Table 2.
Mutagenesis-based data on critical residues for binding of selected ionophore ligands to TM2 domains of GABA-A receptor subunits (legend as in Fig. 1).
Ligands | References | |||||||
---|---|---|---|---|---|---|---|---|
TM2 residue | P | PTZ | BPH | BL | PC | LA | NP * | |
2 | yes | no | yes | no | yes | (I) | ||
3 | yes | yes | (I) | |||||
6 | yes | yes | yes | yes ** | no | yes | (II) | |
9 | yes | no | no | no | no | (III) | ||
15 | yes | (IV) | ||||||
19 | yes | (IV) |
E.g., dieldrin.
partially sensitive (border of the binding pocket?).
References: I (Gurley et al., 1995; Edwards and Lees, 1997; Jursky et al., 2000; Buhr et al., 2001), II (Sugimoto et al., 2002), III (Tierney et al., 1996; Lindquist et al., 2004), IV (Findlay et al., 2001; Dibas et al., 2002)