title: [3H]-monoamine uptake inhibition properties of kava pyrones.
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 [3H]-noradrenaline. Uptake of [3H]-noradrenaline was inhibited in the following order of potency: (+/-)-kavain = (+)-kavain > (+)-methysticine, whereas none of the kava pyrones efficiently blocked the uptake of [3H]-serotonin. The results indicate a pyrone-specific non-stereo-selective inhibition of the [3H]-noradrenaline uptake which might be responsible for or, at least, contribute to the psychotropic properties of kava pyrones.
authors.affiliation: Institute of Naturheilkunde, University Clinics Ulm, Germany.
authors.forename: U
authors.initials: U
authors.lastname: Seitz
authors.forename: A
authors.initials: A
authors.lastname: Schüle
authors.forename: J
authors.initials: J
authors.lastname: Gleitz
mesh_terms: D000818:Animals; D015306:Biogenic Monoamines / Q000037:antagonists & inhibitors* / Q000378:metabolism; D002540:Cerebral Cortex / Q000378:metabolism; D006624:Hippocampus / Q000378:metabolism; D066298:In Vitro Techniques; D020901:Kava; D010936:Plant Extracts / Q000378:metabolism*; D010946:Plants, Medicinal; D011753:Pyrones / Q000378:metabolism*; D051381:Rats; D013574:Synaptosomes / Q000378:metabolism; D014316:Tritium
chemical_list: D015306:Biogenic Monoamines; D010936:Plant Extracts; D011753:Pyrones; D014316:Tritium