[3H]-Monoamine Uptake Inhibition Properties of Kava Pyrones

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Abstract
Three kava pyrones, the natural compounds (+)-methysticine and (+)-kavain, and the synthetic racemate (±)-kavain, were tested concerning their action on in vitro uptake of monoamines in synaptosomes prepared from the cerebral cortex and hippocampus of rats. (±)-Kavain and (+)-kavain were found to potently inhibit the uptake of [3 H]-noradrenaline. Uptake of [3 H]-noradrenaline was inhibited in the following order of potency: (±)-kavain = (+)-kavain > (+)-methysticine, whereas none of the kava pyrones efficiently blocked the uptake of [3 H]-serotonin. The results indicate a pyrone-specific non-stereo-selective inhibition of the [3 H]-noradrenaline uptake which might be responsible for or, at least, contribute to the psychotropic properties of kava pyrones.

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