MDL-29951

MDL-29951 is a novel glycine antagonist of NMDA receptor activation (Ki=0.14 mM, [3H]glycine binding) in vitro and in vivo with IC50 value of 0.14 mM ([3H]glycine binding).MDL-29951 completely inhibited the use-dependent binding of [3H]N-[1-(2-thienyl) cyclohexyl]-piperidine and was noncompetitive, glycine-reversible inhibitor of both NMDA-induced biochemical and electrophysiological responses in brain slice preparations. MDL-29,951 were nearly 2000-fold selective for the glycine binding site relative to the glutamate recognition sites.