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Naloxone

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

No substrate information.


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In Vitro Inhibitors

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Transporter Synonyms Inhibitor IC50 (μM) Ki (μM) Substrate used Cell System Reference
SLC47A1 MATE1 Naloxone 24.1 1-methyl-4-phenylpyridinium (MPP+) CHO-MATE1 Astorga, 2012
SLC47A2 MATE2K Naloxone 43.2 1-methyl-4-phenylpyridinium (MPP+) CHO-MATE2K Astorga, 2012
SLC22A2 OCT2 Naloxone 235.7 1-methyl-4-phenylpyridinium (MPP+) CHO-OCT2 Sandoval, 2018
SLC22A2 OCT2 Naloxone 20.3 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) CHO-OCT2 Sandoval, 2018
ABCC2 MRP2, cMOAT Naloxone >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Naloxone >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC4 MRP4 Naloxone >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
SLC22A2 OCT2 Naloxone 29.5 Metformin CHO-OCT2 Sandoval, 2018
SLC22A2 OCT2 Naloxone 55.1 NBD-MTMA CHO-OCT2 Sandoval, 2018
ABCB11 BSEP Naloxone >133 Taurocholate Sf9 cell membrane vesicles Morgan, 2013
SLC22A2 OCT2 Naloxone 67.3 Tetraethylammonium CHO-OCT2 Sandoval, 2018

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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