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.