两种18F标记的咪唑并[1,2-a]吡啶类似物作为阿尔茨海默病中β-淀粉样蛋白成像潜在剂的合成与评价
Synthesis and evaluation of two 18F-labeled imidazo[1,2-a]pyridine analogues as potential agents for imaging beta-amyloid in Alzheimer's disease.
作者信息
Zeng Fanxing, Southerland Jeanine A, Voll Ronald J, Votaw John R, Williams Larry, Ciliax Brian J, Levey Allan I, Goodman Mark M
机构信息
Department of Radiology, Division of Radiological Sciences, Emory University, Atlanta, GA 30322, USA.
出版信息
Bioorg Med Chem Lett. 2006 Jun 1;16(11):3015-8. doi: 10.1016/j.bmcl.2006.02.055. Epub 2006 Mar 29.
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.
合成了两种新型氟化咪唑并[1,2 - a]吡啶衍生物，即6 - (2'-氟乙基)-2 - (4'-二甲氨基)苯基咪唑并[1,2 - a]吡啶（FEPIP）和6 - (3'-氟丙基)-2 - (4'-二甲氨基)苯基咪唑并[1,2 - a]吡啶（FPPIP）。测定了FEPIP和FPPIP与人AD皮质组织中淀粉样斑块的结合亲和力。用[18F]FPPIP进行放射性标记、体外薄膜放射自显影和微型PET研究，以确定其作为AD患者脑内淀粉样斑块成像放射性配体的效用。
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