A Prodrug of NMDA/Glycine Site Antagonist, L-703,717, with Improved BBB Permeability. 4-Acetoxy Derivative and Its Positron-Emitter Labeled Analog.

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4-Acetoxy derivative (1) of L-703, 717, a high-affinity (IC50=4.5 nM) antagonist for the glycine site of NMDA receptors, was synthesized and its brain uptake was examined using a carbon-11 labeled analog ([11C]1). Initial radioactivity in the brain after intravenous injection of [11C]1 was a 2-fold that of [11C]L-703, 717 in mice. Rapid bioconversion of [11C]1 into [11C]L-703, 717 was demonstrated by metabolite analyses of rat brain after [11C]1 injection. Ex vivo autoradiography of [11C]1 in rat brain showed the same cerebellar localization of radioactivity as [11C]L-703, 717. These results indicate that 1 is a promising pharmacological tool as a prodrug of L-703, 717 with improved BBB permeability.

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