6-[18F]fluoro-A-85380, a novel radioligand for in vivo imaging of central nicotinic acetylcholine receptors

被引：41
|
作者：
Horti, AG
Chefer, SI
Mukhin, AG
Koren, AO
Gündisch, D
Links, JM
Kurian, V
Dannals, RF
London, ED
机构：
[1] NIDA, Brain Imaging Ctr, Intramural Res Program, NIH, Baltimore, MD 21224 USA
[2] Johns Hopkins Med Inst, Div Nucl Med, Baltimore, MD 21205 USA
[3] Johns Hopkins Med Inst, Div Radiat Hlth Sci, Baltimore, MD 21205 USA
来源：
LIFE SCIENCES | 2000年 / 67卷 / 04期
基金：
美国国家卫生研究院;
关键词：
nicotinic acetylcholine receptor; positron emission tomography (nAChRs); 6-[F-18]fluoro-3-(2(S)-azetidinyl-methoxy)pyridine; (6-[F-18]fluoro-A-85380; 6-[F-18]FA);
D O I：
10.1016/S0024-3205(00)00635-4
中图分类号：
R-3 [医学研究方法]; R3 [基础医学];
学科分类号：
1001 ;
摘要：
A novel positron emission tomography (PET) radiotracer, 6-[F-18]fluoro-3-(2(S)-azetidinyl-methoxy)pyridine (6-[F-18]fluoro-A-85380, 6-[F-18]FA) was synthesized by a no-carrier-added fluorination, In 6-[F-18]FA bound to nicotinic acetylcholine receptors (nAChRs), with very high affinity (K-d 28 PM). In PET studies, 6-[F-18]FA specifically labeled central nAChRs in the brain of the Rhesus monkey and demonstrated highest levels of accumulation of radioactivity in brain regions enriched with the a,Pz subtype of nAChR, 6-[F-18]FA exhibited a target-to-non-target ratio (estimated as radioactivity in the thalamus to that in the cerebellum) of binding in primate brain similar to that previously determined for a labeled analog of epibatidine, [F-18]FPH. In contrast to [F-18]FPH, the novel tracer is expected to exhibit substantially less toxicity. Thus, the novel radioligand, 6-[18F]FA, appears to be a suitable candidate for imaging nAChRs in human brain. Published by Elsevier Science Inc.
引用
收藏
页码：PL463 / PL469
页数：7
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