Block of voltage-operated sodium channels by 2,6-dimethylphenol, a structural analogue of lidocaine's aromatic tail.

Journal article

1. The structural features that determine the state-dependent interaction of local anaesthetics with voltage-operated sodium channels are still a matter of debate. We have studied the blockade of sodium channels by 2,6-dimethylphenol, a phenol derivative which resembles the aromatic tail of lidocaine, etidocaine, and bupivacaine. 2. The effects of 2,6-dimethylphenol were studied on heterologously (HEK 293) expressed rat neuronal (rat brain IIA) and human skeletal muscle (hSkM1) sodium channel...

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Authors: Haeseler, G; Bufler, J; Merken, S; Dengler, R; Aronson, J

• Publication status: Published
• Journal: British journal of pharmacology
• Volume: 137
• Issue: 2
• Pages: 285-293
• Publication date: 2002-09-01
• DOI: 10.1038/sj.bjp.0704854
• EISSN: 1476-5381
• ISSN: 0007-1188
• Language: English
• Keywords: Sodium Channel Blockers; Xylenes; Receptors, GABA-A; Humans; Cell Line; Structure-Activity Relationship; Lidocaine