A focused chemical optimization effort of compound 1 based on metabolite elucidation is described, resulting in 15i, a highly potent and selective mGlu5 receptor antagonist with an improved pharmacokinetic profile compared to 1. Characterization of 15i in vivo in the fear-potentiated startle (FPS) paradigm revealed a robust reduction of conditioned fear behavior. This effect nicely correlates with the rat brain pharmacokinetics.
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|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4018045 | PMC |
| http://dx.doi.org/10.1021/ml100215b | DOI Listing |
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