Article Document Academic Article Information Content Entity Continuant Continuant Journal Article Entity Entity Generically Dependent Continuant 2025-05-11T07:10:27 RDF description of Inhibition of ligand binding to G protein-coupled receptors by arachidonic acid - http://repository.healthpartners.com/individual/document-rn18671 Parasympatholytics/chemistry/metabolism 21588 13504 Receptors, Muscarinic/*metabolism Ligands Quinuclidinyl Benzilate/chemistry/metabolism 2022-02-21T22:48:57.408-06:00 Receptors, G-Protein-Coupled/*metabolism Protein Binding Animals 10.1385/jmn:27:2:185 Journal of Molecular Neuroscience Dihydroalprenolol/chemistry/metabolism Inhibition of ligand binding to G protein-coupled receptors by arachidonic acid Diprenorphine/chemistry/metabolism Radioligand Assay document-rn18671 Narcotic Antagonists/chemistry/metabolism 2 N-Methylscopolamine/chemistry/metabolism <p>Arachidonic acid (AA), released in response to muscarinic acetylcholine receptor (mAChR) stimulation, previously has been reported to function as a reversible feedback inhibitor of the mAChR. To determine if the effects of AA on binding to the mAChR are subtype specific and whether AA inhibits ligand binding to other G protein-coupled receptors (GPCRs), the effects of AA on ligand binding to the mAChR subtypes (M1, M2, M3, M4, and M5) and to the micro-opioid receptor, beta2-adrenergic receptor (beta2-AR), 5-hydroxytryptamine receptor (5-HTR), and nicotinic receptors were examined. AA was found to inhibit ligand binding to all mAChR subtypes, to the beta2-AR, the 5-HTR, and to the micro-opioid receptor. However, AA does not inhibit ligand binding to the nicotinic receptor, even at high concentrations of AA. Thus, AA inhibits several types of GPCRs, with 50% inhibition occurring at 3-25 MuM, whereas the nicotinic receptor, a non-GPCR, remains unaffected. Further research is needed to determine the mechanism by which AA inhibits GPCR function.<p> public Muscarinic Antagonists/chemistry/metabolism Receptors, Opioid, mu/*metabolism Serotonin/chemistry/metabolism Arachidonic Acid/chemistry/*metabolism Receptors, Adrenergic, beta-2/*metabolism Molecular Structure Receptors, Serotonin/*metabolism 27 Protein Isoforms/metabolism Adrenergic beta-Antagonists/chemistry/metabolism