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Title: Interactions of Human- and Rat-Organic Anion Transporters with Pravastatin and Cimetidine
Authors: Suparat Khamdang
Michio Takeda
Minoru Shimoda
Rie Noshiro
Shinichi Narikawa
Xiu Lin Huang
Atsushi Enomoto
Pawinee Piyachaturawat
Hitoshi Endou
Kyorin University School of Medicine
Mahidol University
Tokyo University of Agriculture and Technology
Fuji Biomedix Co Ltd
Keywords: Pharmacology, Toxicology and Pharmaceutics
Issue Date: 1-Feb-2004
Citation: Journal of Pharmacological Sciences. Vol.94, No.2 (2004), 197-202
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.
ISSN: 13478613
Appears in Collections:Scopus 2001-2005

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