ROD-188 is a sedative drug that was structurally derived from the GABAAantagonistbicuculline by a team at Roche. Unlike bicuculline, ROD-188 acts as an agonist at GABAA receptors, being a positive allosteric modulator acting at a novel binding site distinct from those of benzodiazepines, barbiturates or muscimol, with its strongest effect produced at the α6β2γ2 subtype of the GABAA receptor. ROD-188 is one of a number of related compounds acting at this novel modulatory site, some of which also act at benzodiazepine receptors.
^US Patent 6649626 N-substituted 1-(lactone) isoquinolones for treating nervous disorders
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