Synthesis and biological evaluation of 99mTc, Re-monoamine-monoamide conjugated to 2-(4-aminophenyl)benzothiazole as potential probes for beta-amyloid plaques in the brain.
The benzothiazole aniline (BTA) conjugated with monoamine-monoamide (MAMA) was synthesized and then labeled with (99m)Tc. Its corresponding rhenium analogue was synthesized, and the fluorescent staining was performed in brain sections of both Tg mouse and Alzheimer's disease (AD) patient. The fluorescent rhenium complex Re-MAMA-BTA selectively bound to the amyloid aggregates in the brain sections of both APP Tg mouse and AD patient. The analogous (99m)Tc-MAMA-BTA complex could enter the normal mouse brain with high initial uptake. These results are encouraging for further exploration of their derivatives as imaging agents for Abeta plaques in the brain.
Chen
Xiangji
X
Key Laboratory of Radiopharmaceuticals, (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
Yu
Pingrong
P
Zhang
Lianfeng
L
Liu
Boli
B
D000544:Alzheimer Disease / Q000000981:diagnostic imaging* / Q000378:metabolism; D000577:Amides / Q000737:chemistry; D000588:Amines / Q000737:chemistry; D016229:Amyloid beta-Peptides / Q000032:analysis* / Q000378:metabolism; D000818:Animals; D052160:Benzothiazoles / Q000737:chemistry; D001812:Blood-Brain Barrier / Q000378:metabolism; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism; D006801:Humans; D007553:Isotope Labeling; D008297:Male; D051379:Mice; D008856:Microscopy, Fluorescence; D008875:Middle Aged; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D012211:Rhenium / Q000737:chemistry; D017556:Technetium Compounds / Q000737:chemistry; D014018:Tissue Distribution
C111133:2-(4-aminophenyl)benzothiazole; C528725:99mTc-MAMA-BTA; D000577:Amides; D000588:Amines; D016229:Amyloid beta-Peptides; D052160:Benzothiazoles; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; D017556:Technetium Compounds; D012211:Rhenium