Ringlike uptake of [18F]FDG in brain abscess: a PET study.
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Brain Abscess↗
Biomedical subjects
M Otsuka
Publications and source records attributed to M Otsuka.
Clinical evaluation of Ga-67 DFO-DAS-fibrinogen scintigraphy.
Gallium-67 DFO-DAS-fibrinogen scintigraphy was performed in four patients for the detection of tumor and thrombosis. No adverse reactions were noted. Scintigrams in a patient with bronchogenic carcinoma accompanied with atelectasis showed abnormal uptake not only in the cancerous region but also in the whole atelectatic region as well. In a patient with hepatoma after TAE, a slight uptake of tracer was noted in the area surrounding the tumorous region, indicating accumulation of the tracer in the microthrombi. In two patients with venous thrombosis, no abnormal uptake was seen. The long interval from the onset of thrombus formation and the commencement of anticoagulant therapy prior to scintigraphy may have caused the false-negative scans in these cases. Further evaluation is necessary with regard to the usefulness of this technique in clinical practice.
Aged↗
Metabolism of denopamine, a new cardiotonic agent, in the rat and dog.
The metabolism of denopamine, (R)-(-)-1-(p-hydroxyphenyl)-2-[(3,4-dimethoxyphenethyl)amino] ethanol, a new, orally active, selectively inotropic cardiotonic agent, was studied in the rat and dog. Animals were given single oral doses of 5 mg/kg of denopamine labeled with 14C. Denopamine was metabolized in the rat and dog by several pathways including conjugation, side chain oxidation, and ring hydroxylation followed by O-methylation. Rats excreted the drug in the urine almost entirely as unchanged drug and its phenolic O-glucuronide whereas in the dog, the major metabolites were the phenolic O-glucuronide, the alcoholic O-glucuronide, and the phenolic O-sulfate of denopamine and the phenolic O-glucuronide of 3-methoxydenopamine. Demethylation, which has been shown to be a major metabolic pathway in man, and side chain oxidation were minor pathways in the rat and dog. Furthermore, a high degree of stereoselective resistance of the alcoholic O-glucuronide of denopamine to hydrolysis by beta-glucuronidase was observed.
Animals↗
Comparative study on the disposition of a new orally active dopamine prodrug, N-(N-acetyl-L-methionyl)-O,O-bis(ethoxycarbonyl)dopamine (TA-870) and dopamine hydrochloride in rats and dogs.
The pharmacokinetics of a dopamine derivative, TA-870, and dopamine (DA) after oral administration are compared in rats and dogs. The maximum concentrations of free DA in plasma after oral administration of TA-870 were 150 ng/ml in the rat (30 mg/kg) and 234 ng/ml in the dog (33.5 mg/kg). On the contrary, the maximum plasma concentrations after oral administration of DA at an equimolar dose to TA-870 were 12 ng/ml in the rat (12 mg/kg) and 36 ng/ml in the dog (13.5 mg/kg). The AUC values of free DA in plasma after oral administration of TA-870 (30 or 33.5 mg/kg) were 4-6 times higher than those after DA in both animal species. The peak tissue levels of radioactivity in rats after oral administration of [14C]TA-870 (30 mg/kg) were also 5.5 times higher in the liver and 1-2 times higher in other tissues than those after [14C]DA dose (12 mg/kg). In rats, the main excretion route of radioactivity after oral administration of [14C]TA-870 or DA was via the urine. The total recoveries of radioactivity in the urine and feces were 91-96% of the dose within 24 hr for both compounds. Biliary excretion in rats accounted for 19.8% of the dose of [14C]TA-870 and 12.6% of the dose of [14C]DA within 24 hr. These results demonstrate that TA-870 was well absorbed from the digestive tract, extensively metabolized to dopamine, and proved to be an orally usable dopamine prodrug.
Animals↗
Identification and measurement of urinary metabolites of afloqualone in man.
Major urinary metabolites in man of 6-amino-2-fluoromethyl-3-(o-tolyl)-4-(3H)-quinazolinone (afloqualone, I), a new centrally acting muscle relaxant, were identified by GC/MS. Simultaneous quantitative determination of the metabolites was made by mass chromatography using deuterium-labeled internal standards. Approximately 4% of the dose was excreted as unchanged I within 32 hr after oral administration. The major metabolites identified in the neutral and basic fractions of the urine were N-acetylafloqualone (II, 0.3% of the dose), N-acetyl-2'-hydroxymethylafloqualone (III, 5.5%), N-glycolylafloqualone (IV, 0.9%), and N-glycolyl-2'-hydroxy-methylafloqualone (V, 1.3%). I and IV were also excreted in conjugated form as N-glucuronide (VI, 8.0%) and O-glucuronide and/or sulfate (VII, 0.4%), respectively. Other phenolic and sulfur-containing metabolites of I, which have previously been identified in the urine of rats, dogs, or monkeys, were not detected in the human urine. Thus, the main routes of metabolism of I in man consist of N-acetylation followed by hydroxylation at the 2'-methyl and acetylmethyl carbons, and glucuronidation of the aromatic amino group. This pattern of metabolism of I in man was in part similar to that observed in rats and monkeys, but drastically different from that in dogs.
Adult↗
Trichosporon detected on bile cytology.
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Aged↗
Protecting the viability of hepatic allografts procured from non-heart-beating donors by blockade of endothelin and platelet activating factor in porcine liver transplantation.
PROBLEM: The function of hepatic allograft from non-heartbeating donors (NHBD) is significantly affected by warm ischemic injury before harvesting. MATERIALS AND METHODS: The effects of the endothelin (ET) antagonist TAK-044 and the platelet activating factor (PAF) antagonist E5880 on the function of grafts from NHBD were evaluated in a porcine orthotopic liver transplantation. The liver grafts were subjected to 90 min of warm ischemia and 4 hours cold preservation. Group 1 (n = 4; n is the number of donor/recipient pairs) was used as a control (untreated). In group 2 (n = 4), donors and recipients were treated with TAK-044 (3 mg/kg). In group 3 (n = 4), pigs were treated with E5880 (0.3 mg/kg). In group 4 (n = 4), pigs were treated with TAK-044 and E5880. RESULTS: The 7 day survival rate of the recipients in groups 1, 2, 3 and 4 was 0, 25, 25 and 100%, respectively (p<0.05, group 1 versus 4). The increases of the serum concentrations of aspartate transaminase, lactate dehydrogenase and arterial lactate 1-4 hours after transplantation were significantly inhibited in the treated groups. CONCLUSION: The blockade of ET and PAF has protective effects on the function of hepatic grafts from NHBD.
Animals↗