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Astemizole

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 Astemizole 26.4 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE1 Wittwer, 2013
ABCB1 MDR1, P-gp Astemizole 1.3 Calcein AM MDR1 expressing LLC-PK1 cells Schwab, 2003
mouse_Abcb1a Mdr, Pgp, Pgy, Mdr3, P-gp, Abcb4, Mdr1a Astemizole 1.3 Calcein AM Mouse mdr1a expressing LLC-PK1 cells Schwab, 2003
mouse_Abcb1b mdr, Mdr1, Pgy1, Abcb1, Mdr1b, Pgy-1 Astemizole 1.7 Calcein AM Mouse mdr1b expressing LLC-PK1 cells Schwab, 2003
ABCB1 MDR1, P-gp Astemizole 2.73 Digoxin MDCKII-MDR1 Keogh, 2006
ABCC2 MRP2, cMOAT Astemizole >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Astemizole >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC4 MRP4 Astemizole >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCB11 BSEP Astemizole 58.8 Taurocholate Sf9 cell membrane vesicles Morgan, 2013

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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