2-[18F]fluoro-A-85380, an in vivo tracer for the nicotinic acetylcholine receptors

被引:76
|
作者
Horti, AG
Scheffel, U
Koren, AO
Ravert, HT
Mathews, WB
Musachio, JL
Finley, PA
London, ED
Dannals, RF
机构
[1] Johns Hopkins Med Inst, Div Nucl Med, Baltimore, MD 21205 USA
[2] Johns Hopkins Med Inst, Div Radiat Hlth Sci, Baltimore, MD 21205 USA
[3] NIDA, Intramural Res Program, Brain Imaging Ctr, Baltimore, MD 21224 USA
关键词
A-85380; derivative; nicotinic receptor; acetylcholine receptor; radiotracer; brain distribution; pharmacology; PET;
D O I
10.1016/S0969-8051(98)00031-6
中图分类号
R8 [特种医学]; R445 [影像诊断学];
学科分类号
1002 ; 100207 ; 1009 ;
摘要
The in vivo brain regional distribution of 2-[F-18]fluoro-A-85380, a novel tracer for positron emission tomographic (PET) studies, followed the regional densities of brain nAChRs reported in the literature. Evidence of binding to nAChRs and high specificity of the binding in vivo was demonstrated by inhibition with nAChR selective ligands as well as with unlabeled 2-fluoro-A-85380. A preliminary toxicology study of the 2-fluoro-A-85380 showed a relatively low biological effect. 2-[F-18]Fluoro-A-85380 holds promise as a useful radiotracer for imaging of nAChRs with PET. (C) 1998 Elsevier Science Inc.
引用
收藏
页码:599 / 603
页数:5
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