Abstract：
:The interactions of sulfonylureas and a novel anti-diabetic drug, nateglinide, with rat renal organic anion transporter (rOAT1) expressed in Xenopus laevis oocytes were studied. Uptake of p-aminohippurate via rOAT1 was markedly inhibited by glibenclamide and nateglinide, and moderately by chlorpropamide and tolbutamide. The inhibition constant values (K(i)) for chlorpropamide, glibenclamide, tolbutamide and nateglinide were 39.5, 1.6, 55.5 and 9.2 microM, respectively. Kinetic analysis showed that the inhibition of p-aminohippurate uptake by glibenclamide was competitive. Sulfonylureas examined and nateglinide did not show a trans-stimulation effect on [14C]p-aminohippurate efflux from rOAT1-expressing oocytes. There was no stimulation of [3H]glibenclamide uptake via rOAT1. These findings suggested that sulfonylureas and nateglinide interact with rOAT1, but these drugs are not translocated via the transporter.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Uwai Y,Saito H,Hashimoto Y,Inui Kdoi
10.1016/s0014-2999(00)00324-1keywords:
subject
Has Abstractpub_date
2000-06-16 00:00:00pages
193-7issue
2eissn
0014-2999issn
1879-0712pii
S0014299900003241journal_volume
398pub_type
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