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

Authors
Scheffel, U Horti, AG Koren, AO Ravert, HT Banta, JP Finley, PA London, ED Dannals, RF
Citation
U. Scheffel et al., 6-[F-18]fluoro-A-85380: An in vivo tracer for the nicotinic acetylcholine receptor, NUCL MED BI, 27(1), 2000, pp. 51-56
Citations number
32
Categorie Soggetti
Medical Research Diagnosis & Treatment
Journal title
NUCLEAR MEDICINE AND BIOLOGY
ISSN journal
09698051 → ACNP
Volume
27
Issue
1
Year of publication
2000
Pages
51 - 56
Database
ISI
SICI code
0969-8051(200001)27:1<51:6AIVTF>2.0.ZU;2-0
Abstract
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 fo llowed the regional densities of brain nicotinic acetylcholine receptors (n AChRs) reported in the literature. Evidence of binding to nAChRs and high s pecificity 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.