Methadone inhibits rhodamine123 transport in Caco-2 cells.
Article Details
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Stormer E, Perloff MD, von Moltke LL, Greenblatt DJ
Methadone inhibits rhodamine123 transport in Caco-2 cells.
Drug Metab Dispos. 2001 Jul;29(7):954-6.
- PubMed ID
- 11408360 [ View in PubMed]
- Abstract
This study investigated the effects of racemic methadone (MET) on P-glycoprotein (P-gp) activity in cell culture. MET showed no differential rates of passage between the basolateral to apical (B to A) and apical to basolateral (A to B) direction across Caco-2 cell monolayers in a transwell system. MET transport in either direction was not importantly influenced by the P-gp inhibitor verapamil. However, MET was a potent inhibitor (IC(50) = 7.5 microM) of rhodamine123 B to A transport across Caco-2 cell monolayers, causing a reduction to 25% of control at 100 microM MET. In this model of Caco-2 monolayers, rates of MET passage between B to A and A to B directions could not be distinguished. However, MET can inhibit P-gp activity at intraluminal concentrations that might be achieved clinically. This may lead to increased bioavailability of coadministered compounds.
DrugBank Data that Cites this Article
- Drug Transporters
Drug Transporter Kind Organism Pharmacological Action Actions Methadone P-glycoprotein 1 Protein Humans UnknownInhibitorDetails - Binding Properties
Drug Target Property Measurement pH Temperature (°C) Methadone P-glycoprotein 1 IC 50 (nM) 7500 N/A N/A Details