Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure–activity relationships and assessment in a rat model of nicotine …

…, R Dahl, A Mangravita-Novo, LH Smith…

Index: Sidique, Shyama; Dhanya, Raveendra-Panickar; Sheffler, Douglas J.; Nickols, Hilary Highfield; Yang, Li; Dahl, Russell; Mangravita-Novo, Arianna; Smith, Layton H.; D'Souza, Manoranjan S.; Semenova, Svetlana; Conn, P. Jeffrey; Markou, Athina; Cosford, Nicholas D.P. Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 9434 - 9445

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Citation Number: 15

Abstract

Compounds that modulate metabotropic glutamate subtype 2 (mGlu2) receptors have the potential to treat several disorders of the central nervous system (CNS) including drug dependence. Herein we describe the synthesis and structure–activity relationship (SAR) studies around a series of mGlu2 receptor positive allosteric modulators (PAMs). The effects of N-substitution (R1) and substitutions on the aryl ring (R2) were identified as key areas ...