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Discovery of 1,5-disubstituted pyridones: a new class of positive allosteric modulators of the metabotropic glutamate 2 receptor.
- Source :
-
ACS chemical neuroscience [ACS Chem Neurosci] 2010 Dec 15; Vol. 1 (12), pp. 788-95. Date of Electronic Publication: 2010 Aug 23. - Publication Year :
- 2010
-
Abstract
- A series of 1,5-disubstituted pyridones was identified as positive allosteric modulators (PAMs) of the metabotropic glutamate receptor 2 (mGluR2) via high throughput screening (HTS). Subsequent SAR exploration led to the identification of several compounds with improved in vitro activity. Lead compound 8 was further profiled and found to attenuate the increase in PCP induced locomotor activity in mice.
- Subjects :
- Allosteric Regulation
Amino Acids chemistry
Animals
Bridged Bicyclo Compounds chemistry
Drug Evaluation, Preclinical
Drug Stability
Excitatory Amino Acid Agonists chemistry
Excitatory Amino Acid Agonists classification
Humans
Hydrophobic and Hydrophilic Interactions
Mice
Molecular Structure
Motor Activity drug effects
Pyridines chemistry
Pyridones chemistry
Pyridones classification
Pyridones isolation & purification
Recombinant Proteins drug effects
Structure-Activity Relationship
Sulfonamides chemistry
Amino Acids pharmacology
Bridged Bicyclo Compounds pharmacology
Excitatory Amino Acid Agonists pharmacology
Pyridines pharmacology
Pyridones pharmacology
Receptors, Metabotropic Glutamate agonists
Sulfonamides pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1948-7193
- Volume :
- 1
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- ACS chemical neuroscience
- Publication Type :
- Academic Journal
- Accession number :
- 22778815
- Full Text :
- https://doi.org/10.1021/cn1000638