Title of article :
4,5,9,10-Tetrahydro-1,4-ethanobenz[b]quinolizine as a prodrug for its quinolizinium cation as a ligand to the open state of the TCP-binding site of NMDA receptors
Author/Authors :
Shigeki Sasaki، نويسنده , , Takahiro Kanda، نويسنده , , Nobuyasu Ishibashi، نويسنده , , Fumihiko Yamamoto، نويسنده , , Terushi Haradahira، نويسنده , , Takashi Okauchi، نويسنده , , Jun Meda، نويسنده , , Kazutoshi Suzuki، نويسنده , , Minoru Maeda، نويسنده ,
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.
