6-[18F]fluoro-A-85380:: An in vivo tracer for the nicotinic acetylcholine receptor

被引：31

作者：

Scheffel, U

Horti, AG

Koren, AO

Ravert, HT

Banta, JP

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, Brain Imaging Ctr, Intramural Res Program, Baltimore, MD USA

[4] CTI Inc, Knoxville, TN USA

来源：

NUCLEAR MEDICINE AND BIOLOGY | 2000年 / 27卷 / 01期

关键词：

6-[F-18]FA; A-85380; derivative; nicotinic acetylcholine receptor (nAChR); mouse brain distribution; radiotracer; PET;

D O I：

10.1016/S0969-8051(99)00082-7

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：

6-[F-18]Fluoro-3-(2(S)-azetidinylmethoxy (6-[F-18]fluoro-A-85380 or 6-[F-18]FA), a new tracer for positron emission tomography, was synthesized by no-carrier-added [F-18] fluorination of 6-iodo-3-((1-tert-butoxycarbonyl-2 (S)-azetidinyl)methoxy)pyridine followed by acidic deprotection. 6-[F-18]FA followed the regional densities of brain nicotinic acetylcholine receptors (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 6-FA. A preliminary toxicology study of the 6-FA showed a relatively low biological effect. NUCL MED BIOL 27;1:51-56, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.

引用

页码：51 / 56

页数：6

共 35 条

[1] Novel 3-pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors [J].