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

Bioorg Med Chem Lett. 2010 Feb 1;20(3):954-7. doi: 10.1016/j.bmcl.2009.12.061. Epub 2009 Dec 22.

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.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / metabolism
  • Brain / diagnostic imaging
  • Brain / metabolism
  • Carrier Proteins / chemistry
  • Carrier Proteins / metabolism*
  • Iodine Radioisotopes / chemistry
  • Iodine Radioisotopes / metabolism*
  • Isoquinolines / metabolism
  • Male
  • Protein Binding / physiology
  • Quinolines / chemistry
  • Quinolines / metabolism*
  • Rats
  • Receptors, GABA-A / chemistry
  • Receptors, GABA-A / metabolism*
  • Tomography, Emission-Computed, Single-Photon* / methods

Substances

  • Antineoplastic Agents
  • Carrier Proteins
  • Iodine Radioisotopes
  • Isoquinolines
  • Quinolines
  • Receptors, GABA-A
  • Tspo protein, rat
  • PK 11195