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
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.