INT95101

Context Info Confidence 0.48 First Reported 2001 Last Reported 2008 Negated 1 Speculated 1 Reported most in Abstract Documents 6 Total Number 7 Disease Relevance 0.75 Pain Relevance 5.07

transmembrane transporter activity (SLC22A8) plasma membrane (SLC22A8) transmembrane transport (SLC22A8)

Anatomy Link Frequency bile 1 oocytes 1 SLC22A8 (Homo sapiens)

Pain Link Frequency Relevance Heat Paracetamol 3 100.00 methotrexate 53 99.76 cINOD 41 99.76 Bile 1 94.32 diclofenac 1 89.20 aspirin 1 82.48

Disease Link Frequency Relevance Heat INFLAMMATION 9 96.96 Disease 2 95.36 Adverse Drug Reaction 1 5.00

Sentences Mentioned In

Key:

Protein

Mutation

Event

Anatomy

Negation

Speculation

Pain term

Disease term

On the other hand, drugs that were not substrates of hOAT3, such as acetaminophen, did not interact with methotrexate.

hOAT3 Neg (not) Binding (interact) of associated with paracetamol and methotrexate

1) Confidence 0.48 Published 2008 Journal Eur. J. Pharmacol. Section Abstract Doc Link 18789319 Disease Relevance 0.13 Pain Relevance 1.67

Estrone sulfate did not show any trans-stimulatory effects on either influx or efflux of [(3)H]estrone sulfate via hOAT3. hOAT3 interacted with chemically heterogeneous anionic compounds, such as nonsteroidal anti-inflammatory drugs, diuretics, sulfobromophthalein, penicillin G, bile salts and tetraethyl ammonium bromide.

hOAT3 Binding (interacted) of in bile associated with bile, inflammation and cinod

2) Confidence 0.32 Published 2001 Journal Mol. Pharmacol. Section Abstract Doc Link 11306713 Disease Relevance 0.10 Pain Relevance 0.19

Methotrexate-loxoprofen interaction: involvement of human organic anion transporters hOAT1 and hOAT3.

hOAT3 Binding (interaction) of associated with methotrexate

3) Confidence 0.31 Published 2004 Journal Drug Metab. Pharmacokinet. Section Title Doc Link 15548848 Disease Relevance 0.18 Pain Relevance 0.60

In this study, we examined the drug interaction via hOAT1 and hOAT3, using Xenopus laevis oocytes. hOAT1 and hOAT3 mediated the methotrexate transport with low affinity (K(m) of 724.0 muM) and high affinity (K(m) of 17.2 muM), respectively.

hOAT3 Spec (examined) Binding (interaction) of in oocytes associated with methotrexate

4) Confidence 0.29 Published 2004 Journal Drug Metab. Pharmacokinet. Section Abstract Doc Link 15548848 Disease Relevance 0.19 Pain Relevance 0.57

Furthermore, it was predicted that hOAT3 is the site of drug interactions between methotrexate and salicylate, phenylbutazone, indomethacin, and probenecid in vivo.

hOAT3 Binding (interactions) of associated with methotrexate

5) Confidence 0.20 Published 2002 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 12130730 Disease Relevance 0 Pain Relevance 0.47

In addition, hOAT1, hOAT3, and hOAT4 are the sites of drug interactions between methotrexate and NSAIDs, probenecid, and penicillin G.

hOAT3 Binding (interactions) of associated with cinod and methotrexate

6) Confidence 0.20 Published 2002 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 12130730 Disease Relevance 0 Pain Relevance 0.48

By comparing the IC(50) values of NSAIDs for hOATs, it was found that hOAT1 and hOAT3 exhibited higher affinity interactions with NSAIDs than did hOAT2 and hOAT4.

hOAT3 Binding (interactions) of associated with cinod

7) Confidence 0.08 Published 2002 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 12388633 Disease Relevance 0.16 Pain Relevance 1.10

General Comments

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