Clinical significance of 5-HT uptake inhibitors

Montgomery, Stuart

doi:10.1002/hup.470060502

Cited by 15 publications

(6 citation statements)

References 19 publications

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“…The serotonergic drugs employed in the present paradigm suppressed the immobility time in forced-swimming. These results are consistent with findings that serotonergic drugs are clinically active in the treatment of depression (1). It has been suggested that SSRIs are not effective in the forced-swimming test (8), and another report indicated that norepinephrine reuptake inhibitors, but not SSRIs are effective in this model (9).…”

supporting

confidence: 90%

“…have established their status as effective antidepressants with effects comparable to the more traditionally used tricyclic and tetracyclic antidepressants (1). Furthermore, it is recognized that the binding sites for the antidepressant imipramine are the 5-HTreuptake pumps (2) and that 5-HT2 receptors are also down-regulated by the repeated administration of antidepressants (3).…”

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confidence: 99%

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Neither the 5-HT1A- nor the 5-HT2-Receptor Subtype Mediates the Effect of Fluvoxamine, a Selective Serotonin Reuptake Inhibitor, on Forced-Swimming-Induced Immobility in Mice

Egawa

Ichimaru

Imanishi

et al. 1995

Japanese Journal of Pharmacology

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ABSTRACT-The effect of fluvoxamine, a selective serotonin (5-HT) reuptake inhibitor, was studied in the forced-swimming test, a model of depression, in mice. Fluvoxamine at 60 mg/kg, p.o. significantly decreased the immobility time in the forced-swimming test. A similar effect was observed by the selective norepinephrine reuptake inhibitor desipramine at the same dose. Furthermore, the suppression of immobility time was slightly potentiated by repeated administration of fluvoxamine, and a significant effect was observed at 30 mg/kg, p.o. The effect of fluvoxamine on forced-swimming was unaffected by the 5-HT2 antagonist ritanserin. On the other hand, the 5-HT1A antagonist Selective serotonin (5-HT) reuptake inhibitors (SSRIs; fluvoxamine, fluoxetine, etc.) have established their status as effective antidepressants with effects comparable to the more traditionally used tricyclic and tetracyclic antidepressants (1). Furthermore, it is recognized that the binding sites for the antidepressant imipramine are the 5-HTreuptake pumps (2) and that 5-HT2 receptors are also down-regulated by the repeated administration of antidepressants (3). These lines of evidence support the 5-HT theory of depressive illness, and it is apparent, therefore, that malfunction of 5-HT transmission is involved in depressive illness.The forced-swimming test has been used elsewhere to evaluate the efficacy of antidepressants (4). There is, however, few reports about the effect of fluvoxamine on the forced-swimming test (5). Furthermore, there is no report about the subchronic effect of fluvoxamine on this model or which 5-HT receptor subtype mediates the effect of fluvoxamine on immobility.In the present experiments, therefore, we investigated Male ICR strain mice weighing 20-30 g (Nihon SLC, Atsugi) were used in the experiment. All animals were housed in the animal rooms (temperature, 20-25C; °hu-midity, 60 ±5%; light on at 7 a.m.; light off at 7 p.m.) for

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supporting

confidence: 90%

mentioning

confidence: 99%

Neither the 5-HT1A- nor the 5-HT2-Receptor Subtype Mediates the Effect of Fluvoxamine, a Selective Serotonin Reuptake Inhibitor, on Forced-Swimming-Induced Immobility in Mice

Egawa

Ichimaru

Imanishi

et al. 1995

Japanese Journal of Pharmacology

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“…In addition, serotonin receptor activation increases anxiolytic-like behavioral responses, as measured by the elevated plus-maze test [ 22 ]. The number of marbles buried is reduced by benzodiazepine receptors agonist (diazepam) and serotonin reuptake inhibitors (fluoxetine and clomipramine) [ 23 ]. Spontaneous locomotor activity is also reduced by dopamine receptor blocking agents [ 24 ].…”

