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Title: Transport properties of nonsteroidal anti-inflammatory drugs by organic anion transporter 1 expressed in Xenopus laevis oocytes
Authors: Nopporn Apiwattanakul
Takashi Sekine
Arthit Chairoungdua
Yoshikatsu Kanai
Noriko Nakajima
Samaisukh Sophasan
Hitoshi Endou
Kyorin University School of Medicine
Mahidol University
Keywords: Biochemistry, Genetics and Molecular Biology;Pharmacology, Toxicology and Pharmaceutics
Issue Date: 18-May-1999
Citation: Molecular Pharmacology. Vol.55, No.5 (1999), 847-854
Abstract: Organic anion transporter 1 (OAT1) is the para-aminohippurate (PAH) transporter in the basolateral membrane of the proximal tubule. The present study investigated whether or not nonsteroidal anti-inflammatory drugs (NSAIDs) are transported by OAT1. All of the NSAIDs tested inhibited [14C]PAH uptake via OAT1 expressed in Xenopus laevis oocytes. Ibuprofen, indomethacin, salicylurate, and naproxen showed the strongest potency to inhibit [14C]PAH uptake (K(i) ~ 2-10 μM); acetylsalicylate, salicylate, and phenacetin exhibited moderate potency (K(i) ~ 300-400 μM), and acetaminophen (paracetamol) exhibited the weakest inhibitory potency (K(i) ~ 2 mM). Radiolabeled acetylsalicylate, salicylate, and indomethacin were taken up by OAT1 and the uptake rate of these three NSAIDs was enhanced by the outwardly directed dicarboxylate gradient. The efflux of the preloaded [14C]PAH from the oocytes via OAT1 was trans-stimulated by PAH and glutarate added to the media. The addition of salicylate acetylsalicylate, or salicylurate into the media also trans-stimulated the efflux of PAH, whereas indomethacin did not. The present study indicates that OAT1 is responsible for the renal uptake and secretion of NSAIDs.
ISSN: 0026895X
Appears in Collections:Scopus 1991-2000

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