Inhibition of synaptosomal high-affinity uptake of dopamine and serotonin by estrogen agonists and antagonists

Michel, Martin C.; Rother, A.; Hiemke, Christoph; Ghraf, Rüdiger

doi:10.1016/0006-2952(87)90629-0

Cited by 53 publications

(25 citation statements)

References 21 publications

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“…In this point, it is important to mention that the behavioral profile induced by EE 2 alone was similar to that produced by mixed reuptake inhibitors that act at both the noradrenergic and serotonergic systems, such as venlafaxine and duloxetine in the FST, that is, these compounds produce a decrease in immobility with a concomitant increase in both swimming and climbing behaviors (Rénéric and Lucki, 1998). Furthermore, in vitro studies have shown that EE 2 inhibits both serotonin and noradrenaline transporters with a similar potency (Michel et al, 1987;Ghraf et al, 1983). At present, data on the mechanism of action of EE 2 on neurotransmitter systems are derived only from in vitro studies and there are no data from behavioral studies.…”

Section: Discussionmentioning

confidence: 86%

“…An important difference between these two estrogens is that the natural estrogen E 2 is more potent at the serotonergic than at the noradrenergic system in decreasing re-uptake sites (Ghraf et al, 1983;Michel et al, 1987), while the synthetic steroidal compound EE 2 inhibits with a comparable efficacy the serotonergic and catecholaminergic sites (Ghraf et al, 1983;Michel et al, 1987). Both estrogens have been used in clinical practice as contraceptive and/or hormonal restitution therapies (Soares et al, 2001).…”

Section: Introductionmentioning

confidence: 99%

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Participation of the 5-HT1A Receptor in the Antidepressant-Like Effect of Estrogens in the Forced Swimming Test

Estrada‐Camarena

Fernández‐Guasti

López‐Rubalcava

2005

Neuropsychopharmacol

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The aim of the present study was to explore the possible participation of the 5-HT 1A receptor in the antidepressant-like action of two estrogenic compounds: 17b-estradiol (E 2 ) and ethynil-estradiol (EE 2 ) in the FST. Ovariectomized female Wistar rats were used in all experiments. As a positive control, the effect of the 5-HT 1A receptor agonist, 8-hydroxy-2-(di-n)-propil-aminotetraline (8-OH-DPAT; 0.0625, 0.125, 0.25 and 0.5 mg/kg) alone or in combination with WAY 100635 (0.5 and 1.0 mg/kg) was analyzed in the FST. In order to analyze the participation of the 5-HT 1A receptor in the antidepressant-like actions of estrogens, the effect of the selective antagonist WAY 100635 (0.5 and 1.0 mg/kg) in combination with E 2 (10 mg/rat) and EE 2 (5 mg/rat) was studied in the FST. In this case, WAY 100635 was administered either simultaneously with the estrogens (48 h before the FST test) or 30 min before the FST. On the other hand, a suboptimal dose of 8-OH-DPAT (0.0625 mg/kg), combined with a noneffective dose of E 2 (2.5 mg/rat) or EE 2 (1.25 mg/rat), was tested in the FST. The results showed that 8-OH-DPAT (0.25 and 0.5 mg/kg), E 2 (10 mg/rat), and EE 2 (5 mg/rat), by themselves, exerted an antidepressant-like action. The antagonist to the 5-HT 1A receptor WAY 100635, when applied together with 8-OH-DPAT or E 2 , blocked their antidepressant-like actions, but not the one induced by EE 2 . Interestingly, when the antagonist was applied 30 min before the FST, it was able to cancel the actions of EE 2 on immobility behavior, and had no effect on the actions of E 2. Finally, when a subthreshold dose of 8-OH-DPAT was combined with a noneffective dose of either E 2 or EE 2 , an antidepressant-like action was observed. The results support the notion that the 5-HT 1A receptor is one of the mediators of the antidepressant-like action of E 2 , and could indirectly contribute to the one induced by EE 2 .

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Section: Discussionmentioning

confidence: 86%

Section: Introductionmentioning

confidence: 99%

Participation of the 5-HT1A Receptor in the Antidepressant-Like Effect of Estrogens in the Forced Swimming Test

Estrada‐Camarena

Fernández‐Guasti

López‐Rubalcava

2005

Neuropsychopharmacol

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“…On the other hand, in vitro studies demonstrate that estrogens can interact, at several levels, with the dopaminergic, the noradrenergic, and the serotonergic systems (Attali et al, 1997;Bethea et al, 1998;Biegon et al, 1983;Cyr et al, 2000;McEwen, 1999;Rubinow et al, 1998). For example, estrogens can inhibit the function of the monoaminergic transporter (Ghraf et al, 1983;Michel et al, 1987;Wilson et al, 1988) and interact with either 5-HT 1A , 5-HT 2A , or b-adrenergic receptors in several brain areas (Biegon et al, 1983;Fink et al, 1996;Kendall et al, 1982;Mize and Alper, 2000;Ö sterlund et al, 1999;Raap et al, 2000;Sumner and Fink, 1995). Interestingly, estrogenic compounds modify those neurotransmitter systems that are targets of antidepressant treatments.…”

