Discovery of (-)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone--a potent NR2B-selective N-methyl D-aspartate (NMDA) antagonist for the treatment of pain.

doi:10.1016/J.BMCL.2007.08.014

Paper

Discovery of (-)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone--a potent NR2B-selective N-methyl D-aspartate (NMDA) antagonist for the treatment of pain.

Published Oct 15, 2007 · M. Kawai, K. Ando, Yuka Matsumoto

Bioorganic & medicinal chemistry letters

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13

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Abstract

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Study Snapshot

(-)-6-[2-(4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl)-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone) shows potential as an oral NMDA antagonist for pain treatment

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Discovery of (-)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone--a potent NR2B-selective N-methyl D-aspartate (NMDA) antagonist for the treatment of pain.

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References

Citations

Phenol (bio)isosteres in drug design and development

Phenol bioisosteres can enhance drug stability, receptor selectivity, and therapeutic efficacy while addressing challenges like potency and side effects.

GluN2A and GluN2B N-Methyl-D-Aspartate Receptor (NMDARs) Subunits: Their Roles and Therapeutic Antagonists in Neurological Diseases

GluN2A and GluN2B NMDAR subunits play crucial roles in cognitive processes and neurodegenerative diseases like Parkinson's and Alzheimer's, and targeting these subunits could lead to neuroprotective drugs with optimal therapeutic profiles.

Phase 1 Clinical Results for NP10679, a pH‐sensitive GluN2B‐selective N‐methyl‐d‐aspartate Receptor Inhibitor

NP10679 is a well-tolerated, pH-sensitive NMDA receptor inhibitor that selectively targets ischemic tissue while minimizing nonselective blockade in healthy brain, with potential applications in acute brain injury and neuropsychiatric indications.

A comprehensive description of GluN2B-selective N-methyl-D-aspartate (NMDA) receptor antagonists.

GluN2B-selective NMDA antagonists show potential as effective treatments for various CNS diseases, with two main categories: prototypical and atypical antagonists.

A cascade C-H functionalization/cyclization reaction of N-arylpyridin-2-amines with α,β-unsaturated aldehydes for the synthesis of dihydroquinolinone derivatives under rhodium catalysis.

This novel cascade C-H functionalization/cyclization reaction under rhodium catalysis allows for the synthesis of dihydroquinolinone derivatives in moderate to excellent yields.