Deltorphin is a peptide enriched in aromatic and acidic residues, forming motifs that influence helix-loop transitions. The sequence supports research into receptor-like recognition, hydrophobic clustering, and solvent-dependent conformations. Researchers use it to study packing interactions and backbone dynamics. Its defined architecture aids rigorous biophysical profiling.
CAT No: R2237
CAS No:119975-64-3
Synonyms/Alias:Deltorphin;119975-64-3;Dermenkephalin;Deltorphin A;L-alpha-Asparagine, L-tyrosyl-D-methionyl-L-phenylalanyl-L-histidyl-L-leucyl-L-methionyl-;Tyr-met-phe-his-leu-met-asp-NH2;CHEMBL20775;CHEBI:81455;DTXSID60152630;Tyrosyl-methionyl-phenylalanyl-histidyl-leucyl-methionyl-aspartamide;(3S)-4-amino-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-oxobutanoic acid;(5R,8S,11S,14S,17S,20S)-11-((1H-imidazol-4-yl)methyl)-5-((S)-2-amino-3-(4-hydroxyphenyl)propanamido)-8-benzyl-20-carbamoyl-14-isobutyl-17-(2-(methylthio)ethyl)-6,9,12,15,18-pentaoxo-2-thia-7,10,13,16,19-pentaazadocosan-22-oic acid;L-alpha-Asparagine, N2-(N-(N-(N-(N-(N-L-tyrosyl-D-methionyl)-L-phenylalanyl)-L-histidyl)-L-leucyl)-L-methionyl)-;H-Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2;DTXCID3075121;GLXC-25917;3-(2-{2-[2-(2-{2-[2-Amino-3-(4-hydroxy-phenyl)-propionylamino]-4-methylsulfanyl-butyrylamino}-3-phenyl-propionylamino)-3-(3H-imidazol-4-yl)-propionylamino]-4-methyl-pentanoylamino}-4-methylsulfanyl-butyrylamino)-succinamic acid;BDBM50000518;AKOS037647558;AKOS040744531;AS-74086;DA-72655;H-Tyr-(D)Met-Phe-His-Leu-Met-Asp-NH2;HY-129271;CS-0104599;C18010;G77949;Q5254878;3-(2-{2-[2-(2-{2-[2-Amino-3-(4-hydroxy-phenyl)-propionylamino]-4-methylsulfanyl-butyrylamino}-3-phenyl-propionylamino)-3-(3H-imidazol-4-yl)-propionylamino]-4-methyl-pentanoylamino}-4-methylsulfanyl-butyrylamino)-succinamic acid (deltorphin A);
Deltorphin, a naturally occurring heptapeptide opioid, is renowned for its exceptional selectivity and affinity for delta-opioid receptors. Isolated originally from amphibian skin, this compound has become a valuable tool in neuroscience and pharmacological research due to its potent biological activity and unique receptor specificity. Unlike many other opioid peptides, deltorphin demonstrates a high degree of resistance to enzymatic degradation, enabling it to maintain its bioactivity for extended periods during experimental applications. Its well-defined structure and high receptor selectivity make it an indispensable molecule for dissecting the physiological and biochemical roles of delta-opioid receptors in various biological systems. Researchers often utilize deltorphin to probe receptor-ligand interactions, investigate signal transduction pathways, and explore the broader implications of delta-opioid modulation in the central nervous system and peripheral tissues.
Receptor Pharmacology: Deltorphin serves as a gold-standard ligand for studying delta-opioid receptor pharmacology. Its exceptional selectivity allows scientists to distinguish delta-opioid receptor-mediated effects from those mediated by mu- or kappa-opioid receptors, providing clarity in receptor subtype research. By employing this peptide in binding assays and functional studies, researchers can characterize the distribution, density, and functional properties of delta-opioid receptors in neural and non-neural tissues. This specificity aids in mapping receptor localization and understanding receptor-mediated signaling mechanisms, advancing our knowledge of opioid receptor biology.
Neuroscience Research: In neurobiological investigations, deltorphin is widely used to elucidate the role of delta-opioid receptors in modulating neurotransmitter release, synaptic plasticity, and neuronal excitability. When applied to neural tissue preparations or in vivo models, it enables the dissection of delta-opioid receptor contributions to pain perception, mood regulation, and neuroprotection. Its ability to selectively activate these receptors makes it a vital tool for studying endogenous opioid systems and their interactions with other neurotransmitter pathways, ultimately deepening our understanding of brain function and behavior.
Peptide Structure-Activity Relationship (SAR) Studies: The well-characterized amino acid sequence and receptor-binding profile of deltorphin make it an ideal candidate for structure-activity relationship (SAR) analyses. By synthesizing analogs and derivatives of this peptide, researchers can systematically investigate how specific structural modifications impact receptor affinity, selectivity, and biological activity. These studies are instrumental in identifying key pharmacophores and guiding the rational design of novel delta-opioid ligands with improved properties for experimental or therapeutic exploration.
Drug Discovery and Development: Deltorphin's high receptor selectivity and resistance to enzymatic degradation position it as a valuable template for the development of new delta-opioid receptor agonists. Medicinal chemists utilize it as a starting point to design and synthesize compounds with enhanced bioavailability, stability, and receptor specificity. These efforts contribute to the identification of lead molecules for further pharmacological evaluation, supporting the early stages of drug discovery programs targeting the delta-opioid system for a range of potential applications.
Signal Transduction Pathway Analysis: The use of deltorphin in cellular and molecular studies facilitates the investigation of intracellular signaling cascades activated by delta-opioid receptor engagement. By applying this peptide to cultured cells or tissue samples, researchers can monitor downstream effects such as G-protein activation, second messenger production, and gene expression changes. These insights are critical for unraveling the complex network of signaling events associated with delta-opioid receptor activation and for identifying novel molecular targets within these pathways.
Behavioral Pharmacology: In behavioral studies, deltorphin is employed to assess the functional outcomes of delta-opioid receptor activation on animal models. Its application enables researchers to evaluate changes in nociception, reward processing, anxiety-like behaviors, and locomotor activity, thereby revealing the physiological relevance of delta-opioid signaling in various behavioral paradigms. These investigations provide a foundation for understanding how modulation of delta-opioid receptors influences complex behaviors and may inform future research directions in neuropsychopharmacology.
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