A lipophilic thioflavin-T derivative for positron emission tomography (PET) imaging of amyloid in brain.
The synthesis of a new lipophilic thioflavin-T analogue (2-[4' -(methylamino)phenyl]benzothiazole, 6) with high affinity for amyloid is reported. Intravenous injection of [(11)C]-labeled 6 in control mice resulted in high brain uptake. Amyloid deposits were imaged with multiphoton microscopy in the brains of living transgenic mice following the systemic injection of unlabeled 6. [(11)C]6 is a promising amyloid imaging agent for Alzheimer's disease.
Mathis
Chester A
CA
PET Facility, Department of Radiology, University of Pittsburgh, PA 15213, USA. mathisca@msx.upmc.edu
Bacskai
Brian J
BJ
Kajdasz
Stephen T
ST
McLellan
Megan E
ME
Frosch
Matthew P
MP
Hyman
Bradley T
BT
Holt
Daniel P
DP
Wang
Yanming
Y
Huang
Guo-Feng
GF
Debnath
Manik L
ML
Klunk
William E
WE
D000544:Alzheimer Disease / Q000000981:diagnostic imaging; D000682:Amyloid / Q000378:metabolism*; D000818:Animals; D052160:Benzothiazoles; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000000981:diagnostic imaging*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D051379:Mice; D008822:Mice, Transgenic; D008853:Microscopy; D058225:Plaque, Amyloid / Q000000981:diagnostic imaging*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry*; D014055:Tomography, Emission-Computed
D000682:Amyloid; D052160:Benzothiazoles; D019275:Radiopharmaceuticals; D013844:Thiazoles; C009462:thioflavin T