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Disposition of 1,4,6,8-tetramethyl-furoquinolinone in normal and ascitic tumor bearing mice
No full textI.F. 0.687
1,4,6,8-Tetramethyl-2H-furo[2,3h]quinolin-2-one (FQ) belongs to a series of furocoumarin isosters, designed to obtain new drugs for photochemotherapy. The objective of this study was to characterize the disposition of orally administered 3H-FQ in normal and ascitic tumor bearing mice and to evaluate the influence of UVA irradiation in control mice. This compound was rapidly absorbed and its decay in serum was biphasic. Binding to serum proteins, which was maximum at 30 min (74 %), time-dependently declined. FQ was distributed to all the studied tissues, primarily to the liver and kidneys. The administered radioactivity was excreted mostly in the urine (43 %) and was associated with polar metabolites. The unchanged compound was not present to any detectable extent in the urine. Elimination in the faeces, that may include FQ not absorbed, was low (14 % of administered radioactivity), emphasizing the quantitatively efficient gastrointestinal absorption of the drug. UVA irradiation of FQ-treated mice for 2 h caused a significant increase in radioactivity measured in serum as well as in the liver. In mice bearing Ehrlich ascitic tumor, serum and tissue concentrations were lower than in control animals, possibly due to the larger volume of body fluids (10+/-4 ml of ascitic fluid) available for drug distribution
ADENOSINE MODULATES NO RELEASE IN AN EXPERIMENTAL INFLAMMATION MODEL OF RAT VASCULAR SMOOTH MUSCLE CELLS
No full text
Disposition of 4, 6, 4'-trimethylangelicin in mice maintained in the dark and after uva irradiation.
No full textimpact factor 0.79
The disposition of the furocoumarin 4,6,4'-trimethylangelicin (4,6,4'-TMA) was studied in mice. After oral administration of (3)H 4,6,4'-TMA, radioactivity measured in serum shows fast absorption and slow elimination. Serum protein binding is higher as compared to 8-methoxypsoralen (8-MOP), currently used in photochemotherapy (PUVA) and linearly declines from 30 min to 6 h after administration. Distribution in the various organs was similar to that of 8-MOP and was relatively uninfluenced by UVA radiation, required for the biological effects of 4,6,4'-TMA. Mice eliminate (3)H 4,6,4'-TMA mostly through the urine, but also through the faeces. Two metabolites were identified in the urine and serum of the treated mice, one of which proved to be a derivative of 4,6,4'-TMA, formed by hydrogenation of the double 4',5' bond of the furocoumarin nucleus
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