Tarek Z. Deeb, Yasuko Nakamura, Greg D. Frost, Paul A. Davies and Stephen J. Moss Disrupted Cl− homeostasis contributes to reductions in the inhibitory efficacy of diazepam during hyperexcited states European Journal of Neuroscience 38
Several commonly used therapeutic drugs target Cl− permeable GABAA receptors. In the current study, hyperexcitability caused by glutamate or by inhibition of KCC2 rapidly increased Cl− levels inside neurons. This buildup reduced the ability of diazepam to suppress neuronal activity. However, the same conditions did not affect inhibition by propofol. Changes in intracellular Cl− could therefore selectively impact the therapeutic efficacy of GABAA modulators during specific pathological states.
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