Discovery of 1,5-disubstituted pyridones: A new class of positive allosteric modulators of the metabotropic glutamate 2 receptor

ACS Chemical Neuroscience

Volumn 1, Issue 12, 2010, Pages 788-795

  Cid, Jose María ^a,d   Duvey, Guillaume ^b   Cluzeau, Philippe ^b   Nhem, Vanthea ^b   MacAry, Karim ^b   Raux, Alexandre ^b   Poirier, Nicolas ^b   Muller, Jessica ^b   Boléa, Christelle ^b   Finn, Terry ^b   Poli, Sonia ^b   Epping Jordan, Mark ^b   Chamelot, Emilie ^b   Derouet, Francis ^b   Girard, Francoise ^b   MacDonald, Gregor J ^c   Vega, Juan Antonio ^a   De Lucas, Ana Isabel ^a   Matesanz, Encarnación ^a   Lavreysen, Hilde ^c   Linares, María Lourdes ^a   Oehlrich, Daniel ^a   Oyarzábal, Julen ^a   Tresadern, Gary ^a   Trabanco, Andrés A ^a   Andrés, Jose Ignacio ^a   Le Poul, Emmanuel ^b   Imogai, Hassan ^b   Lutjens, Robert ^b   Rocher, Jean Philippe ^b   more..

^a JOHNSON AND JOHNSON   (United States)

^b ADDEX PHARMACEUTICALS   (Switzerland)

^c JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

^d Structural Biology and Biocomputing Programme   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

1,5 PYRIDONE DERIVATIVE; 4 [2 AMINO 4 (METHYLTHIO)BUTYRYLAMINO] 2 THIABICYCLO[3.1.0]HEXANE 4,6 DICARBOXYLIC ACID 2,2 DIOXIDE; EGLUMETAD; LY 487379; METABOTROPIC RECEPTOR 2; PHENCYCLIDINE; PYRIDONE DERIVATIVE; UNCLASSIFIED DRUG;

ALLOSTERISM; ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; LOCOMOTION; MOUSE; NONHUMAN; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION;

MUS;

EID: 78650315615     PISSN: None     EISSN: 19487193     Source Type: Journal    
DOI: 10.1021/cn1000638     Document Type: Article

References (20)

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20. Details of the protocol for the in vivo assay: Phencyclidine (PCP)-induced hyperlocomotion in mice Male C57BL6/j mice (Charles River, France) were housed 5 per cage and kept under a 12-h light/dark cycle under constant temperature and humidity conditions. All experimental procedures were performed in full compliance with the French and European legislation governing the protection of vertebrate animals used in scientific research. Tested mGluR2 PAM compounds, (cpd 8, LY487379) were synthesized in house, and phencyclidine (PCP) was purchased from Sigma-Aldrich (France). Nonhabituated animals were treated with the vehicle, or 200 mg/kg ip of either cpd 8 or LY487379, and immediately challenged with either PCP (5.0 mg/kg, ip) or vehicle and individually placed into open-fields for a 30-min period. The distance traveled by animals was measured using video tracking and computerized analysis systems (Viewpoint, France) and the data analyzed using GraphPad Prism (v. 4.01, GraphPad, San Diego, CA, USA).