Influence of CGS 8216 on some acute effects of ethanol.

The central pharmacological effects of ethanol are well known and resemble those of the benzodiazepines (BZD). In addition BZD may interact with ethanol, resulting in enhanced cerebral depression. Ro 15-4513, BZD inverse agonist, potentially antagonizes a lot of effects of ethanol but not all. In our study, another BZD inverse agonist, CGS 8216, reverses the hypnotic effect of ethanol and hypoactivity in mice and rats. CGS 8216 increased also ethanol's locomotor stimulation in mice. This supports the hypothesis that some effects of ethanol are mediated by the GABA-BZD-chloride channel receptor complex. Our behavioural experiments described in this report suggest that CGS 8216, like Ro 15-4513, may act on the alpha-6 subunit of this receptor complex.