Synthesis of two novel [18F]fluorobenzene-containing radiotracers via spirocyclic iodonium ylides and positron emission tomography imaging of translocator protein (18 kDa) in ischemic brain

2018 ◽  
Vol 16 (37) ◽  
pp. 8325-8335 ◽  
Author(s):  
Masayuki Fujinaga ◽  
Katsushi Kumata ◽  
Yiding Zhang ◽  
Akiko Hatori ◽  
Tomoteru Yamasaki ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Positron Emission Tomography Imaging ◽  
Translocator Protein ◽  
Emission Tomography ◽  
Ischemic Brain ◽  
Tomography Imaging ◽  
Positron Emission ◽  
Translocator Protein 18 Kda ◽  
Iodonium Ylides ◽  
The Brain

A new radiotracer for imaging TSPO: Ki, 0.70 nM and no radiolabeled metabolite in the brain.

scholarly journals Diphenhydramine as a selective probe to study H+-antiporter function at the blood–brain barrier: Application to [11C]diphenhydramine positron emission tomography imaging

2016 ◽  
Vol 37 (6) ◽  
pp. 2185-2195 ◽  
Author(s):  
Sylvain Auvity ◽  
Hélène Chapy ◽  
Sébastien Goutal ◽  
Fabien Caillé ◽  
Benoit Hosten ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Blood Brain Barrier ◽  
Positron Emission Tomography Imaging ◽  
Emission Tomography ◽  
Brain Barrier ◽  
Tomography Imaging ◽  
Blood Brain ◽  
Positron Emission ◽  
The Brain

Diphenhydramine, a sedative histamine H1-receptor (H1R) antagonist, was evaluated as a probe to measure drug/H+-antiporter function at the blood–brain barrier. In situ brain perfusion experiments in mice and rats showed that diphenhydramine transport at the blood–brain barrier was saturable, following Michaelis–Menten kinetics with a Km = 2.99 mM and Vmax = 179.5 nmol s−1 g−1. In the pharmacological plasma concentration range the carrier-mediated component accounted for 77% of diphenhydramine influx while passive diffusion accounted for only 23%. [14C]Diphenhydramine blood–brain barrier transport was proton and clonidine sensitive but was influenced by neither tetraethylammonium, a MATE1 (SLC47A1), and OCT/OCTN (SLC22A1-5) modulator, nor P-gp/Bcrp (ABCB1a/1b/ABCG2) deficiency. Brain and plasma kinetics of [11C]diphenhydramine were measured by positron emission tomography imaging in rats. [11C]Diphenhydramine kinetics in different brain regions were not influenced by displacement with 1 mg kg−1 unlabeled diphenhydramine, indicating the specificity of the brain positron emission tomography signal for blood–brain barrier transport activity over binding to any central nervous system target in vivo. [11C]Diphenhydramine radiometabolites were not detected in the brain 15 min after injection, allowing for the reliable calculation of [11C]diphenhydramine brain uptake clearance (Clup = 0.99 ± 0.18 mL min−1 cm−3). Diphenhydramine is a selective and specific H+-antiporter substrate. [11C]Diphenhydramine positron emission tomography imaging offers a reliable and noninvasive method to evaluate H+-antiporter function at the blood–brain barrier.

Positron-Emission-Tomography Imaging of Long-Term Expression of the 18kDa Translocator Protein After Sudden Cardiac Arrest in Rats

Shock ◽  
2020 ◽  
Vol Publish Ahead of Print ◽  
Author(s):  
Daniel C. Schroeder ◽  
Erik Popp ◽  
Cathrin Rohleder ◽  
Stefanie Vus ◽  
David de la Puente Bethencourt ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Cardiac Arrest ◽  
Sudden Cardiac Arrest ◽  
Positron Emission Tomography Imaging ◽  
Translocator Protein ◽  
Emission Tomography ◽  
Tomography Imaging ◽  
Positron Emission
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