New iodinated quinoline-2-carboxamides for SPECT imaging of the translocator protein

Louise Stevenson, Adriana A. S. Tavares, Aurelie Brunet, Fiona I. McGonagle, Deborah Dewar, Sally L. Pimlott, Andrew Sutherland*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract

With the aim of developing new SPECT imaging agents for the translocator protein (TSPO), a small library of iodinated quinoline-2-carboxamides have been prepared and tested for binding affinity with TSPO. N,N-Diethyl-3-iodomethyl-4-phenylquinoline-2-carboxamide was found to have excellent affinity (K(i) 12.0 nM), comparable to that of the widely used TSPO imaging agent PK11195. (c) 2009 Elsevier Ltd. All rights reserved.

Original languageEnglish
Pages (from-to)954-957
Number of pages4
JournalBioorganic & Medicinal Chemistry Letters
Volume20
Issue number3
DOIs
Publication statusPublished - 1 Feb 2010

Keywords

  • SPECT
  • Imaging
  • Translocator protein
  • Quinoline-2-carboxamides
  • Heterocyclic synthesis
  • PERIPHERAL BENZODIAZEPINE-RECEPTOR
  • POSITRON-EMISSION-TOMOGRAPHY
  • CARBOXAMIDE DERIVATIVES
  • HIGH-AFFINITY
  • 18 KDA
  • POTENTIAL RADIOLIGANDS
  • BINDING-SITES
  • LIGAND
  • PET
  • BRAIN

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