Fluoro-pegylated (FPEG) imaging agents targeting Abeta aggregates.
A novel approach of producing positron emission tomography (PET) imaging agents through the formation of bioconjugates based on a pegylation-fluorination strategy resulting in fluoro-pegylated (FPEG) molecules is reported. This approach offers a simple and easy method by which to incorporate 18F in the target molecule without an appreciable increase in the lipophilicity. After 18F labeling, this convenient approach leads to PET imaging probes binding to Abeta aggregates in the brain (an important factor associated with Alzheimer's disease) using the known core structures, such as [2-(4-dimethylaminophenyl)-vinyl]-benzoxazol (3') or 2-phenylbenzothiazole (4). This approach appears to be effective in some core structures, but it cannot be uniformly applied to all structures.
Stephenson
Karin A
KA
Department of Radiology, University of Pennsylvania, 3700 Market Street, Room 305, Philadelphia, Pennsylvania 19104, USA. kunghf@sunmac.spect.upenn.edu
Chandra
Rajesh
R
Zhuang
Zhi-Ping
ZP
Hou
Catherine
C
Oya
Shunichi
S
Kung
Mei-Ping
MP
Kung
Hank F
HF
D016229:Amyloid beta-Peptides / Q000032:analysis* / Q000378:metabolism*; D000818:Animals; D001345:Autoradiography; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism; D005461:Fluorine / Q000737:chemistry*; D051379:Mice; D015394:Molecular Structure; D011092:Polyethylene Glycols / Q000737:chemistry*; D049268:Positron-Emission Tomography; D013696:Temperature
D016229:Amyloid beta-Peptides; D005461:Fluorine; D011092:Polyethylene Glycols