Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues

David J. Behm, John J. McAtee, Jason W. Dodson, Michael J. Neeb, Harvey E. Fries, C.A. Evans, K D Hoffman, Stephen Harrison, Jin-Huei Lai, Chang‐Fu Wu,

British Journal of Pharmacology · 2008 · 31 citations · 38 references

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Abstract

Collectively, such findings suggest that caution should be taken when interpreting data generated using palosuran. The loss of UT affinity/activity observed in intact cells and tissues cf. membranes offers a potential explanation for the disappointing clinical efficacy reported with palosuran in diabetic nephropathy patients. As such, the (patho)physiological significance of U-II in diabetic renal dysfunction remains uncertain.

References

38