A 1-methyl-4-piperidinyl cytectrene carboxylate labeled by the technetium 99m, a radiotracer for rat brain acetylcholinesterase activity.
Alzheimer's disease (AD) is a degenerative neurological disorder that causes progressive and irreversible loss of connections between brain cells and loss of mental functions. Clinical and postmortem studies show that the biochemical changes in brains of AD patients include decrease in acetylcholinesterase (AChE) activity. Our aim was to study AChE activity using piperidinyl ester labelled with technetium-99m. In vivo and in vitro studies demonstrated that labelled piperidinyl ester was a substrate for AChE. The hydrolytic rate of this substrate was measured and the specificity was evaluated using the inhibitor BW284c51. The rhenium analogues of the technetium-labelled substrate were used to determine the affinity constant (K(m)) and the maximum reaction velocity (V(max)) because of the high specific activity of technetium. The high hydrolytic rate and high specificity of the substrate for AChE make it suitable as an in vivo radiotracer for studying AChE activity in the brain.
Radiopharmaceutical Unit, National Centre of Sciences and Nuclear Technologies, Sidi Thabet 2020, Tunisia. najoua.mejri@gmail.com
Najoua
N
Mejri
Chokri
C
Barhoumi
Moez
M
Trabelsi
Abdelkader
A
Mekni
Nadia Malek
NM
Said
Mouldi
M
Saidi
D000110:Acetylcholinesterase / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000166:cytology / Q000201:enzymology*; D006868:Hydrolysis; D007700:Kinetics; D008297:Male; D015609:Organotechnetium Compounds / Q000737:chemistry* / Q000378:metabolism*; D011849:Radioactive Tracers; D051381:Rats; D017208:Rats, Wistar; D012211:Rhenium / Q000737:chemistry / Q000378:metabolism; D013379:Substrate Specificity; D013667:Technetium / Q000737:chemistry*
D015609:Organotechnetium Compounds; D011849:Radioactive Tracers; C549478:technetium 99m 1-methyl-4-piperidinyl cytectrene carboxylate; D012211:Rhenium; D013667:Technetium; D000110:Acetylcholinesterase