A highly selective, potent antagonist for the opioid δ-receptor. It exhibits partial agonist in vitro activity at δ receptors at high concentrations.
CAT No: R1076
CAS No:89352-67-0
Synonyms/Alias:ICI 174,864;92535-15-4;N,N-diallyl-Tyr-Aib-Aib-Phe-Leu;89352-67-0;Ici 174865;Ici 174,865;N,N-Diallyl-tyr-aib-aib-phe-leu-OH;ICI-174865;ICI-174,865;CHEMBL47545;N,N-Diallyl-tyrosyl-aminoisobutyryl-aminoisobutyryl-phenylalanyl-leucine;L-Leucine, N-(N-(N-(N-(N,N-di-2-propenyl-L-tyrosyl)-2-methylalanyl)-2-methylalanyl)-L-phenylalanyl)-;N-(N-(N-(N-(N,N-di-2-Propenyl-L-tyrosyl)-2-methylalanyl)-2-methylalanyl)-L-phenylalanyl)-L-leucine;(2S)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-[bis(prop-2-enyl)amino]-3-(4-hydroxyphenyl)propanoyl]amino]-2-methylpropanoyl]amino]-2-methylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoic acid;(2S,5S,14S)-15-allyl-5-benzyl-14-(4-hydroxybenzyl)-2-isobutyl-8,8,11,11-tetramethyl-4,7,10,13-tetraoxo-3,6,9,12,15-pentaazaoctadec-17-en-1-oic acid;NIH10893;DTXSID10919119;BDBM50006946;AKOS024458657;DA-54236;PD071343;CS-0134163;L-Leucine,N,N-di-2-propen-1-yl-L-tyrosyl-2-methylalanyl-L-phenylalanyl-;L-Leucine, N,N-di-2-propen-1-yl-L-tyrosyl-2-methylalanyl-2-methylalanyl-L-phenylalanyl-;2-[2-(2-{2-[2-Diallylamino-3-(4-hydroxy-phenyl)-propionylamino]-2-methyl-propionylamino}-2-methyl-propionylamino)-3-phenyl-propionylamino]-4-methyl-pentanoic acid;N-{2-Benzyl-1,4,7,10-tetrahydroxy-11-[(4-hydroxyphenyl)methyl]-5,5,8,8-tetramethyl-12-(prop-2-en-1-yl)-3,6,9,12-tetraazapentadeca-3,6,9,14-tetraen-1-ylidene}leucine;
ICI 174,864 is a synthetic peptide compound recognized as a highly selective antagonist of the delta opioid receptor (DOR). Structurally, it is a peptide-based molecule designed to interact specifically with opioid receptor subtypes, making it a valuable tool in neuropharmacological and receptor signaling studies. Its high affinity and selectivity for the DOR have positioned it as an essential reagent for dissecting the physiological and biochemical roles of delta opioid receptors in various experimental models. The compound is widely utilized in academic and industrial research settings to probe the intricacies of opioid receptor function, signal transduction, and ligand-receptor interactions.
Receptor Pharmacology: ICI 174,864 is extensively used to characterize the pharmacological properties of delta opioid receptors in both in vitro and in vivo systems. By selectively blocking DOR-mediated responses, researchers can delineate the contribution of this receptor subtype to physiological processes such as pain modulation, mood regulation, and neuroprotection. Its use enables the isolation of DOR-specific pathways from those mediated by other opioid receptors, thereby providing precise insights into receptor pharmacodynamics and downstream signaling events.
Signal Transduction Studies: The compound serves as a powerful tool for investigating intracellular signaling cascades initiated by delta opioid receptor activation. By antagonizing DOR, it allows researchers to evaluate the impact of receptor inhibition on second messenger systems, such as cyclic AMP production, calcium flux, and protein kinase activation. These studies are critical for unraveling the molecular mechanisms underlying opioid receptor function and for identifying potential targets for further pharmacological intervention.
Ligand Binding Assays: ICI 174,864 is frequently employed in radioligand binding assays and competition studies to assess the affinity and selectivity of novel opioid ligands. Its well-characterized binding profile makes it an ideal reference compound for validating assay systems and for benchmarking the binding properties of experimental molecules. Utilizing this antagonist in binding studies supports the development of new DOR-targeted compounds and enhances the reliability of receptor-ligand interaction data.
Neuroscience Research: In the field of neuroscience, ICI 174,864 is utilized to dissect the role of delta opioid receptors in neural circuitry, synaptic plasticity, and neurotransmitter release. Its ability to selectively inhibit DOR function enables detailed exploration of receptor involvement in behavioral paradigms, neurochemical modulation, and neurodevelopmental processes. The compound's application in brain slice preparations, cultured neurons, and animal models contributes to a deeper understanding of opioid receptor dynamics within the central nervous system.
Peptide Structure-Activity Relationship (SAR) Analysis: As a synthetic peptide antagonist, ICI 174,864 provides a template for structure-activity relationship studies aimed at optimizing receptor selectivity and potency. Researchers employ it to investigate the influence of specific amino acid substitutions and conformational constraints on DOR binding and antagonistic activity. These SAR investigations inform the rational design of next-generation peptide ligands with improved pharmacological profiles, supporting the advancement of peptide-based drug discovery and molecular pharmacology research.
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