endogenous opioid pathways and mechanisms of pain modulation. DALARGIN's stability and defined activity profile further enhance its utility in experimental models focused on neurobiology, receptor signaling, and peptide-receptor interactions.
Receptor binding studies: DALARGIN serves as a reference ligand for characterizing opioid receptor subtypes in vitro. Its defined affinity for delta and mu opioid receptors allows researchers to delineate receptor distribution, binding kinetics, and competitive interactions with other endogenous or synthetic peptides. Through radioligand binding assays and displacement studies, scientists can utilize DALARGIN to map receptor populations, quantify receptor density, and investigate the molecular determinants of ligand selectivity, which are critical for advancing opioid pharmacology.
Signal transduction analysis: The peptide is widely used to investigate downstream signaling events initiated by opioid receptor activation. By applying DALARGIN to cultured neuronal or heterologous expression systems, researchers can monitor changes in second messenger pathways, such as inhibition of adenylyl cyclase activity or modulation of ion channel conductance. These studies provide mechanistic insights into how opioid peptides regulate cellular excitability, neurotransmitter release, and synaptic plasticity, contributing to a comprehensive understanding of neuromodulation.
Peptide-receptor interaction modeling: The defined amino acid sequence and receptor specificity of DALARGIN make it an ideal candidate for structural and computational modeling. Researchers employ it in molecular docking simulations, NMR spectroscopy, and crystallography to elucidate the conformational dynamics of peptide-receptor complexes. These investigations aid in identifying key interaction motifs, informing the rational design of novel peptide analogs with tailored pharmacological profiles and improved receptor selectivity.
Peptide stability and degradation studies: As a synthetic peptide, DALARGIN is frequently used to assess the metabolic stability and proteolytic degradation of opioid peptides in biological matrices. By tracking its breakdown products in plasma, tissue homogenates, or cell culture, investigators can evaluate the influence of peptidases and other proteolytic enzymes on peptide half-life and bioavailability. Such studies are essential for optimizing peptide-based research tools and for understanding the factors that govern peptide persistence in experimental systems.
Analytical method development: DALARGIN is also employed as a standard or reference compound in the development and validation of analytical techniques for peptide quantification. Its well-characterized properties facilitate the calibration of HPLC, mass spectrometry, and immunoassay platforms, enabling precise measurement of peptide concentrations in complex biological samples. These analytical applications support rigorous pharmacokinetic, biodistribution, and metabolism studies, ensuring reliable data generation in peptide research workflows.
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