Effect of ipragliflozin, an SGLT2 inhibitor, on progression of diabetic microvascular complications in spontaneously diabetic Torii fatty rats

Takakura, Shoji; Toyoshi, Tohru; Hayashizaki, Yuka; Takasu, Toshiyuki

doi:10.1016/j.lfs.2016.01.042

Cited by 52 publications

(52 citation statements)

References 39 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In addition, some observational studies found that use of thiazolidinediones was associated with increased risk of diabetic macular edema (DME) . In contrast, a pre‐clinical study showed that control of hyperglycaemia with ipragliflozin, a sodium‐glucose co‐transporter 2 (SGLT2) inhibitor, slowed the progression of retinopathy, nephropathy and neuropathy …”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Comparisons of diabetic retinopathy events associated with glucose‐lowering drugs in patients with type 2 diabetes mellitus: A network meta‐analysis

Tang

Zhao

et al. 2018

Diabetes Obesity Metabolism

View full text Add to dashboard Cite

show abstract

Section: Introductionmentioning

confidence: 99%

“…9,10 In contrast, a pre-clinical study showed that control of hyperglycaemia with ipragliflozin, a sodium-glucose co-transporter 2 (SGLT2) inhibitor, slowed the progression of retinopathy, nephropathy and neuropathy. 11 Huilin Tang and Guangyao Li contributed equally to this work, and are listed as co-first authors. photocoagulation.…”

Section: Introductionmentioning

confidence: 99%

Comparisons of diabetic retinopathy events associated with glucose‐lowering drugs in patients with type 2 diabetes mellitus: A network meta‐analysis

Tang

Zhao

et al. 2018

Diabetes Obesity Metabolism

View full text Add to dashboard Cite

show abstract

“…The effectiveness of SGLT2 inhibitors in decreasing blood glucose in diabetic patients has been proven in phase I to III clinical trials[6, 7]. Some animal experiments also suggested that SGLT2 inhibitors were effective in preventing diabetic vascular complications including diabetic nephropathy[8, 9]. However, the increased urinary glucose excretion associated with SGLT2 inhibition would result in an osmotic diuresis that could be associated with a reduction in intravascular volume and electrolyte disorder.…”

Section: Introductionmentioning

confidence: 99%

Effect of Dapagliflozin Treatment on Fluid and Electrolyte Balance in Diabetic Rats

Chen

LaRocque

Efe

et al. 2016

The American Journal of the Medical Sciences

View full text Add to dashboard Cite

Aim This study evaluates the effect of dapagliflozin, a SGLT2 inhibitor, on fluid/electrolyte balance and its effect on urea transporter-A1 (UT-A1), aquaporin-2 (AQP2) and Na-K-2Cl cotransporter (NKCC2) protein abundance in diabetic rats. Methods Diabetes mellitus was induced by injection of streptozotocin into the tail vein. Serum Na+, K+, Cl− concentration, urine Na+, K+, Cl− excretion, blood glucose, urine glucose excretion, urine volume, urine osmolality and urine urea excretion were analyzed after the administration of dapagliflozin. UT-A1, AQP2 and NKCC2 proteins were detected by western blot. Results Dapagliflozin treatment decreased blood glucose by 38% at day 7 and 47% at day 14 and increased the urinary glucose excretion rate compared with the untreated diabetic animals. Increased 24-h urine volume, decreased urine osmolality and hyponatremia, hypokalemia and hypochloremia observed in diabetic rats were attenuated by dapagliflozin treatment. Western analysis showed that UT-A1, AQP2 and NKCC2 proteins are up-regulated in DM rats over control rats; dapagliflozin treatment results in a further increase in IM tip UT-A1 protein abundance by 42% at day 7 and 46% at day 14, but it did not affect the DM-induced up-regulation of AQP2 and NKCC2 proteins. Conclusion Dapagliflozin treatment augmented the compensatory changes in medullary transport proteins in DM. These changes will tend to conserve solute and water even with persistent glycosuria. Therefore, diabetic rats treated with dapagliflozin have a mild osmotic diuresis compared to non-diabetic animals, but this does not result in an electrolyte disorder or significant volume depletion.

show abstract

“…, ; Takakura et al. ). However, in this study, both plasma concentration of ipragliflozin and enhanced urinary glucose excretion following single oral administration of ipragliflozin were determined.…”

Section: Discussionmentioning

confidence: 99%

Functional imaging of pharmacological action of SGLT2 inhibitor ipragliflozin via PET imaging using ¹¹C‐MDG

Mitsuoka

Hayashizaki

Murakami

et al. 2016

Pharmacology Res & Perspec

Self Cite

View full text Add to dashboard Cite

Sodium‐dependent glucose cotransporter 2 (SGLT2) is a pharmacological target of type 2 diabetes mellitus. The aim of this study was to noninvasively visualize the pharmacological action of a selective SGLT2 inhibitor ipragliflozin in the kidney using positron emission tomography (PET) imaging with 11C‐methyl‐d‐glucoside (11C‐MDG), an SGLT‐specific radio‐labeled substrate. PET imaging with 11C‐MDG in vehicle‐treated rats demonstrated that intravenously injected 11C‐MDG substantially accumulated in the renal cortex, reflecting that the compound was reabsorbed by SGLTs. In contrast, ipragliflozin‐treated rats showed significantly lower uptake of 11C‐MDG in renal cortex in a dose‐related manner, suggesting that ipragliflozin inhibited the renal reabsorption of 11C‐MDG. This method of visualizing the mode of action of an SGLT2 inhibitor in vivo has demonstrated the drug's mechanism in reducing renal glucose reabsorption in kidney in living animals.

show abstract

Effect of ipragliflozin, an SGLT2 inhibitor, on progression of diabetic microvascular complications in spontaneously diabetic Torii fatty rats

Cited by 52 publications

References 39 publications

Comparisons of diabetic retinopathy events associated with glucose‐lowering drugs in patients with type 2 diabetes mellitus: A network meta‐analysis

Comparisons of diabetic retinopathy events associated with glucose‐lowering drugs in patients with type 2 diabetes mellitus: A network meta‐analysis

Effect of Dapagliflozin Treatment on Fluid and Electrolyte Balance in Diabetic Rats

Functional imaging of pharmacological action of SGLT2 inhibitor ipragliflozin via PET imaging using ¹¹C‐MDG

Contact Info

Product

Resources

About

Effect of ipragliflozin, an SGLT2 inhibitor, on progression of diabetic microvascular complications in spontaneously diabetic Torii fatty rats

Cited by 52 publications

References 39 publications

Comparisons of diabetic retinopathy events associated with glucose‐lowering drugs in patients with type 2 diabetes mellitus: A network meta‐analysis

Comparisons of diabetic retinopathy events associated with glucose‐lowering drugs in patients with type 2 diabetes mellitus: A network meta‐analysis

Effect of Dapagliflozin Treatment on Fluid and Electrolyte Balance in Diabetic Rats

Functional imaging of pharmacological action of SGLT2 inhibitor ipragliflozin via PET imaging using 11C‐MDG

Contact Info

Product

Resources

About

Functional imaging of pharmacological action of SGLT2 inhibitor ipragliflozin via PET imaging using ¹¹C‐MDG