scholarly journals A novel 18F-labelled high affinity agent for PET imaging of the translocator protein

2015 ◽  
Vol 6 (8) ◽  
pp. 4772-4777 ◽  
Author(s):  
Adele Blair ◽  
Filip Zmuda ◽  
Gaurav Malviya ◽  
Adriana A. S. Tavares ◽  
Gilles D. Tamagnan ◽  
...  

A novel 18F-labelled quinoline-2-carboxamide has been characterised as a novel PET imaging agent for the translocator protein.

2015 ◽  
Vol 42 (9) ◽  
pp. 711-719 ◽  
Author(s):  
Wai-Fung Chau ◽  
Andrew M.A. Black ◽  
Alan Clarke ◽  
Clare Durrant ◽  
Ingvil Gausemel ◽  
...  

2010 ◽  
Vol 6 (3) ◽  
pp. 354-361 ◽  
Author(s):  
Unsong Oh ◽  
Masahiro Fujita ◽  
Vasiliki N. Ikonomidou ◽  
Iordanis E. Evangelou ◽  
Eiji Matsuura ◽  
...  

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Anton Lindberg ◽  
Ryosuke Arakawa ◽  
Tsuyoshi Nogami ◽  
Sangram Nag ◽  
Magnus Schou ◽  
...  

Abstract Background Over the last decade, a few radioligands have been developed for PET imaging of brain 5-HT1B receptors. The 5-HT1B receptor is a G-protein-coupled receptor (GPCR) that exists in two different agonist affinity states. An agonist ligand is expected to be more sensitive towards competition from another agonist, such as endogenous 5-HT, than an antagonist ligand. It is of interest to know whether the intrinsic activity of a PET radioligand for the 5-HT1B receptor impacts on its ability to detect changes in endogenous synaptic 5-HT density. Three high-affinity 11C-labeled 5-HT1B PET radioligands with differing intrinsic activity were applied to PET measurements in cynomolgus monkey to evaluate their sensitivity to be displaced within the brain by endogenous 5-HT. For these experiments, fenfluramine was pre-administered at two different doses (1.0 and 5.0 mg/kg, i.v.) to induce synaptic 5-HT release. Results A dose-dependent response to fenfluramine was detected for all three radioligands. At the highest dose of fenfluramine (5.0 mg/kg, i.v.), reductions in specific binding in the occipital cortex increased with radioligand agonist efficacy, reaching 61% for [11C]3. The most antagonistic radioligand showed the lowest reduction in specific binding. Conclusions Three 5-HT1B PET radioligands were identified with differing intrinsic activity that could be used in imaging high- and low-affinity states of 5-HT1B receptors using PET. From this limited study, radioligand sensitivity to endogenous 5-HT appears to depend on agonist efficacy. More extensive studies are required to substantiate this suggestion.


2021 ◽  
Vol 93 ◽  
pp. 37-45
Author(s):  
Kim H. Kwan ◽  
Ingrid J.G. Burvenich ◽  
Margaret M. Centenera ◽  
Yit Wooi Goh ◽  
Angela Rigopoulos ◽  
...  

2021 ◽  
Vol 96-97 ◽  
pp. S51-S52
Author(s):  
Antonia Högnäsbacka ◽  
Esther Kooijman ◽  
Robert Schuit ◽  
Maxime Schreurs ◽  
Mariska Verlaan ◽  
...  

2004 ◽  
Vol 32 (6) ◽  
pp. 724-724 ◽  
Author(s):  
Damian Wild ◽  
Helmut R. Mäcke ◽  
Beatrice Waser ◽  
Jean Claude Reubi ◽  
Mihaela Ginj ◽  
...  

2007 ◽  
Vol 50 (3) ◽  
pp. 165-170 ◽  
Author(s):  
Eyup Akgün ◽  
Philip S. Portoghese ◽  
Munawwar Sajjad ◽  
Hani A. Nabi
Keyword(s):  

Sign in / Sign up

Export Citation Format

Share Document