Hyperforin enhances the extracellular concentrations of catecholamines, serotonin and glutamate in the rat locus coeruleus

Inhibition of Synaptosomal Uptake of 3H-L-glutamate and 3H-GABA by Hyperforin, a Major Constituent of St. John's Wort The Role of Amiloride Sensitive Sodium Conductive Pathways

“…This contrasts to all clinically used antidepressant drugs, which are only weak inhibitors of L-glutamate and GABA uptake, especially in relationship to their potent inhibition of serotonin and/or norepinephrine uptake (Tatsumi et al 1997;Richelson and Pfenning 1984). Some experimental findings indicated that administration of hypericum extract or of hyperforin lead to an enhanced glutamatergic and GABAergic neurotransmission in animal or human brain Schellenberg et al 1998;Kaehler et al 1999). However, the possible relevance of these effects for the antidepressant activity is not yet known.…”

“…It is a potent inhibitor of the uptake of serotonin, norepinephrine and dopamine, it is active in several biochemical and behavioral models of antidepressant activity (Bhattacharya et al 1998;Chatterjee et al 1998aChatterjee et al , 1998bMüller et al 1997), it is responsible for specific changes of the rat and human EEG typically seen for specific serotonin reuptake inhibitors Schellenberg et al 1998) and it elevates extracellular concentrations of serotonin, norepinephrine, and dopamine in the rat brain after i.p. administration (Kaehler et al 1999). In addition to this rather typical antidepressant profile, hyperforin also potently inhibits the synaptosomal uptake of L-glutamate and GABA (Müller et al 1998;Chatterjee et al 1998a) and also enhances extracellular L-glutamate levels in rat brain (Kaehler et al 1999).…”

“…administration (Kaehler et al 1999). In addition to this rather typical antidepressant profile, hyperforin also potently inhibits the synaptosomal uptake of L-glutamate and GABA (Müller et al 1998;Chatterjee et al 1998a) and also enhances extracellular L-glutamate levels in rat brain (Kaehler et al 1999). Since this property is unique among all other antidepressant compounds known, it was investigated in further detail.…”

Hypericumperforatum L. Showed Antinociceptive Effects Through Opioidergic And Serotonergic Systems

“…On the other hand, the release of prostaglandins and leukotrienes B4 in inflammatory processes is an amplifier for pain mechanisms (Kümper, 1989;Kaehler, 1999;Obach, 2000) that this effect is blocked by COX-1 and 5-LO inhibitors (Obach, 2000). On the other hand leukotriene D4 antagonists and inhibitors of COX-1 reduces tonic pains, such as the second phase of the http: //dx.doi.org/10.15405/epsbs.2017.09.4 Corresponding Author: Freshteh Motamedi Selection and peer-review under responsibility of the Organizing Committee of the conference eISSN: 2357-1330 44 formalin test and reduce pain caused by acetic acid (Kaehler, 1999;Nathan, 2001;Perfumi et al 2001). 5-LO inhibitory role in the release of prostaglandins and different leukotrienes production during the second phase of the formalin test (Kümper, 1989;Obach, 2000;Perfumi et al 2001;Dimpfel, Todorova, & Vonderheid-Guth, 1999) is extremely clear.…”

“…5-LO inhibitory role in the release of prostaglandins and different leukotrienes production during the second phase of the formalin test (Kümper, 1989;Obach, 2000;Perfumi et al 2001;Dimpfel, Todorova, & Vonderheid-Guth, 1999) is extremely clear. Given the role of 5-LO inhibitors in the production of arachidonic metabolites acid and the metabolites such as leukotriene D4 (Kaehler, 1999) and prostaglandins (Perfumi et al 2001) in tonic pains such as the second phase of the formalin test can suggest possible analgesic effect of the extract through effects inhibition of COX-1 and 5-LO introduced in the second phase of the test.…”