Seven out of 20 assayed picrotoxane terpenoids inhibited specific binding of [35S]t-butylbicyclophosphorothionate to rat brain membranes, with IC50 values of 0.0075–6.0 μm. Picrodendrin Q was identified as the most potent compound, being about 27-fold more potent than picrotoxinin. The high activity of picrodendrins A, M, and Q suggests the significance of the spiro α-ethylidene γ-lactone moiety for the interaction of picrodendrins with the GABAA receptor-coupled picrotoxinin binding site.
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Ozoe et al. (1994) studied this question.
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