Article
Benzodiazepines modulate GABAA receptors by regulating the preactivation step after GABA binding.
The Journal of neuroscience : the official journal of the Society for Neuroscience - 25 Apr 2012
Gielen Marc C, Lumb Michael J, Smart Trevor G
Abstract excerpt
GABA(A) receptors (GABA(A)Rs) composed of αβγ subunits are allosterically modulated by the benzodiazepines (BDZs). Agonists at the BDZ binding site potentiate submaximal GABA responses by increasing the apparent affinity of GABA(A)Rs for GABA. Although BDZs were initially thought to affect the binding of GABA agonists, recent studies suggest an effect on receptor gating; however, the involvement of preactivation...
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