Ontology highlight
ABSTRACT:
SUBMITTER: Harland AA
PROVIDER: S-EPMC4885601 | biostudies-literature | 2016 May
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20160516 10
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 ...[more]