Author(s)

A. Blair, L. Stevenson, D. Dewar, S. L. Pimlott, A. Sutherland

ISBN

2040-2503

Publication year

2013

Periodical

Medchemcomm

Periodical Number

11

Volume

4

Pages

1461-1466

Author Address

Sutherland, A Univ Glasgow, Sch Chem, WestCHEM, Joseph Black Bldg, Glasgow G12 8QQ, Lanark, Scotland Univ Glasgow, Sch Chem, WestCHEM, Glasgow G12 8QQ, Lanark, Scotland Univ Glasgow, Coll Med Vet & Life Sci, Inst Neurosci & Psychol, Glasgow G12 8QQ, Lanark, Scotland Univ Glasgow, West Scotland Radionuclide Dispensary, Glasgow G11 6NT, Lanark, Scotland North Glasgow Univ Hosp NHS Trust, Glasgow G11 6NT, Lanark, Scotland

Full version

In an effort to develop a new SPECT imaging agent for the translocator protein (TSPO), a series of novel iodinated quinoline-2-carboxamides have been synthesised and evaluated for binding affinity using rat brain homogenates. The outcome of the biological testing in combination with HPLC determination of the physicochemical properties of these compounds directed the design of new analogues resulting in 4-(2-iodophenyl)quinoline-2-N-diethylcarboxamide, a new TSPO ligand with higher affinity than the widely used clinical imaging agent PK11195.