NDLI: Interaction of Ibuprofen and Other Structurally Related NSAIDs with the Sodium-Coupled Monocarboxylate Transporter SMCT1 (SLC5A8)

Content Provider	Springer Nature Link
Author	Itagaki, Shirou Gopal, Elangovan Zhuang, Lina Fei, You Jun Miyauchi, Seiji Prasad, Puttur D. Ganapathy, Vadivel
Copyright Year	2006
Abstract	Sodium-coupled monocarboxylate transporter 1 (SMCT1) is a Na$^{+}$-coupled transporter for monocarboxylates. Many nonsteroidal anti-inflammatory drugs (NSAIDs) are monocarboxylates. Therefore, we investigated the interaction of these drugs with human SMCT1 (hSMCT1).We expressed hSMCT1 in a mammalian cell line and in Xenopus laevis oocytes and used the uptake of nicotinate and propionate-induced currents to monitor its transport function, respectively. We also used [$^{14}$C]-nicotinate and [$^{3}$H]-ibuprofen for direct measurements of uptake in oocytes.In mammalian cells, hSMCT1-mediated nicotinate uptake was inhibited by ibuprofen and other structurally related NSAIDs. The inhibition was Na$^{+}$ dependent. With ibuprofen, the concentration necessary for 50% inhibition was 64 ± 16 μM. In oocytes, the transport function of hSMCT1 was associated with inward currents in the presence of propionate. Under identical conditions, ibuprofen and other structurally related NSAIDs failed to induce inward currents. However, these compounds blocked propionate-induced currents. With ibuprofen, the blockade was dose dependent, Na$^{+}$ dependent, and competitive. However, there was no uptake of [$^{3}$H]-ibuprofen into oocytes expressing hSMCT1, although the uptake of [$^{14}$C]-nicotinate was demonstrable under identical conditions.Ibuprofen and other structurally related NSAIDs interact with hSMCT1 as blockers of its transport function rather than as its transportable substrates.
Starting Page	1209
Ending Page	1216
Page Count	8
File Format	PDF
ISSN	07248741
Journal	Pharmaceutical Research
Volume Number	23
Issue Number	6
e-ISSN	1573904X
Language	English
Publisher	Springer-Verlag
Publisher Date	2006-06-01
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	blocker electrophysiology ibuprofen sodium dependence SMCT1 Pharmacology/Toxicology Pharmacy Biochemistry Medical Law Biomedical Engineering
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology Molecular Medicine Pharmacology (medical) Biotechnology Pharmaceutical Science

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