The identification of novel orally active mGluR5 antagonist GSK2210875

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 24, 2010, Pages 7521-7524

  Pilla, Maria ^b   Andreoli, Michela ^b   Tessari, Michela ^b   Delle Fratte, Sonia ^b   Roth, Adelheid ^b   Butler, Sharon ^c   Brown, Fiona ^c   Shah, Parita ^c   Bettini, Ezio ^b   Cavallini, Palmina ^b   Benedetti, Roberto ^b   Minick, Doug ^c   Smith, Paul ^a   Tehan, Ben ^a   D'Alessandro, Pier ^a   Lorthioir, Olivier ^a   Ball, Catherine ^a   Garzya, Vincenzo ^a   Goodacre, Caroline ^a   Watson, Stephen ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

^b Medicines Research Centre   (Italy)

^c Molecular Discovery Research   (United Kingdom)

Author keywords

Allosteric modulator; Brain free fraction; Family C GPCR; GPCR; Metabotropic glutamate receptor; mGluR; mGluR5; Negative allosteric modulator

Indexed keywords

GSK 2210875; METABOTROPIC RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG;

ARTICLE; DRUG POTENCY; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HIGH THROUGHPUT SCREENING; HUMAN; IN VITRO STUDY; IN VIVO STUDY; NEOPHOBIA; NONHUMAN; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ALLOSTERIC REGULATION; ANIMALS; BRAIN; HETEROCYCLIC COMPOUNDS, 3-RING; MICE; RATS; RECEPTORS, METABOTROPIC GLUTAMATE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 78449269999     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.09.120     Document Type: Article

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