Section: Introductionmentioning

confidence: 99%

“…It is important to mention that the estrogenic activity on each of these systems varies depending on the estrogen nature (Chang and Chang, 1999;Ghraf et al, 1983;Michel et al, 1987). Thus, the natural estrogen E 2 decreases both serotonin and noradrenaline reuptake sites, being more potent at the serotonergic than at the noradrenergic system (Ghraf et al, 1983;Michel et al, 1987).…”

Section: Introductionmentioning

confidence: 99%

“…Thus, the natural estrogen E 2 decreases both serotonin and noradrenaline reuptake sites, being more potent at the serotonergic than at the noradrenergic system (Ghraf et al, 1983;Michel et al, 1987). By contrast, the synthetic steroidal compound, ethynil-estradiol (EE 2 ), inhibits, with comparable efficacy, both the serotonergic and the catecholaminergic transporters (Ghraf et al, 1983;Michel et al, 1987).…”

Section: Introductionmentioning

confidence: 99%

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Antidepressant-Like Effect of Different Estrogenic Compounds in the Forced Swimming Test

Estrada‐Camarena

Fernández‐Guasti

López‐Rubalcava

2002

Neuropsychopharmacol

185

124

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The present study evaluated the possible antidepressant-like action of the natural estrogen 17b-estradiol (E 2 , 2.5-10 mg/rat), the synthetic steroidal estrogen ethinyl-estradiol (EE 2 , 1.25-10.0 mg/rat), and the nonsteroidal synthetic estrogen, diethyl-stilbestrol (DES, 0.25-1.0 mg/ rat) in ovariectomized adult female Wistar rats using the forced swimming test (FST). The behavioral profile induced by the estrogens was compared with that induced by the antidepressants fluoxetine (FLX, 2.5-10 mg/kg) and desipramine (DMI, 2.5-10 mg/kg). In addition, the temporal course of the antidepressant-like action of the estrogenic compounds was analyzed. FLX and DMI induced an antidepressant-like effect characterized by a reduced immobility and increased swimming for FLX and decreased immobility and increased climbing for DMI. Both E 2 and EE 2 produced a decrease in immobility and an increase in swimming, suggesting an antidepressant-like action. DES did not affect the responses in this animal model of depression at any dose tested. The time course analysis of the actions of E 2 (10 mg/rat) and EE 2 (5 mg/rat) showed that both compounds induced an antidepressant-like effect observed 1 h after their injection lasting for 2-3 days.

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Distribution of organic cation transporter 3, a corticosterone‐sensitive monoamine transporter, in the rat brain

Gasser

Orchinik

Raju

et al. 2008

J of Comparative Neurology

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Organic cation transporter 3 (OCT3) is a high-capacity, low-affinity transporter that mediates bidirectional, sodium-independent transport of dopamine, norepinephrine, epinephrine, serotonin, and histamine. OCT3-mediated transport is directly inhibited by corticosterone, suggesting a potential role for the transporter in mediating some of the effects of stress and glucocorticoids on monoaminergic neurotransmission. To elucidate the importance of OCT3 in clearance of extracellular monoamines in the brain, we used immunohistochemical techniques to describe the distribution of OCT3-like-immunoreactive (OCT3-ir) cells throughout the rostrocaudal extent of adult male rat brains. OCT3-ir cell bodies were widely distributed throughout the brain, with the highest densities observed in the superior and inferior colliculi, islands of Calleja, subiculum, lateral septum, lateral and dorsomedial hypothalamic nuclei, and granule cell layers of the main and accessory olfactory bulbs, the cerebellum, and the retrosplenial granular cortex. OCT3-ir cells and/or fibers were also observed in circumventricular organs, and OCT3-ir ependymal cells were observed in the linings of all cerebral ventricles. The widespread distribution of OCT3-ir cell bodies, including regions receiving dense monoaminergic projections, suggests an important role for this transporter in regulating extracellular concentrations of monoamines in the rat brain and is consistent with the hypothesis that corticosterone-induced inhibition of OCT3-mediated transport may contribute to effects of acute stress or corticosterone on monoaminergic neurotransmission.

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Inhibition of synaptosomal high-affinity uptake of dopamine and serotonin by estrogen agonists and antagonists

Cited by 53 publications

References 21 publications

Participation of the 5-HT1A Receptor in the Antidepressant-Like Effect of Estrogens in the Forced Swimming Test

Participation of the 5-HT1A Receptor in the Antidepressant-Like Effect of Estrogens in the Forced Swimming Test

Antidepressant-Like Effect of Different Estrogenic Compounds in the Forced Swimming Test

Distribution of organic cation transporter 3, a corticosterone‐sensitive monoamine transporter, in the rat brain

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