Abstract
Hydroalcoholic hypericum extract inhibits the synaptosomal uptake of serotonin, norepinephrine, and dopamine with about similar affinities and leads to a significant down-regulation of cortical beta-adrenoceptors and 5-HT2-receptors after subchronic treatment of rats. While neither hypericine nor kaempferol did show any reuptake inhibiting properties, hyperforin was identified as the unspecific reuptake inhibitor of hypericum extracts with half-maximal inhibitory concentrations for the three synaptosomal uptake systems mentioned above between 80 and 200 nmol/l. Moreover, a hyperforin-enriched (38%) CO2 extract also leads to a significant beta-receptor down-regulation after subchronic treatment. The data suggest hyperforin as the active principle of hypericum extracts in biochemical models of antidepressant activity.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Brain / drug effects*
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Brain / enzymology
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Bridged Bicyclo Compounds
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Dopamine / metabolism
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Female
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Hypericum
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Male
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Mice
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Monoamine Oxidase / metabolism
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Neurotransmitter Uptake Inhibitors / chemistry
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Neurotransmitter Uptake Inhibitors / metabolism
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Neurotransmitter Uptake Inhibitors / pharmacology*
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Norepinephrine / metabolism
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Perylene / analogs & derivatives*
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Perylene / chemistry
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Perylene / pharmacology
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Phloroglucinol / analogs & derivatives
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Plant Extracts / chemistry
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Plant Extracts / pharmacology
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Plants, Medicinal
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Quercetin / analogs & derivatives*
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Quercetin / chemistry
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Quercetin / pharmacology
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Rats
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Rats, Wistar
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Receptors, Adrenergic, beta / metabolism
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Receptors, Serotonin / metabolism
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Serotonin / metabolism
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Synaptosomes / drug effects*
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Synaptosomes / metabolism
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Terpenes / analysis
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Terpenes / pharmacology
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Xanthenes / chemistry*
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Xanthenes / pharmacology*
Substances
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Bridged Bicyclo Compounds
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Neurotransmitter Uptake Inhibitors
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Plant Extracts
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Receptors, Adrenergic, beta
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Receptors, Serotonin
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Terpenes
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Xanthenes
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Serotonin
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Perylene
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Quercetin
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Phloroglucinol
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Monoamine Oxidase
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hyperforin
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Dopamine
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Norepinephrine