Methylene blue inhibits GABA_A receptors by interaction with GABA binding site.

ABSTRACT: Methylene blue (MB) is commonly used in diagnostic procedures and is also used to treat various medical conditions. Neurological effects of MB have been reported in clinical observations and experimental studies. Thus the modulation of GABA_A receptor function by MB was investigated. Whole-cell GABA-activated currents were recorded from HEK293 cells expressing various GABA_A receptor subunit configurations. MB inhibition of GABA currents was apparent at 3 μM, and it had an IC₅₀ of 31 μM in human α1β2γ2 receptors. The MB action was rapid and reversible. MB inhibition was not mediated via the picrotoxin site, as a mutation (T6'F of the β2 subunit) known to confer resistance to picrotoxin had no effect on MB-induced inhibition. Blockade of GABA_A recep

SUBMITTER: Chen Z 

PROVIDER: S-EPMC5506546 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature