Title of article :
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/Authors :
Dehua Huang، نويسنده , , Steve F. Poon، نويسنده , , Deborah F. Chapman، نويسنده , , Janice Chung، نويسنده , , Merryl Cramer، نويسنده , , Thomas S. Reger، نويسنده , , Jeffrey R. Roppe، نويسنده , , Lida Tehrani، نويسنده , , Nicholas D.P Cosford، نويسنده , , NICHOLAS D. SMITH & ANDREW C. YIP، نويسنده ,
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.
Keywords :
e-mail: nicholas_smith@merck.com , Metabotropic glutamate , Tetrazole.* Corresponding author. Tel.: +1 858 202 5248 , Antagonist , fax: +1 858 2025743
