Discovery of Novel Triazole-Based Opioid Receptor Antagonists
- 21 June 2006
- journal article
- letter
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 49 (14), 4044-4047
- https://doi.org/10.1021/jm0601250
Abstract
We report the computer-aided design, chemical synthesis, and biological evaluation of a novel family of δ opioid receptor (DOR) antagonists containing a 1,2,4-triazole core structure that are structurally distinct from other known opioid receptor active ligands. Among those δ antagonists sharing this core structure, 8 exhibited strong binding affinity (Ki = 50 nM) for the DOR and appreciable selectivity for δ over μ and κ opioid receptors (δ/μ = 80; δ/κ > 200).Keywords
This publication has 34 references indexed in Scilit:
- Enrichment of Ligands for the Serotonin Receptor Using the Shape Signatures ApproachJournal of Chemical Information and Modeling, 2004
- Identification of Opioid Ligands Possessing Mixed μ Agonist/δ Antagonist Activity among Pyridomorphinans Derived from Naloxone, Oxymorphone, and HydropmorphoneJournal of Medicinal Chemistry, 2004
- The δ-Opioid Receptor Agonist (+)BW373U86 Regulates BDNF mRNA Expression in RatsNeuropsychopharmacology, 2003
- Shape Signatures: A New Approach to Computer-Aided Ligand- and Receptor-Based Drug DesignJournal of Medicinal Chemistry, 2003
- Retention of Supraspinal Delta-like Analgesia and Loss of Morphine Tolerance in δ Opioid Receptor Knockout MiceNeuron, 1999
- Naltrindole, an opioid delta receptor antagonist, blocks cocaine-induced facilitation of responding for rewarding brain stimulationLife Sciences, 1993
- Design of peptidomimetic .delta. opioid receptor antagonists using the message-address conceptJournal of Medicinal Chemistry, 1990
- Bivalent ligands and the message-address concept in the design of selective opioid receptor antagonistsTrends in Pharmacological Sciences, 1989
- Mannich reactions of heterocycles with dimethyl(methylene) ammonium chloride: A high yield, one‐step conversion of estazolam to adinazolamJournal of Heterocyclic Chemistry, 1988
- Genetic Mechanisms Determining the Central Visual Pathways of MiceScience, 1973