Picrodendrins, a New Group of Picrotoxane Terpenoids: Structure-Activity Profile of Action at the GABA<sub>A</sub>Receptor-coupled Picrotoxinin Binding Site in Rat Brain

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  • Picrodendrins, a New Group of Picrotoxane Terpenoids: Structure-Activity Profile of Action at the GABAA Receptor-coupled Picrotoxinin Binding Site in Rat Brain.

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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. 0μM. 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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