Exploration of the structure-activity relationship of a novel tetracyclic class of TSPO ligands-potential novel positron emitting tomography imaging agents.

Authors :: O'Shea D
Ahmad R
Årstad E
Avory M
Chau WF
Durrant C
Hirani E
Jones PA
Khan I
Luthra SK
Mantzilas D
Morisson-Iveson V
Passmore J
Robins EG
Shan B
Wadsworth H
Walton S
Zhao Y
Trigg W
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Apr 15; Vol. 23 (8), pp. 2368-72. Date of Electronic Publication: 2013 Feb 24.
Publication Year :: 2013
Abstract: A series of novel TSPO ligands based on the tetracyclic class of translocator protein (TSPO) ligands first described by Okubo et al. 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.<br /> (Copyright © 2013 Elsevier Ltd. All rights reserved.)

Subjects :: Animals
Fluorine Radioisotopes chemistry
Isotope Labeling methods
Ligands
Protein Transport
Rats
Receptors, GABA chemistry
Structure-Activity Relationship
Positron-Emission Tomography methods
Receptors, GABA analysis
Receptors, GABA metabolism

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