title: Preliminary studies of acetylcholinesterase activity in the rat brain using N-phenylferrocenecarboxamide labelled by the technetium-99m.
abstract: There is currently great interest in developing radiolabeled substrates for acetylcholinesterase that would be useful in the in vivo imaging of patients with Alzheimer's disease. The reduction of acetylcholinesterase (AChE) activity in the brain has been measured in dementia disorders such as Alzheimer's disease and dementia with Lewy bodies using (11)C and (18)F-labeled acetylcholine analogues. Our aim was to develop a new 99mTc-labeled acetylcholine analogue: N-phenylferrocenecarboxamide labelled with technetium-99m (99mTc-TPCC) to study acetylcholinesterase activity. In vivo and in vitro studies demonstrated that the labelled compound was a substrate for acetylcholinesterase. The hydrolytic rate of this substrate was measured and the specificity was evaluated using the inhibitor BW 284 C51. In rat experiments, the 99mTc-TPCC showed desirable properties for studying the acetylcholinesterase in the rat brain: high hydrolytic rate and a moderate specificity of the substrate for acetylcholinesterase.
authors: Research Unit of Medical, Agricultural and Environmental Use of Nuclear Applications (CNSTN) Tunisia. najoua.mejri@gmail.com
authors: Najoua
authors: N
authors: Mejri
authors: Nadia Malek
authors: NM
authors: Said
authors: Sihem
authors: S
authors: Guizani
authors: Imen
authors: I
authors: Essouissi
authors: Mouldi
authors: M
authors: Saidi
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism*; D000818:Animals; D002093:Benzenaminium, 4,4'-(3-oxo-1,5-pentanediyl)bis(N,N-dimethyl-N-2-propenyl-), Dibromide / Q000378:metabolism; D001921:Brain / Q000201:enzymology* / Q000378:metabolism; D005296:Ferrous Compounds / Q000097:blood / Q000737:chemistry / Q000378:metabolism; D005978:Glutathione / Q000378:metabolism; D006868:Hydrolysis; D007553:Isotope Labeling; D008297:Male; D000075163:Metallocenes; D057054:Molecular Imaging; D015609:Organotechnetium Compounds / Q000097:blood / Q000737:chemistry / Q000378:metabolism; D011849:Radioactive Tracers; D011854:Radiochemistry; D051381:Rats; D017208:Rats, Wistar; D013667:Technetium
chemical_list: D005296:Ferrous Compounds; D000075163:Metallocenes; D015609:Organotechnetium Compounds; D011849:Radioactive Tracers; C584532:tricarbonyl(N-phenylcyclopentadienylcarboxamide)technetium(I); D002093:Benzenaminium, 4,4'-(3-oxo-1,5-pentanediyl)bis(N,N-dimethyl-N-2-propenyl-), Dibromide; D013667:Technetium; D000110:Acetylcholinesterase; D005978:Glutathione; C004998:ferrocene