Tricyclic thienopyridine–pyrimidones/thienopyrimidine–pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain
Copyright policy )Tricyclic thienopyridine–pyrimidones/thienopyrimidine–pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain
Introduction of small unsaturated alkylamino groups at the 4-position of the A-ring of the tricyclic framework (triazafluorenone) afforded extremely potent and selective mGluR1 antagonists with desirable properties. Compounds 11q and 11s are active in the SNL pain model with ED(50)s 3.3 and 6.4 mg/kg respectively. Metabolic outcome of propargyl amino moiety was studied.
- Schering-Plough United States
- University of Eastern Piedmont Amadeo Avogadro Italy
neuropathic pain, Dose-Response Relationship, Drug, Pyridines, Administration, Oral, antagonist, tricyclic, Receptors, Metabotropic Glutamate, Rats, Inhibitory Concentration 50, Structure-Activity Relationship, Pyrimidines, Animals, Humans, Neuralgia, mGluR1, chronic pain, Heterocyclic Compounds, 3-Ring
neuropathic pain, Dose-Response Relationship, Drug, Pyridines, Administration, Oral, antagonist, tricyclic, Receptors, Metabotropic Glutamate, Rats, Inhibitory Concentration 50, Structure-Activity Relationship, Pyrimidines, Animals, Humans, Neuralgia, mGluR1, chronic pain, Heterocyclic Compounds, 3-Ring
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