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Piper methysticum

Evidence for kavain binding sites in the brain

Kavapyrones, compounds isolated from Piper methysticum, have been shown to possess pharmacological properties, including anxiolytic, anticonvulsive, and muscle-relaxant effects. ()-kavain is a synthetic kavapyrone originally isolated in the form of (+) kavain. Previously observed effects of kavapyrones have reflected considerable similarity to effects of benzodiazepines. Using these observations and the results of studies suggesting that kavapyrones are involved in modulating one GABA receptor (GABAA), researchers hypothesized that the neurological activity of kavapyrones may be related to some type of interaction with another binding site – a site that in turn modulates activity at the GABA site. Recently, using an analytical technique called fluorescence correlation spectroscopy, specific interactions have been identified between a derivative of kavain and human cortical neurons. Follow-up saturation studies supported the existence of a receptor site. The researchers also enthusiastically present their “spacer” method for probing ligand-receptor models.

Boonen G, Pramanik A, Rigler R, et al. Evidence for specific interactions between kavain and human cortical neurons monitored by fluorescence correlation spectroscopy. Planta Medica 2000; 66: 7-10.

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