It is widely accepted that uptake and efflux transporters on clearance organs play crucial roles in drug disposition. Although in vitro transporter assay system can identify the intrinsic properties of the target transporters, it is not so easy to precisely predict in vivo pharmacokinetic parameters from in vitro data. Positron emission tomography (PET) imaging is a useful tool to directly assess the activity of drug transporters in humans.
View Article and Find Full Text PDFVarious positron emission tomography (PET) probes have been developed to assess in vivo activities in humans of drug transporters, which aid in the prediction of pharmacokinetic properties of drugs and the impact of drug-drug interactions. We developed a new PET probe, sodium (3, 5)-3, 5-dihydroxy-7-((1 2, 6, 8)-6-hydroxy-2-methyl-8- ((1-[C]-()-2-methyl-but-2-enoyl) oxy) -1, 2, 6, 7, 8, 8-hexahydronaphthalen-1-yl) heptanoate ([C]DPV), and demonstrated its usefulness for the quantitative investigation of Oatps (gene symbol ) and Mrp2 (gene symbol ) in rats. To further analyze the species differences and verify the pharmacokinetic parameters in humans, serial PET scanning of the abdominal region with [C]DPV was performed in six healthy volunteers with and without an OATP1Bs and MRP2 inhibitor, rifampicin (600 mg, oral), in a crossover fashion.
View Article and Find Full Text PDFPurpose: Gastrointestinal (GI) bleeding scintigraphy in combination with single-photon emission computed tomography/computed tomography (SPECT/CT) remains to be studied in detail. This study aimed to examine the diagnostic ability of this tool.
Methods: GI bleeding scintigraphy using (99m)Tc-human serum albumin-diethylenetriaminepentaacetic acid was performed for 38 patients with suspected GI bleeding.
Nihon Hoshasen Gijutsu Gakkai Zasshi
August 2004
We have been using an X-ray angiography system that incorporates a flat panel detector (FPD) since December 2001. This system is equipped with the scintillator-type FPD PaxScan 4030A from Varian Medical Systems, and for objective comparison of the image intensifier (I.I.
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