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

© Georg Thieme Verlag Stuttgart · New York

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
Further Information

Publication History

Publication Date:
20 April 2007 (online)


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-HT2-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.