2-[18F]F-A-85380: a PET radioligand for alpha4beta2 nicotinic acetylcholine receptors.

Journal Article

2-[18F]fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-[18F]F-A-85380), a ligand for nicotinic acetylcholine receptors (nAChRs) was evaluated in an in vitro binding assay with membranes of rat brain and in vivo by PET in Rhesus monkey brain. The ligand has high affinity for alpha4beta2 nAChRs (K(D)=50 pM), crosses the blood-brain barrier, and distributes in the monkey brain in a pattern consistent with that of alpha4beta2 nAChRs. The specific/non-specific binding ratio increased steadily, reaching a value of 3.3 in the thalamus at 4 h. The specific binding of 2-[18F]F-A-85380 was reversed by cytisine. These results, in combination with the data demonstrating low toxicity of 2-[18F]F-A-85380, indicate that this ligand shows promise for use with PET in human subjects.

Full Text

Duke Authors

Cited Authors

  • Chefer, SI; Horti, AG; Koren, AO; Gündisch, D; Links, JM; Kurian, V; Dannals, RF; Mukhin, AG; London, ED

Published Date

  • September 9, 1999

Published In

Volume / Issue

  • 10 / 13

Start / End Page

  • 2715 - 2721

PubMed ID

  • 10511429

International Standard Serial Number (ISSN)

  • 0959-4965

Language

  • eng

Conference Location

  • England