Results: 4

1.
Figure 3

Figure 3. From: The role of the equilibrative and concentrative nucleoside transporters in the intestinal absorption of the nucleoside drug, ribavirin, in wild-type and Ent1(-/-) mice.

Dose-normalized plasma ribavirin concentrations after 20 μM (●) ribavirin intestinal perfusions in wild-type mice (filled symbols) were significantly greater than in Ent1(−/−) mice (open symbols) at 33 minutes, but there was no significant difference after 200 (▲)or 5000 (■) μM perfusions. *= p<0.05 20 μM wild-type compared to 20 μM Ent1(−/−). N=4 for all treatments. Error bars indicate standard deviations in all panels.

Aaron M. Moss, et al. Mol Pharm. 2012 September 4;9(9):2442-2449.
2.
Figure 4

Figure 4. From: The role of the equilibrative and concentrative nucleoside transporters in the intestinal absorption of the nucleoside drug, ribavirin, in wild-type and Ent1(-/-) mice.

A graphical illustration describing the proposed mechanisms of intestinal absorption of 20 or 200 and 5000 μM ribavirin in mice. The absorption of ribavirin into the enterocytes from the intestinal lumen is a saturable, sodium-dependent process, largely mediated by mCnt2. Once in the enterocytes, the vectorial transport of ribavirin into the mesenteric blood is mediated by mEnt1 plus other unknown transport processes which are also saturable. In addition, phosphorylation as well as non-phosphorylation metabolism are saturable elimination processes that influence the intestinal bioavailability and portal concentrations of ribavirin or its metabolites. The size of the arrows show the relative magnitude of the pathways.

Aaron M. Moss, et al. Mol Pharm. 2012 September 4;9(9):2442-2449.
3.

Figure 2. From: The role of the equilibrative and concentrative nucleoside transporters in the intestinal absorption of the nucleoside drug, ribavirin, in wild-type and Ent1(-/-) mice.

Dose-normalized intestinal total radioactivity concentrations at 30 minutes after 200 and 5000 μM ribavirin intestinal perfusions in wild-type and Ent1(−/−) mice in the presence of sodium were significantly greater than after 20 μM perfusions (A). The same trend was observed for intestinal ribavirin plus phosphorylated metabolites concentration, but the fold-change was greater between 200 and 5000 vs. 20 μM perfusions (B). In contrast to the perfusions in the presence of sodium, in the absence of sodium, the intestinal ribavirin concentration after 200 μM perfusions was considerably reduced (C). In 2A and 2B, ***= p<0.001, **=p<0.01 compared to 20 μM wild-type; †††= p<0.001, ††= p<0.01 compared to 20 μM Ent1(−/−). In 2C, ***= p<0.001 compared to all others; †††= p<0.001 compared to 20 μM in absence of sodium. N=4 for all treatments. Error bars indicate standard deviations in all panels.

Aaron M. Moss, et al. Mol Pharm. 2012 September 4;9(9):2442-2449.
4.

Figure 1. From: The role of the equilibrative and concentrative nucleoside transporters in the intestinal absorption of the nucleoside drug, ribavirin, in wild-type and Ent1(-/-) mice.

The effective ribavirin intestinal permeability (Peff) in wild-type mice was not significantly different than in Ent1(−/−) mice, in the presence of sodium, after 30 minutes of 20, 200 or 5000 μM ribavirin intestinal perfusions (A). In contrast, ribavirin’s Peff in wild-type and Ent1(−/−) mice was significantly reduced in the absence of sodium (B). Ribavirin’s Peff after 20 μM perfusions was unaffected by 250 μM thymidine, a Cnt3 inhibitor, but was significantly reduced by 500 μM formycin B, a Cnt2 inhibitor (C). The inset graphs in 1A and 1B display the % ribavirin remaining in the intestinal lumen of mice during 20 μM (triangles), 200 μM (squares) and 5000 μM (diamonds, 1A only) perfusions displayed by the main graph. In 1A, **= p<0.01, compared to higher concentrations. In 1B **= p<0.01, *= p<0.05 compared to same concentration in absence of sodium. In 1C *= p<0.05 compared to +Na+; †= p<0.05 compared to –Na+. N=4 for all treatments. Error bars indicate standard deviations in all panels.

Aaron M. Moss, et al. Mol Pharm. 2012 September 4;9(9):2442-2449.

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