the persistent inhibitory properties of saxagliptin on renal dipeptidyl peptidase-4: studies with hk-2 cells in vitro and normal rats in vivo
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2017
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Abstract
Saxagliptin, a potent and selective DPP-4 inhibitor, exhibits a slow dissociation from DPP-4. We investigated the sustained effects of saxagliptin on renal DPP-4 activity in a washout study using renal tubular (HK-2) cells, and in a pharmacodynamic study using normal rats. In HK-2 cells, the inhibitory potency of saxagliptin on DPP-4 activity persisted after washout, while that of sitagliptin was clearly reduced. In normal rats, a single treatment of saxagliptin or sitagliptin inhibited the plasma DPP-4 activity to similar levels. The inhibitory action of saxagliptin on the renal DPP-4 activity was retained, even when its inhibitory effect on the plasma DPP-4 activity disappeared. However, the inhibitory action of sitagliptin on the renal DPP-4 activity was abolished in correlation with the inhibition of the plasma DPP-4 activity. In situ staining showed that saxagliptin suppressed the DPP-4 activity in both glomerular and tubular cells and its inhibitory effects were significantly higher than those of sitagliptin. Saxagliptin exerted a sustained inhibitory effect on the renal DPP-4 activity in vitro and in vivo. The long binding action of saxagliptin in renal tubular cells might involve the sustained inhibition of renal DPP-4.
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| Authors | ;Masako Uchii;Mariko Sakai;Yuhei Hotta;Satoshi Saeki;Naoya Kimoto;Akinori Hamaguchi;Tetsuya Kitayama;Shunji Kunori |
| Journal | plant direct |
| Year | 2017 |
| DOI |
10.1016/j.jphs.2017.10.003
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