Metabotropic glutamate 2/3 receptors (mGlu2/3R) are class C G-protein coupled receptors that are highly expressed in the central nervous system and modulate neuronal excitability. Negative modulation of the mGlu2/3R receptors has demonstrated an anti-depressant profile and wake-promoting signature in preclinical animal models, thus making these receptors attractive therapeutic targets. This communication will discuss the synthesis and medicinal chemistry optimization of the bicyclo[3.1.0]hexane glutamic acid scaffold to produce selective orthosteric mGluR 2/3 antagonists, such as compound 1. 

Discovery, synthesis, and characterization of a potent antagonist of the metabotropic glutamate 2/3 receptors possessing anti-depressant and wake-promoting properties

248th National Meeting (2014)

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