Literature DB >> 11150706

Pharmacological evaluation of [11C]donepezil as a tracer for visualization of acetylcholinesterase by PET.

F De Vos 1, P Santens, H Vermeirsch, I Dewolf, F Dumont, G Slegers, R A Dierckx.   

Abstract

Donepezil is a highly potent and selective reversible achetylcholinesterase inhibitor. [(11)C]Donepezil is prepared by methylation with [(11)C]CH(3)I of the corresponding 6'-O-desmethylprecursor. Tissue distribution in mice revealed a high uptake in brain and rapid clearance from the blood. Metabolization studies in mice indicated the formation of one (11)C-labeled polar metabolite that didn't penetrate the blood-brain barrier. Regional brain distribution in rabbits didn't reflect the measured achetylcholinesterase distribution in rabbit brain.

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Year:  2000        PMID： 11150706     DOI： 10.1016/s0969-8051(00)00166-9

Source DB:  PubMed          Journal:  Nucl Med Biol        ISSN： 0969-8051            Impact factor:   2.408


  5 in total

1.  PET radiopharmaceuticals for probing enzymes in the brain.

Authors:  Jason P Holland; Paul Cumming; Neil Vasdev
Journal:  Am J Nucl Med Mol Imaging       Date:  2013-04-09

2.  In vivo visualization of donepezil binding in the brain of patients with Alzheimer's disease.

Authors:  Nobuyuki Okamura; Yoshihito Funaki; Manabu Tashiro; Motohisa Kato; Yoichi Ishikawa; Masahiro Maruyama; Hiroyasu Ishikawa; Kenichi Meguro; Ren Iwata; Kazuhiko Yanai
Journal:  Br J Clin Pharmacol       Date:  2007-12-07       Impact factor: 4.335

Review 3.  Acetylcholine esterase activity in mild cognitive impairment and Alzheimer's disease.

Authors:  Karl Herholz
Journal:  Eur J Nucl Med Mol Imaging       Date:  2008-03       Impact factor: 9.236

4.  2,3-dihydro-1H-cyclopenta[b]quinoline derivatives as acetylcholinesterase inhibitors-synthesis, radiolabeling and biodistribution.

Authors:  Paweł Szymański; Alice Lázničková; Milan Lázniček; Marek Bajda; Barbara Malawska; Magdalena Markowicz; Elżbieta Mikiciuk-Olasik
Journal:  Int J Mol Sci       Date:  2012-08-13       Impact factor: 6.208

5.  Distribution of intravenously administered acetylcholinesterase inhibitor and acetylcholinesterase activity in the adrenal gland: 11C-donepezil PET study in the normal rat.

Authors:  Tadashi Watabe; Sadahiro Naka; Hayato Ikeda; Genki Horitsugi; Yasukazu Kanai; Kayako Isohashi; Mana Ishibashi; Hiroki Kato; Eku Shimosegawa; Hiroshi Watabe; Jun Hatazawa
Journal:  PLoS One       Date:  2014-09-16       Impact factor: 3.240
  5 in total

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