dose of picrotoxin (which is a 1 : 1 molecular complex of picrotin and picrotoxinin
) in the rat (data is not available in the mouse) translates into peak serum levels of [approximately equal to]2 [micro]M of picrotin and picrotoxinin
, which are reached in [approximately equal to]30 min and rapidly decay to baseline levels in [approximately equal to]60 min .
Ticku, "Interactions of pentamethylenetetrazole and tetrazole analogues with the picrotoxinin
site of the benzodiazepine-GABA receptor-ionophore complex," European Journal of Pharmacology, vol.
Ligands for the binding sites of GABA, benzodiazepines, bariburates, picrotoxinin
and loreclezole did not affect the binding of valerenic acid.
Ethanol alleviates suppression in this situation, but isopropyl-bicyclophosphate, a drug that binds to the picrotoxinin
site of the GABA receptor complex, reversed the effects of ethanol on punished responding in a dose-dependent manner.
Betz, "The atypicalM2 segment of the [beta] subunit confers picrotoxinin
resistance to inhibitory glycine receptor channels," The EMBO Journal, vol.