DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist.
CAT No: R1322
CAS No:78123-71-4
Synonyms/Alias:DAMGO;DAGO;78123-71-4;glyol;Dagol;DAMGE;2-Ala-4-mephe-5-gly-enkephalin;Tyr-ala-gly-(nme)phe-gly-ol;RX 783006;(D-Ala(2)-mephe(4)-gly-ol(5))enkephalin;(2S)-2-amino-N-[(2R)-1-[[2-[[(2S)-1-(2-hydroxyethylamino)-1-oxo-3-phenylpropan-2-yl]-methylamino]-2-oxoethyl]amino]-1-oxopropan-2-yl]-3-(4-hydroxyphenyl)propanamide;Enkephalin, ala(2)-mephe(4)-gly(5)-;CHEBI:272;CHEMBL38874;Tyr-D-Ala-Gly-MePhe-Gly-ol;Enkephalin, alanyl(2)-methylphenylalanyl(4)-glycine(5)-;950492-85-0;[3H]DAMGO;Tyr-D-Ala-Gly-MePhe-Gly(ol);Tyr-D-Ala-Gly-NMe-Phe-Gly-ol;Tyr-D-Ala-Gly-(NMe)Phe-Gly-ol;Tyr-D-Ala-Gly-N(Me)Phe-Gly-ol;Tyr-D-Ala-Gly-N-Me-Phe-Gly-ol;Ala(2)-mephe(4)-gly-ol(5) enkephalin;Tyr-D-Ala-Gly-N-Methyl-Phe-Gly-ol;D-Ala2-MePhe4-Met(0)5-enkephalin-ol;Enkephalin, Ala(2)-MePhe(4)-Gly-ol(5)-;C26H35N5O6;H-Tyr-D-Ala-Gly-N-Me-Phe-Glycinol;[D-Ala2, NMe-Phe4, Gly-ol5]-enkephalin;2YM5VT3MNR;RX783006;Dagol;L-Phenylalaninamide, L-tyrosyl-D-alanylglycyl-N-(2-hydroxyethyl)-Nalpha-methyl-;Tyr-DAla-Gly-MePhe-Gly-ol;SCHEMBL725750;GTPL1647;Tyr-D-Ala-Gly-NMePhe-Gly-ol;BDBM21015;H-Tyr-D-Ala-Gly-MePhe-Gly-ol;Tyr-D-Ala2-Gly-NMePhe-Gly-ol;DTXSID30228775;HPZJMUBDEAMBFI-WTNAPCKOSA-N;HY-P0210;Tyr-D-Ala-Gly-N(CH3)Phe-Gly-ol;H-Tyr-D-Ala-Gly-N(Me)Phe-Gly-ol;HB2409;AKOS024456435;NCGC00167303-01;(2S)-2-[[2-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]acetyl]-methylamino]-N-(2-hydroxyethyl)-3-phenylpropanamide;AS-83278;BD173150;BD174973;DA-72545;CS-0021316;G12226;Q5204254;[tyrosyl-3,5-3H(N)]-D-Ala2-Mephe4-glyol5-enkephalin;3: PN: WO2009046859 PAGE: 98 CLAIMED PROTEIN;158: PN: US20030176421 PAGE: 54-55 CLAIMED PROTEIN;L-TYROSYL-D-ALANYLGLYCYL-N-(2-HYDROXYETHYL)-N.ALPHA.-METHYL-L-PHENYLALANINAMIDE;L-Tyrosyl-D-alanylglycyl-N-(2-hydroxyethyl)-Nalpha-methyl-L-phenylalaninamide;(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]-N-methylacetamido}-N-(2-hydroxyethyl)-3-phenylpropanamide;(2S)-2-amino-N-[(1R)-2-[[2-[[(1S)-1-benzyl-2-(2-hydroxyethylamino)-2-oxo-ethyl]-methyl-amino]-2-oxo-ethyl]amino]-1-methyl-2-oxo-ethyl]-3-(4-hydroxyphenyl)propanamide;(S)-2-amino-N-((R)-1-(2-(((S)-1-(2-hydroxyethylamino)-1-oxo-3-phenylpropan-2-yl)(methyl)amino)-2-oxoethylamino)-1-oxopropan-2-yl)-3-(4-hydroxyphenyl)propanamide;Benzenepropanimidic?acid, .alpha.-amino-4-hydroxy-N-[(1R,2Z)-2-hydroxy-2-[[2-[[(1S,2Z)-2-hydroxy-2-[(2-hydroxyethyl)imino]-1-(phenylmethyl)ethyl]methylamino]-2-oxoethyl]imino]-1-methylethyl]-, (.alpha.S)-;
DAMGO (Tyr-D-Ala-Gly-N-MePhe-Gly-ol) is a synthetic peptide that functions as a highly selective agonist for the mu-opioid receptor (MOR). Structurally derived from the endogenous opioid peptide enkephalin, DAMGO is engineered to enhance receptor specificity, metabolic stability, and resistance to enzymatic degradation. Its unique sequence and modified residues confer high affinity and selectivity for MOR, making it a valuable molecular tool within neuropharmacology, pain research, and receptor signaling studies. DAMGO's ability to mimic the action of endogenous opioids while offering improved experimental control has established it as a gold standard ligand for probing mu-opioid receptor function in both in vitro and in vivo models.
Receptor Pharmacology: DAMGO is extensively employed in receptor pharmacology to characterize the binding properties, activation mechanisms, and downstream signaling pathways of mu-opioid receptors. Its high selectivity enables researchers to isolate MOR-mediated responses from those of delta and kappa opioid receptors, facilitating precise dissection of opioid receptor subtypes in neuronal and non-neuronal systems. By serving as a reference agonist, DAMGO supports the development of receptor binding assays, competitive ligand studies, and functional analyses of receptor mutants or engineered constructs.
Signal Transduction Studies: In cellular and molecular neuroscience, DAMGO is widely used to investigate the intracellular signaling cascades triggered by MOR activation. Upon binding, it induces canonical G protein-coupled receptor (GPCR) signaling events, such as inhibition of adenylate cyclase, modulation of ion channel activity, and activation of MAP kinase pathways. These properties make DAMGO an indispensable tool for elucidating the molecular mechanisms underlying opioid-induced signal transduction, receptor desensitization, and regulatory feedback processes.
Electrophysiological Applications: The selective activation of mu-opioid receptors by DAMGO is critical in electrophysiological experiments aimed at understanding synaptic transmission and neuronal excitability. By applying DAMGO to brain slices, cultured neurons, or heterologous expression systems, investigators can assess its effects on membrane potential, synaptic currents, and neuronal firing rates. These studies contribute to a deeper understanding of opioid modulation in pain pathways, reward circuits, and other neurophysiological processes.
Neurobehavioral Research: DAMGO is frequently utilized in preclinical behavioral assays to model the effects of mu-opioid receptor activation on nociception, reward, motivation, and learning. Its robust and reproducible pharmacological profile allows researchers to delineate the specific contributions of MOR signaling to behavioral outcomes in rodent and other animal models. Such applications are instrumental in advancing knowledge of opioid receptor function and the neurobiological basis of pain and addiction.
Peptide Structure-Activity Relationship (SAR) Analysis: As a synthetic peptide with defined modifications, DAMGO serves as a reference compound in structure-activity relationship studies of opioid peptides. Researchers use it to compare the effects of amino acid substitutions, backbone alterations, and chemical modifications on MOR binding and activation. These SAR investigations inform the rational design of novel peptide ligands with tailored pharmacological properties, supporting drug discovery efforts and fundamental research into opioid receptor biology.
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