Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine.
Article Details
- CitationCopy to clipboard
Khamdang S, Takeda M, Shimoda M, Noshiro R, Narikawa S, Huang XL, Enomoto A, Piyachaturawat P, Endou H
Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine.
J Pharmacol Sci. 2004 Feb;94(2):197-202.
- PubMed ID
- 14978359 [ View in PubMed]
- Abstract
We have elucidated the interactions of human and rat organic anion transporters (hOATs and rOATs) with pravastatin and cimetidine. Pravastatin inhibited hOAT1/rOAT1, hOAT2/rOAT2, hOAT3/rOAT3, and hOAT4. The mode of inhibition was noncompetitive for hOAT1 and hOAT2, whereas it was competitive for hOAT3 and hOAT4. Cimetidine also inhibited hOAT1/rOAT1, hOAT3/rOAT3, and hOAT4. The mode of inhibition was a combination of competitive and noncompetitive manners for hOAT1, whereas it was competitive for hOAT3. The effects of OAT inhibitors on OAT1, OAT2, and OAT3 exhibited some but not so remarkable interspecies differences between humans and rats. In conclusion, we have characterized pravastatin and cimetidine as OAT inhibitors.
DrugBank Data that Cites this Article
- Drug Transporters
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Cilastatin Solute carrier family 22 member 6 IC 50 (nM) 2550000 N/A N/A Details Cilastatin Solute carrier family 22 member 8 IC 50 (nM) 249000 N/A N/A Details Cimetidine Solute carrier family 22 member 11 IC 50 (nM) >2000000 N/A N/A Details Cimetidine Solute carrier family 22 member 6 IC 50 (nM) 492000 N/A N/A Details Cimetidine Solute carrier family 22 member 8 IC 50 (nM) 92400 N/A N/A Details Probenecid Solute carrier family 22 member 11 IC 50 (nM) 25400 N/A N/A Details Probenecid Solute carrier family 22 member 6 IC 50 (nM) 12300 N/A N/A Details Probenecid Solute carrier family 22 member 7 IC 50 (nM) 668000 N/A N/A Details Probenecid Solute carrier family 22 member 8 IC 50 (nM) 4930 N/A N/A Details