Functional imaging of pharmacological action of SGLT 2 inhibitor ipragliflozin via PET imaging using 11 C‐ MDG

Sodium‐dependent glucose cotransporter 2 ( SGLT 2) is a pharmacological target of type 2 diabetes mellitus. The aim of this study was to noninvasively visualize the pharmacological action of a selective SGLT 2 inhibitor ipragliflozin in the kidney using positron emission tomography ( PET ) imaging with 11 C‐methyl‐ d ‐glucoside ( 11 C‐ MDG ), an SGLT ‐specific radio‐labeled substrate. PET imaging with 11 C‐ MDG in vehicle‐treated rats demonstrated that intravenously injected 11 C‐ MDG substantially accumulated in the renal cortex, reflecting that the compound was reabsorbed by SGLT s. In contrast, ipragliflozin‐treated rats showed significantly lower uptake of 11 C‐ MDG in renal cortex in a dose‐related manner, suggesting that ipragliflozin inhibited the renal reabsorption of 11 C‐ MDG . This method of visualizing the mode of action of an SGLT 2 inhibitor in vivo has demonstrated the drug's mechanism in reducing renal glucose reabsorption in kidney in living animals.