Table 1.
Pharmacological properties of neuronal and oligodendroglial GABAARs.
| Neurons | |||
|---|---|---|---|
| Drug | Synaptic (αxβxγ2) | Extrasynaptic (αxβxδ) | Oligodendroglial cells |
| GABA | Low EC50 1–30 μM | Low EC50 0.5 nM–10 μM | High EC50 70–100 μM |
| (Gibbs et al., 1996; Baur and Sigel, 2003; Mortensen et al., 2012) | (Brown et al., 2002; Wallner et al., 2003; Mortensen et al., 2012) | (Williamson et al., 1998; Arellano et al., 2016) | |
| THIP | No effect | + | No effect |
| (Mortensen et al., 2010) | (Brown et al., 2002; Meera et al., 2011) | (Arellano et al., 2016) | |
| Zn2+ | Low or No effect | − | − |
| (Hosie et al., 2003) | (Carver et al., 2016) | (Bronstein et al., 1998; Passlick et al., 2013; Arellano et al., 2016) | |
| β-CCB | − or No effect | No effect | + |
| (Peña et al., 1986; Cisneros-Mejorado et al., 2020) | (Jiménez-González et al., 2011) | (Arellano et al., 2016; Cisneros-Mejorado et al., 2020) | |
| DMCM | − | − | − |
| (Peña et al., 1986) | (Brown et al., 2002) | (von Blankenfeld et al., 1991; Arellano et al., 2016) | |
| Diazepam | + | No effect | + |
| (Walters et al., 2000; Goodkin and Kapur, 2009) | (Goodkin and Kapur, 2009) | (von Blankenfeld et al., 1991; Passlick et al., 2013; Arellano et al., 2016) | |
| Indiplon | + | No effect | No effect |
| (Petroski et al., 2006) | (Michelsen et al., 2007) | (Arellano et al., 2016) | |
| Flunitrazepam | + | No effect | + |
| (Goodkin and Kapur, 2009) | (Goodkin and Kapur, 2009) | (von Blankenfeld et al., 1991; Arellano et al., 2016) | |
| Loreclezole | +* | +* | + |
| (Wingrove et al., 1994) | (Wingrove et al., 1994) | (Arellano et al., 2016) | |
(+) Potentiator/agonist; (−) Inhibitor; (*) β2 or β3 subunit required.