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  • Title: 2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.
    Author: Huang D, Poon SF, Chapman DF, Chung J, Cramer M, Reger TS, Roppe JR, Tehrani L, Cosford ND, Smith ND.
    Journal: Bioorg Med Chem Lett; 2004 Nov 15; 14(22):5473-6. PubMed ID: 15482906.
    Abstract:
    Structure-activity relationship studies on 3-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile 2 led to the discovery of 2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl)pyridine (10)-a highly potent and selective mGlu5 receptor antagonist with good brain penetration and in vivo receptor occupancy in rat and cross-species oral bioavailability.
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