Synthesis, physicochemical and biological studies of technetium-99m labeled tacrine derivative as a diagnostic tool for evaluation of cholinesterase level

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• 作者：Ewa Gniazdowska^a ; Przemysław Koźmiński^a ; ^{p.kozminski@ichtj.waw.pl} ; Marek Wasek^b ; Marek Bajda^c ; Joanna Sikora^d ; Elżbieta Mikiciuk-Olasik^e ; Paweł Szymański^f ; ^{pawel.szymanski@umed.lodz.pl}
• 关键词：Tac ; tacrine (1 ; 2 ; 3 ; 4-tetrahydroacridin-9-amine) ; AD ; Alzheimer&rsquo ; s disease ; AChE ; acetylcholinesterase ; CNS ; central nervous system ; IC50 ; half maximal inhibitory concentration ; BM ; biologically active molecule ; BFCA ; Bifunctional Coupling Agent ; NS3 ; tris(2-mercaptoethyl)-amine ; CN-BFCA ; isocyanobutyric acid succinimidyl ester ; n.c.a. ; no carrier added ; HPLC ; high-performance liquid chromatography ; RT ; retention time ; PBS ; phosphate buffered saline ; TFA ; trifluoroacetic acid ; RCP ; radioche
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：1 February 2017
• 年：2017
• 卷：25
• 期：3
• 页码：912-920
• 全文大小：880 K
• 卷排序：25

文摘

Labeling procedure of tacrine derivatives with technetium-99m. Determination of physicochemical properties of the conjugates. In vitro and in vivo studies of biological properties of the conjugates. 99mTc-tacrine derivative conjugates as diagnostic tool for cholinesterase level evaluation.