Abstract
A new derivative of 4,5,9,10-tetrahydro-1,4-ethanobenz[ b]quinolizine ( 2) has been designed as a prodrug for its quinolizinium cation ( 1) that is a potent antagonist of the TCP-binding site of NMDA receptors at the open state. The 11C-labeled 2 showed high accumulation of radioactivity in the brain in an in vivo biodistribution study. The speculation of 2 as a prodrug of 1 has been proven by the fact that 1 was observed in a high ratio to 2 in an analysis by RP-HPLC of the brain homogenates.
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