| Title : Synthesis and biological evaluation of 1-(4-[18F]fluorobenzyl)-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine for in vivo studies of acetylcholinesterase - Lee_2000_Nucl.Med.Biol_27_741 |
| Author(s) : Lee SY , Choe YS , Sugimoto H , Kim SE , Hwang SH , Lee K , Choi Y , Lee J , Kim B |
| Ref : Nucl Med Biol , 27 :741 , 2000 |
|
Abstract :
We synthesized and evaluated 1-(4-fluorobenzyl)-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine (4-FDP), which is an analog of donepezil. The 4-[(18)F]FDP was prepared by reductive alkylation of debenzylated donepezil with 4-[(18)F]fluorobenzaldehyde in high radiochemical yield (decay-corrected, 40-52%) and with high effective specific activity (30-38 GBq/micromol). Tissue distribution studies in mice demonstrated nonspecific distribution of the 4-[(18)F]FDP in brain regions, suggesting that this radioligand may not be a suitable agent for in vivo studies of acetylcholinesterase (AChE), despite its potent in vitro biological activity. |
| PubMedSearch : Lee_2000_Nucl.Med.Biol_27_741 |
| PubMedID: 11150705 |
Lee SY, Choe YS, Sugimoto H, Kim SE, Hwang SH, Lee K, Choi Y, Lee J, Kim B (2000)
Synthesis and biological evaluation of 1-(4-[18F]fluorobenzyl)-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine for in vivo studies of acetylcholinesterase
Nucl Med Biol
27 :741
Lee SY, Choe YS, Sugimoto H, Kim SE, Hwang SH, Lee K, Choi Y, Lee J, Kim B (2000)
Nucl Med Biol
27 :741