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Studies on the mechanisms of action of picrotoxin, quercetin and pregnanolone at the GABAρ1 receptor
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Studies on the mechanisms of action of picrotoxin, quercetin and pregnanolone at the GABAρ1 receptor
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Journal Article
Studies on the mechanisms of action of picrotoxin, quercetin and pregnanolone at the GABAρ1 receptor
2004
Overview
The mechanisms of action of antagonists of the γ‐aminobutyric acid C (GABAC) receptor picrotoxin, quercetin and pregnanolone were studied. Ionic currents (chloride), mediated through human homomeric GABAρ1 receptors expressed in Xenopus oocytes, were recorded by two‐electrode voltage clamp. Dose–response (D–R) curves and kinetic measurements of GABAρ1 currents were carried out in the presence or absence of antagonists. Use‐dependent actions were also evaluated. Picrotoxin, quercetin and pregnanolone exerted noncompetitive actions. IC50 values measured at the EC50 for GABA (1 μM) were as follows: picrotoxin 0.6±0.1 μM (Hill coefficient n=1.0±0.2); quercetin 4.4±0.4 μM (n=1.5±0.2); pregnanolone 2.1±0.5 μM (n=0.8±0.1). These antagonists produced changes only in the slope of the linear current–voltage relationships, which was indicative of voltage‐independent effects. The effect of picrotoxin on GABAρ1 currents was use‐dependent, strongly relied on agonist concentration and showed a slow onset and offset. The mechanism was compatible with an allosteric inhibition and receptor activation was a prerequisite for antagonism. The effect of quercetin was use‐independent, showed relatively fast onset and offset, and resulted in a slowed time course of the GABA‐evoked currents. The effect of pregnanolone was use‐independent, presented fast onset and a very slow washout, and did not affect current activation. All the antagonists accelerated the time course of deactivation of the GABAρ1 currents. British Journal of Pharmacology (2004) 141, 717–727. doi:10.1038/sj.bjp.0705657
Publisher
Blackwell Publishing Ltd,Nature Publishing
