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Use of [18F]FDOPA-PET for in vivo evaluation of dopaminergic dysfunction in unilaterally 6-OHDA-lesioned rats
Ki values determined using [18F]FDOPA-PET correlated significantly with the severity of dopaminergic dysfunction, which is useful in the development of new drugs and therapies for Parkinson's disease (PD).
In Vivo Expression of Cyclooxygenase-1 in Activated Microglia and Macrophages During Neuroinflammation Visualized by PET with 11C-Ketoprofen Methyl Ester
11C-ketoprofen methyl ester is identified as a COX-1–selective PET probe and a time-dependent expression of COx-1 in activated microglia and macrophages during the neuroinflammatory process in the living brain is demonstrated.
mRNA Expression and Transport Characterization of Conditionally Immortalized Rat Brain Capillary Endothelial Cell Lines; a New in vitro BBB Model for Drug Targeting
The conditionally immortalized rat brain capillary endothelial cell lines (TR-BBB) had endothelial makers, expressed mRNA for tight-junction strand proteins and the influx and efflux transporters and produced GLUT-1, which is capable of 3-OMG transport activity.
Evaluation of dextromethorphan metabolism using hepatocytes from CYP2D6 poor and extensive metabolizers.
Cryopreserved human hepatocytes of CYP2D6 poor metabolizer (PM) for the estimation of the metabolism in PM using dextromethorphan (DEX) as the probe drug for CYP1D6 substrate reflected the clinical data, and results would suggest that CYP 2D6 PM hepatocytes could be a good in vitro tool for estimating CYP3A4/5 PM pharmacokinetics.
Whole-body distribution and radiation dosimetry of [11C]telmisartan as a biomarker for hepatic organic anion transporting polypeptide (OATP) 1B3.
Telmisartan is a safe PET tracer with a dosimetry profile comparable to other common (11)C PET tracers.
Structure-activity relationship study of novel NR2B-selective antagonists with arylamides to avoid reactive metabolites formation.
A novel potent NMDA-NR2B selective antagonist without the reactive metabolites formation issue was identified. Through this study, a close correlation between reactive metabolites formation and
PET Imaging–Based Evaluation of Hepatobiliary Transport in Humans with (15R)-11C-TIC-Me
PET image analysis with (15R)-11C-TIC-Me is useful for investigating variations in OATP function in the human hepatobiliary transport system and demonstrated that in humans, ( 15R)- 11C- TIC–associated radioactivity is excreted into the bile by organic anion transport systems.
Characterization of the Amino Acid Transport of New Immortalized Choroid Plexus Epithelial Cell Lines: A Novel In Vitro System for Investigating Transport Functions at the Blood-Cerebrospinal Fluid
Immortalized choroid plexus epithelial cell lines were successfully established from Tg rats and have the properties of choroids plexUS epithelial cells, and amino acid transport activity was observed in vivo.
General method for the (11)C-labeling of 2-arylpropionic acids and their esters: construction of a PET tracer library for a study of biological events involved in COXs expression.
(11)C-labeling of 2-arylpropionic acids and their methyl esters as PET tracers of NSAIDs to construct a potentially useful PET tracer library for in vivo imaging of inflammation involved in COXs expression is succeeded.
The involvement of organic anion transporting polypeptide in the hepatic uptake of telmisartan in rats: PET studies with [¹¹C]telmisartan.
The results suggested that the hepatic uptake of telmisartan mainly consists of a saturable process mediated by Oatps in rats, according to noninvasive real-time measurement of tissue radioactivity with the use of PET.