Synthesis and evaluation of two 18F-labeled imidazo[1,2-a]pyridine analogues as potential agents for imaging beta-amyloid in Alzheimer's disease.
Two new fluorinated imidazo[1,2-a]pyridine derivatives, 6-(2'-fluoroethyl)-2-(4'-dimethylamino)phenylimidazo[1,2-a]pyridine (FEPIP) and 6-(3'-fluoropropyl)-2-(4'-dimethylamino)phenylimidazo[1,2-a]pyridine (FPPIP), were synthesized. The binding affinity for FEPIP and FPPIP to amyloid plaques in human AD cortical tissues was determined. Radiolabeling, in vitro film autoradiography, and micro-PET study were performed with [18F]FPPIP to determine its utility as a radioligand for amyloid plaque imaging in the brain of AD patients.
Zeng
Fanxing
F
Department of Radiology, Division of Radiological Sciences, Emory University, Atlanta, GA 30322, USA.
Southerland
Jeanine A
JA
Voll
Ronald J
RJ
Votaw
John R
JR
Williams
Larry
L
Ciliax
Brian J
BJ
Levey
Allan I
AI
Goodman
Mark M
MM
D000544:Alzheimer Disease / Q000175:diagnosis* / Q000378:metabolism*; D016229:Amyloid beta-Peptides / Q000378:metabolism*; D000818:Animals; D005462:Fluorine Radioisotopes / Q000737:chemistry; D006801:Humans; D008253:Macaca mulatta; D015394:Molecular Structure; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry*
D016229:Amyloid beta-Peptides; D005462:Fluorine Radioisotopes; D011725:Pyridines; C001439:imidazo(1,2-a)pyridine