Exploration of the structure-activity relationship of the diaryl anilide class of ligands for translocator protein--potential novel positron emitting tomography imaging agents.
A series of novel ligands based on the diaryl anilide (DAA) class of translocator protein (TSPO) ligands was synthesised and evaluated as potential positron emitting tomography (PET) ligands for imaging TPSO in vivo. Fluorine-18 labelling of the molecules was achieved using direct radiolabelling or synthon based labelling approaches. Several of the ligands prepared have promising profiles as potential TSPO PET imaging ligands and will be evaluated further as potential clinical imaging agents.
GE Healthcare, The Grove Centre, White Lion Road, Amersham, Bucks HP7 9LL, UK.
Harry
H
Wadsworth
Paul A
PA
Jones
Wai-Fung
WF
Chau
Clare
C
Durrant
Véronique
V
Morisson-Iveson
Joanna
J
Passmore
Dennis
D
O'Shea
Duncan
D
Wynn
Imtiaz
I
Khan
Andrew
A
Black
Michelle
M
Avory
William
W
Trigg
D000813:Anilides / Q000737:chemistry* / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000378:metabolism; D002352:Carrier Proteins / Q000032:analysis* / Q000737:chemistry / Q000378:metabolism; D005462:Fluorine Radioisotopes; D006321:Heart; D008024:Ligands; D049268:Positron-Emission Tomography / Q000379:methods*; D051381:Rats; D017208:Rats, Wistar; D011963:Receptors, GABA-A / Q000032:analysis* / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship; D014018:Tissue Distribution
D000813:Anilides; D002352:Carrier Proteins; D005462:Fluorine Radioisotopes; D008024:Ligands; D011963:Receptors, GABA-A; C069997:Tspo protein, rat