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The sedating effect of first generation H1-antihistamines has been associated with their ability to penetrate the blood-brain barrier (BBB) and lack of efflux by P-glycoprotein (Pgp). Second generation H1-antihistamines are relatively free of sedation and their limited brain penetration has been suggested to arise from Pgp-mediated efflux. The objective of(More)
Brain tumors are one of the most lethal and difficult to treat. Their treatment is limited by the inadequate delivery of antitumor drugs to the tumor. In order to overcome this limitation, the possibility of the nose-brain direct transport pathway was evaluated using methotrexate (MTX) as a model antitumor agent. The direct transport of nasal MTX to the(More)
In order to develop a new positron emission tomography (PET) probe to study hepatobiliary transport mediated by the multi-drug and toxin extrusion transporter 1 (MATE1), (11)C-labelled metformin was synthesized and then evaluated as a PET probe. [(11)C]Metformin ([(11)C]4) was synthesized in three steps, from [(11)C]methyl iodide. Evaluation by small animal(More)
The purpose of this study was to establish a method for imaging the process of gastrointestinal (GI) absorption and subsequent biodistribution in the human body after oral drug administration, using positron emission tomography (PET) with 2-[(18)F]fluoro-2-deoxy-D-glucose ([(18)F]FDG). First, we developed a method to deliver the radiotracer safely into the(More)
To evaluate the function of multidrug and toxin extrusion proteins (MATEs) using 11C-labeled metformin ([11C]metformin) by positron emission tomography (PET). PET was performed by intravenous bolus injection of [11C]metformin. Pyrimethamine at 0.5 and 5 mg/kg was intravenously administered to mice 30 min prior to the scan. Integration plot analysis was(More)
We developed a pravastatin derivative, sodium (3R,5R)-3,5-dihydroxy-7-((1S,2S,6S,8S)-6-hydroxy-2-methyl-8-((1-[(11)C]-(E)-2-methyl-but-2-enoyl)oxy)-1,2,6,7,8,8a-hexahydronaphthalen-1-yl)heptanoate ([(11)C]DPV), as a positron emission tomography (PET) probe for noninvasive measurement of hepatobiliary transport, and conducted pharmacokinetic analysis in rats(More)
A case of schwannoma of the cervical spinal cord presenting with cervical angina is reported. A 49-year-old man was admitted to our hospital with severe chest pain, cold sweats, and unconsciousness. Extensive cardiac examination showed no abnormal findings. Neurological deficits were muscular weakness and atrophy of the left arm, bilateral hypersthesia of(More)
To develop potent drugs for oral use, information on their pharmacokinetic (PK) properties after oral administration is of great importance. We have recently reported the utility of positron emission tomography (PET) for the analysis of gastrointestinal (GI) absorption of radiolabeled compounds. In this study, PET image analysis was performed in rats using(More)
To dynamically analyze the processes of oral absorption and hepatobiliary distribution of telmisartan using positron emission tomography (PET). 11C-labeled telmisartan ([11C]TEL) was orally administered to rats with or without non-radiolabeled telmisartan (0.5, and 10 mg/kg). PET scanning of abdominal region and whole body was performed under conscious(More)
OBJECTIVE AND IMPORTANCE A patient with an extensive cranial base meningioma that included bilateral invasion of Meckel's cave underwent surgical resection and had an unexpected rare complication, malocclusion from bilateral trigeminal dysfunction. CLINICAL PRESENTATION A 19-year-old male patient was admitted to our hospital with alternating painful(More)