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Figure 1. Uptake of relebactam into human OAT1, OAT3 and OCT2 stably transfected cells. Time-dependent uptake of ... Figure 1. Uptake of relebactam into.

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Presentation on theme: "Figure 1. Uptake of relebactam into human OAT1, OAT3 and OCT2 stably transfected cells. Time-dependent uptake of ... Figure 1. Uptake of relebactam into."— Presentation transcript:

1 Figure 1. Uptake of relebactam into human OAT1, OAT3 and OCT2 stably transfected cells. Time-dependent uptake of ... Figure 1. Uptake of relebactam into human OAT1, OAT3 and OCT2 stably transfected cells. Time-dependent uptake of relebactam (2 μM) into MDCKII and MDCKII-OAT1 cells (a), MDCKII and MDCKII-OAT3 cells (b), and CHO-K1 and CHO-K1-OCT2 cells (c). Positive controls: uptake of [<sup>3</sup>H]PAH (1 μM) (d), [<sup>3</sup>H]ES (1 μM) (e) and [<sup>14</sup>C]TEA (1 μM) (f) for OAT1, OAT3 and OCT2, respectively, measured at 7 min. Values shown are mean ± SEM of experiments performed in triplicate. **P < 0.01; *P < 0.05. ES, estrone sulphate; PAH, p-aminohippuric acid; SEM, standard error of the mean; TEA, tetraethylammonium. Unless provided in the caption above, the following copyright applies to the content of this slide: © The Author(s) Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. All rights reserved. For permissions, please article is published and distributed under the terms of the Oxford University Press, Standard Journals Publication Model ( J Antimicrob Chemother, dkz101, The content of this slide may be subject to copyright: please see the slide notes for details.

2 Figure 2. Uptake of relebactam into human OAT4 transiently transfected HEK293 cells. Time-dependent uptake of ... Figure 2. Uptake of relebactam into human OAT4 transiently transfected HEK293 cells. Time-dependent uptake of [<sup>14</sup>C]relebactam (10 μM) into HEK293 and HEK293-OAT4 cells pretreated with (a) or without 5 mM glutaric acid (d). Uptake in the transfected cell line was significantly different from the parental cell line (P < 0.01). Uptake of [<sup>14</sup>C]relebactam (10 μM) into HEK293 and HEK293-OAT4 cells, pretreated with (b) or without 5 mM glutaric acid (e), in the presence and the absence of probenecid (1 mM) at 15 min. Positive controls: uptake of [<sup>3</sup>H]ES (1 μM) into HEK293 and HEK293-OAT4 cells, pretreated with (c) or without 5 mM glutaric acid (f), in the presence and the absence of probenecid (1 mM) at 15 min. Values shown are mean ± SEM of experiments performed in triplicate. ES, estrone sulphate; SEM, standard error of the mean. Unless provided in the caption above, the following copyright applies to the content of this slide: © The Author(s) Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. All rights reserved. For permissions, please article is published and distributed under the terms of the Oxford University Press, Standard Journals Publication Model ( J Antimicrob Chemother, dkz101, The content of this slide may be subject to copyright: please see the slide notes for details.

3 Figure 3. Uptake of [14C]relebactam into human MATE1 and MATE2K stably transfected CHO-K1 and MDCKII cells. ... Figure 3. Uptake of [<sup>14</sup>C]relebactam into human MATE1 and MATE2K stably transfected CHO-K1 and MDCKII cells. Time-dependent uptake of [<sup>14</sup>C]relebactam (10 μM) into CHO-K1 and CHO-K1-MATE1 cells (a), and MDCKII and MDCKII-MATE2K cells (d). Uptake in the transfected cell line was significantly different from that in the parental cell line (P < 0.05). Uptake of [<sup>14</sup>C]relebactam (10 μM) into CHO-K1 and CHO-K1-MATE1 cells in the presence and the absence of control inhibitor quinidine (100 μM) (b), and MDCKII and MDCKII-MATE2K cells in the presence and the absence of control inhibitor pyrimethamine (5 μM) (e) at 20 min. Positive controls: uptake of [<sup>14</sup>C]metformin (5 μM) into CHO-K1 and CHO-K1-MATE1 cells in the presence and the absence of control inhibitor quinidine (100 μM) (c), and MDCKII and MDCKII-MATE2K cells in the presence and the absence of control inhibitor pyrimethamine (5 μM) (f) at 20 min. Values shown are mean ± SEM of experiments performed in triplicate. SEM, standard error of the mean. Unless provided in the caption above, the following copyright applies to the content of this slide: © The Author(s) Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. All rights reserved. For permissions, please article is published and distributed under the terms of the Oxford University Press, Standard Journals Publication Model ( J Antimicrob Chemother, dkz101, The content of this slide may be subject to copyright: please see the slide notes for details.

4 Figure 4. Kinetics of OAT3-mediated uptake of relebactam
Figure 4. Kinetics of OAT3-mediated uptake of relebactam. (a) Concentration-dependent uptake of relebactam into MDCKII ... Figure 4. Kinetics of OAT3-mediated uptake of relebactam. (a) Concentration-dependent uptake of relebactam into MDCKII and MDCKII-OAT3 cells at 5 min. (b) OAT3-mediated uptake of relebactam at 5 min. Values shown are mean ± SEM of experiments performed in triplicate. SEM, standard error of the mean. Unless provided in the caption above, the following copyright applies to the content of this slide: © The Author(s) Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. All rights reserved. For permissions, please article is published and distributed under the terms of the Oxford University Press, Standard Journals Publication Model ( J Antimicrob Chemother, dkz101, The content of this slide may be subject to copyright: please see the slide notes for details.

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