Decreased agonist sensitivity of human GABAA receptors by an amino acid variant, isoleucine to valine, in the α1 subunit
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Volatile anesthetic effects on isolated GABA synapses and extrasynaptic receptors
2011, NeuropharmacologyCitation Excerpt :Previous molecular biological studies identified the binding site of volatile anesthetics on GABAA receptors (Mihic et al., 1997; Krasowski et al., 1998; Koltchine et al., 1999; Siegwart et al., 2003), and indicated that the subunit components of GABAA receptor were important for volatile anesthetics. The GABAA receptor is composed of pentamer subunits, and the subunit composition is important to determine their subcellular distribution patterns as well as pharmacological properties (Westh-Hansen et al., 1997a, 1997b; Belelli et al., 1999; Korpi et al., 2002; Mohler et al., 2002). GABAA receptors containing α5-subunit involved in tonic inhibitory conductance (Caraiscos et al., 2004a) are highly sensitive to low concentrations of isoflurane (Caraiscos et al., 2004b).
Exploring ligand recognition and ion flow in comparative models of the human GABA type A receptor
2007, Journal of Molecular Graphics and ModellingMolecular modelling of the GABA<inf>A</inf> ion channel protein
2007, Journal of Molecular Graphics and ModellingFour amino acids in the α subunits determine the γ-aminobutyric acid sensitivities of GABA<inf>A</inf> receptor subtypes
2004, Journal of Biological ChemistryCitation Excerpt :However, it may contribute to the low affinity binding site, which has been interpreted as a conformational variant of the high affinity site (32). A previous study (33) showed that exchange of the isoleucine belonging to the α1ITED motif by valine decreases both the sensitivity to GABA and the affinity of agonist GABAA receptor ligands in mutant α1β2γ2 receptors. The discrepancies between these data and our results may be caused by the nature of the introduced amino acid.
On the Benzodiazepine Binding Pocket in GABA<inf>A</inf> Receptors
2004, Journal of Biological ChemistryThe GABA<inf>A</inf> receptor α<inf>1</inf> subunit Pro<sup>174</sup>-Asp<sup>191</sup> segment is involved in GABA binding and channel gating
2003, Journal of Biological Chemistry