Section: Discussionmentioning

confidence: 99%

Anxiolytic Effects of Herbal Ethanol Extract from Gynostemma pentaphyllum in Mice after Exposure to Chronic Stress

et al. 2013

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In this study, the effects of herbal ethanol extracts of Gynostemma pentaphyllum (GP-EX), on chronic electric footshock (EF) stress-induced anxiety disorders were investigated in mice, which were orally treated with GP-EX (30 mg/kg and 50 mg/kg) once a day for 14 days, followed by exposure to EF stress (2 mA, with an interval and duration of 10 s for 3 min). After the final exposure to EF stress, the elevated plus-maze and marble burying tests were performed, and the levels of dopamine and serotonin in the brain, the serum levels of corticosterone, and the expression of c-Fos in the paraventricular nuclei (PVN) were determined. Treatment with GP-EX (30 mg/kg and 50 mg/kg) significantly recovered the number of entries into open arms and time spent on open arms, which was reduced by chronic EF stress. GP-EX (30 mg/kg and 50 mg/kg) also reduced the number of marbles buried, which was increased by chronic EF stress. In addition, electric EF stress significantly decreased the levels of dopamine and serotonin in the brain, which was recovered by treatment with GP-EX (30 mg/kg and 50 mg/kg). The serum levels of corticosterone, which were markedly increased by chronic EF stress, were reduced by treatment with GP-EX (30 mg/kg and 50 mg/kg). Chronic EF stress-induced increases in c-Fos expression were also markedly reduced by GP-EX (30 mg/kg and 50 mg/kg) in the PVN. These results suggest that GP-EX shows anxiolytic functions, determined by the elevated plus-maze and marble burying tests, which are mediated by modulating the activity of dopamine and serotonin neurons as well as the expression of c-Fos in the brain, and the serum levels of corticosterone. Clinical trials of herbal GP-EX and its bioactive components need further investigation.

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“…Clinical reports indicate that because norfluoxetine has a long half-life of 10 days, a 5 week interval is recommended prior to initiating treatment with certain other agents, such as monoamine oxidase inhibitors (Montgomery, 1991), with which fluoxetine may have a toxic interaction.…”

Section: Discussionmentioning

confidence: 99%

Neurochemical evidence that the antidepressant paroxetine is a selective serotonin reuptake inhibitor in man

et al. 1993

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Paroxetine, a clinically effective antidepressant, has been shown to be a potent and selective inhibitor of 5‐hydroxytryptamine (5‐HT, or serotonin) reuptake in rodent brain tissues; however, to date only indirect evidence of similar selectivity in man has been available. In the current study, paroxetine (10 to 40 mg daily) or placebo was administered to young, healthy volunteers for 28 d. Plasma samples were obtained at regular intervals and were assessedfor either [3H]‐ 5‐HT or [3H]‐norepinephrine (NE) uptake inhibiting properties in rat cortical synaptosomal preparations. Plasma samples obtained from those subjects administered paroxetine demonstrated weak inhibition of [3H]‐5‐HT uptake into rat cortical synaptosomal preparations 2, 4, and 6 h after the first dose was administered on day 1. However, significant inhibition was observed on day 7 and at steady‐state levels on day 28 (54% and 66%, respectively). No inhibition of [3H]‐5‐HT uptake was observed with plasma samples obtained following a 2 week wash‐outperiod (day 42). Plasma samples obtained from subjects administered paroxetine had no effect on [3H]‐NE uptake, while plasma samples from subjects administered placebo did not alter [3H]‐5‐HT or [3H]‐NE uptake. These results demonstrate that paroxetine, at clinically relevant doses, is a selective serotonin reuptake inhibitor in man. Depression 1:263–267 (1993). © 1993 Wiley‐Liss, Inc.

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Clinical significance of 5-HT uptake inhibitors

Cited by 15 publications

References 19 publications

Neither the 5-HT1A- nor the 5-HT2-Receptor Subtype Mediates the Effect of Fluvoxamine, a Selective Serotonin Reuptake Inhibitor, on Forced-Swimming-Induced Immobility in Mice

Neither the 5-HT1A- nor the 5-HT2-Receptor Subtype Mediates the Effect of Fluvoxamine, a Selective Serotonin Reuptake Inhibitor, on Forced-Swimming-Induced Immobility in Mice

Anxiolytic Effects of Herbal Ethanol Extract from Gynostemma pentaphyllum in Mice after Exposure to Chronic Stress

Neurochemical evidence that the antidepressant paroxetine is a selective serotonin reuptake inhibitor in man

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