Hyperforin Represents the Neurotransmitter Reuptake Inhibiting Constituent of Hypericum Extract

W. E. Müller; A. Singer; M. Wonnemann; U. Hafner; M. Rolli; C. Schäfer

doi:10.1055/s-2007-979341

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Pharmacopsychiatry 1998; 31: 16-21
DOI: 10.1055/s-2007-979341

Original Paper

Hyperforin Represents the Neurotransmitter Reuptake Inhibiting Constituent of Hypericum Extract

W. E. Müller¹ ^, ² , A. Singer¹ , M. Wonnemann¹ , U. Hafner² , M. Rolli² , C. Schäfer²

¹Department of Pharmacology, Biocenter University of Frankfurt, Frankfurt, Germany
²Department of Psychopharmacology, Central Institute of Mental Health, Mannheim, Germany

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Publication Date:
20 April 2007 (online)

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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 (3-adrenoceptors and β-HT_2-receptors after sub-chronic 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 200nmol/l. Moreover, a hyperforin-enriched (38 %) CO₂ extract also leads to a significant β-receptor down-regulation after subchronic treatment. The data suggest hyperforin as the active principle of hypericum extracts in biochemical models of antidepressant activity.