| Abstract |
A series of fused tricyclic mGluR1 antagonists containing a pyridone ring were synthesized. In vitro, these antagonists were potent against both human and rat isozymes, as well as selective for inhibiting mGluR1 over mGluR5. When dosed orally, several examples were active in vivo in a rat SNL test. |
| Authors | Chad E Bennett, Duane A Burnett, William J Greenlee, Chad E Knutson, Peter Korakas, Cheng Li, Deen Tulshian, Wen-Lian Wu, Rosalia Bertorelli, Silva Fredduzzi, Mariagrazia Grilli, Gianluca Lozza, Angelo Reggiani, Alessio Veltri |
| Journal | Bioorganic & medicinal chemistry letters
(Bioorg Med Chem Lett)
Vol. 22
Issue 4
Pg. 1575-8
(Feb 15 2012)
ISSN: 1464-3405 [Electronic] England |
| PMID | 22266036
(Publication Type: Journal Article)
|
| Copyright | Copyright © 2012 Elsevier Ltd. All rights reserved. |
| Chemical References |
- Analgesics
- Pyridones
- Receptors, Metabotropic Glutamate
- metabotropic glutamate receptor type 1
|
| Topics |
- Administration, Oral
- Analgesics
(pharmacology)
- Animals
- Cells, Cultured
- Cyclization
- Humans
- Inhibitory Concentration 50
- Molecular Structure
- Neuralgia
(drug therapy)
- Protein Binding
(drug effects)
- Pyridones
(chemical synthesis, chemistry, pharmacology)
- Rats
- Receptors, Metabotropic Glutamate
(antagonists & inhibitors)
|
