{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Harland AA"],"funding":["NIDA NIH HHS","National Institute on Drug Abuse","NIGMS NIH HHS"],"pagination":["4985-98"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC4885601"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["59(10)"],"pubmed_abstract":["N-Acetylation of the tetrahydroquinoline (THQ) core of a series of μ-opioid receptor (MOR) agonist/δ-opioid receptor (DOR) antagonist ligands increases DOR affinity, resulting in ligands with balanced MOR and DOR affinities. We report a series of N-substituted THQ analogues that incorporate various carbonyl-containing moieties to maintain DOR affinity and define the steric and electronic requirements of the binding pocket across the opioid receptors. 4h produced in vivo antinociception (ip) for 1 h at 10 mg/kg."],"journal":["Journal of medicinal chemistry"],"pubmed_title":["Effects of N-Substitutions on the Tetrahydroquinoline (THQ) Core of Mixed-Efficacy μ-Opioid Receptor (MOR)/δ-Opioid Receptor (DOR) Ligands."],"pmcid":["PMC4885601"],"funding_grant_id":["R01 DA003910","DA003910","T32 DA007268","T32 DA007267","T32 GM007767"],"pubmed_authors":["Traynor JR","Harland AA","Pogozheva ID","Mosberg HI","Bender AM","Griggs NW","Anand JP","Jutkiewicz EM","Gao C"],"additional_accession":[]},"is_claimable":false,"name":"Effects of N-Substitutions on the Tetrahydroquinoline (THQ) Core of Mixed-Efficacy μ-Opioid Receptor (MOR)/δ-Opioid Receptor (DOR) Ligands.","description":"N-Acetylation of the tetrahydroquinoline (THQ) core of a series of μ-opioid receptor (MOR) agonist/δ-opioid receptor (DOR) antagonist ligands increases DOR affinity, resulting in ligands with balanced MOR and DOR affinities. We report a series of N-substituted THQ analogues that incorporate various carbonyl-containing moieties to maintain DOR affinity and define the steric and electronic requirements of the binding pocket across the opioid receptors. 4h produced in vivo antinociception (ip) for 1 h at 10 mg/kg.","dates":{"release":"2016-01-01T00:00:00Z","publication":"2016 May","modification":"2024-11-13T13:25:50.809Z","creation":"2019-03-27T02:14:47Z"},"accession":"S-EPMC4885601","cross_references":{"pubmed":["27148755"],"doi":["10.1021/acs.jmedchem.6b00308"]}}