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Article

Stereoselective block of hERG channel by (S)-methadone and QT interval prolongation in CYP2B6 slow metabolizers.

Clinical pharmacology and therapeutics - 1 May 2007

Eap C B, Crettol S, Rougier J-S, Schläpfer J, Sintra Grilo L, Déglon J-J, Besson J, Croquette-Krokar M, Carrupt P-A, Abriel H

Abstract excerpt

Methadone inhibits the cardiac potassium channel hERG and can cause a prolonged QT interval. Methadone is chiral but its therapeutic activity is mainly due to (R)-methadone. Whole-cell patch-clamp experiments using cells expressing hERG showed that (S)-methadone blocked the hERG current 3.5-fold more potently than (R)-methadone (IC50s (half-maximal inhibitory concentrations) at 37 degrees C: 2 and 7 microM). As...

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Share to Cytochrome P-450 CYP2B6

Methodology Data sources Editorial policy Privacy Delete account & data About Contact Helena Bioinformatics

Share to ERG1 Potassium Channel

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Source

Identifiers

PMID: 17329992
DOI: 10.1038/sj.clpt.6100120

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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