The Benzodiazepine Site Of Gabaa Receptors

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GABAA receptors are transmembrane proteins that are assembled from subunits into a pentameric structure forming an ion-channel through which the influx of chloride ions is regulated. In addition to the binding site for the endogenous agonist GABA, the GABAA receptors have binding sites for compounds that allosterically modify the chloride channel gating of GABA. The most well-known class of such compounds is the BZDs and the binding site for this class of compounds has been named the BZD site. The pharmacological effects of the BZDs (anxiolytic, anticonvulsant, muscle relaxant, and sedative-hypnotic) make them the most important GABAA receptor-modulating drugs in clinical use.

In addition to the BZD class of compounds, it has been shown that many other classes of compounds bind to the BZD site and a pharmacophore model including several classes of compounds have been developed (see Further Readings). In addition, naturally occurring and synthetic derivatives of flavones have also been shown to bind to the BZD site. The flavone class of compounds is the starting point for the case study described in this chapter.

At present there is no experimentally determined 3D structure for any of the subtypes of the GABAA receptor. Thus, in the computational part of a drug discovery project dealing with this class of receptors, the use of ligand-based drug design methods is the only alternative. For a more detailed discussion on GABAA receptors and their ligands, see Chapter 15 and the use of GABA ligands as hypnotics is discussed in Chapter 20.

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