New iodinated quinoline-2-carboxamides for SPECT imaging of the translocator protein.
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.
Stevenson
Louise
L
WestCHEM, Department of Chemistry, The Joseph Black Building, University of Glasgow, Glasgow G12 8QQ, UK.
Tavares
Adriana A S
AA
Brunet
Aurélie
A
McGonagle
Fiona I
FI
Dewar
Deborah
D
Pimlott
Sally L
SL
Sutherland
Andrew
A
D000818:Animals; D000970:Antineoplastic Agents / Q000378:metabolism; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism; D002352:Carrier Proteins / Q000737:chemistry / Q000378:metabolism*; D007457:Iodine Radioisotopes / Q000737:chemistry / Q000378:metabolism*; D007546:Isoquinolines / Q000378:metabolism; D008297:Male; D011485:Protein Binding / Q000502:physiology; D011804:Quinolines / Q000737:chemistry / Q000378:metabolism*; D051381:Rats; D011963:Receptors, GABA-A / Q000737:chemistry / Q000378:metabolism*; D015899:Tomography, Emission-Computed, Single-Photon / Q000379:methods
D000970:Antineoplastic Agents; D002352:Carrier Proteins; D007457:Iodine Radioisotopes; D007546:Isoquinolines; D011804:Quinolines; D011963:Receptors, GABA-A; C069997:Tspo protein, rat; C037850:PK 11195