TABLE 1

KF24345 inhibition of [³H]formycin B uptake by PK15-hENT1/hENT2 transfectants, human U2-OS cells, mouse C2C12 myoblasts, and rMVECs

[³H]Formycin B (10 μM) uptake assays were conducted in the presence and absence of a range of concentrations of KF24345 as shown in Fig. 2. U2-OS cells were tested both in the absence (total uptake) and presence (ei-mediated uptake) of 100 nM NBMPR. Results were fitted to both one-site and two-site inhibition models and statistically evaluated (F test; P < 0.05; GraphPad Prism version 4) for the best fit. Pseudo Hill coefficients (n_H) for KF24345 inhibition of [³H]formycin B uptake were calculated as the negative slopes of linear plots of inhibitor concentration (abscissa) versus log (B/B₀ - B), where B is the uptake in the presence of inhibitor, and B₀ is the uptake in the absence of inhibitor. Each value is the mean ± S.E.M. from at least five experiments conducted in duplicate.