Effects of N-Substitutions on the Tetrahydroquinoline (THQ) Core of Mixed-Efficacy μ-Opioid Receptor (MOR)/δ-Opioid Receptor (DOR) Ligands | Zendy

Aubrie A. Harland | Zendy; Aaron M. Bender | Zendy; Nicholas W. Griggs | Zendy; Chao Gao | Zendy; Jessica P. Anand | Zendy; Irina D. Pogozheva | Zendy; John R. Traynor | Zendy; Emily M. Jutkiewicz | Zendy; Henry I. Mosberg | Zendy

Open Access

Effects of N-Substitutions on the Tetrahydroquinoline (THQ) Core of Mixed-Efficacy μ-Opioid Receptor (MOR)/δ-Opioid Receptor (DOR) Ligands

Author(s) -

Aubrie A. Harland,

Aaron M. Bender,

Nicholas W. Griggs,

Chao Gao,

Jessica P. Anand,

Irina D. Pogozheva,

John R. Traynor,

Emily M. Jutkiewicz,

Henry I. Mosberg

Publication year - 2016

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/acs.jmedchem.6b00308

Subject(s) - chemistry , opioid receptor , steric effects , opioid , stereochemistry , receptor , agonist , antagonist , affinities , ligand (biochemistry) , pharmacology , biochemistry , medicine

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.

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