Förstera B , Castro PA , Moraga-Cid G , Aguayo LG .

R01 AA015150 NIAAA NIH HHS

Figure 1. Acute effects of ethanol on GABAergic transmission. The scheme illustrates several potential acute pre and postsynaptic sites for the effects of ethanol on GABAergic neurotransmission. Reported changes on the release of presynaptic GABA might be mediated by changes on calcium release from intracellular calcium stores (ICS) following activation of G-protein coupled receptors (GPCR) or phosphorylation by protein kinase A (PKA) and C (PKC). Changes on the activation of GPCR, such as GABABR, could affect GABA release and alter the tonic Cl− current associated to non-synaptic GABAAR δ containing receptors through spillover of synaptically released GABA. At postsynaptic domains, acute low ethanol concentrations of alcohol appear to modulate primarily non-synaptic GABAAR (see thicker arrow) by a mechanism that might involve direct binding to the general anesthetics site of action or by intracellular signaling pathways, G protein, PKC and PKA or calcium release. The scheme also shows representative traces of a phasic current, activated by synaptic receptors, and a sustained small desensitizing tonic current, mediated by non synaptic receptors.

Figure 2. Sites of action for allosteric modulation of GABAAR. Schematic illustration of the overall architecture and putative modulatory sites of action on GABAAR. The model is based in the X-ray structure of GABAAR β3 subunit (PDB: 4COF; see Miller and Aricescu, 2014). (A) Upper view of the putative subunit stoichiometry and global architecture of the αβγ/δ GABAAR. The cartoon shows the binding sites for GABA and Benzodiazepine (BDZ). (B) Lateral view showing the suggested binding sites for ethanol (red spheres) and Picrotoxin (blue spheres). This crystal structure lacks the intracellular domain between TM3 and TM4 which was shown to be critical for the modulation of the receptor by G protein and phosphorylation pathways.

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