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Article

The low-potency, voltage-dependent HERG blocker propafenone--molecular determinants and drug trapping.

Molecular pharmacology - 1 Nov 2004

Witchel Harry J, Dempsey Christopher E, Sessions Richard B, Perry Matthew, Milnes James T, Hancox Jules C, Mitcheson John S

Abstract excerpt

The molecular determinants of high-affinity human ether-a-go-go-related gene (HERG) potassium channel blockade by methanesulfonanilides include two aromatic residues (Phe656 and Tyr652) on the inner helices (S6) and residues on the pore helices that face into the inner cavity, but determinants for lower-affinity HERG blockers may be different. In this study, alanine-substituted HERG channel mutants of inner...

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Identifiers

PMID: 15308760
DOI: 10.1124/mol.104.001743

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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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