2-styryl-pyridines and 2-(3,4-dihydro-naphthalen-2-yl)-pyridines as potent NR1/2B subtype selective NMDA receptor antagonists

A series of 2-styryl-pyridines and 2-(3,4-dihydro-naphthalen-2-yl)-pyridines was prepared and evaluated as NR1/2B subtype selective NMDA receptor antagonists. The SAR developed in this series resulted in the discovery of high affinity antagonists that are selective (vs. alpha(1) and M-1 receptors) and are active in vivo.