Effect of flibanserin (BIMT 17), fluoxetine, 8-OH-DPAT and buspirone on serotonin synthesis in rat brain

@article{Brambilla1999EffectOF,
  title={Effect of flibanserin (BIMT 17), fluoxetine, 8-OH-DPAT and buspirone on serotonin synthesis in rat brain},
  author={Alessandro Brambilla and A. Baschirotto and N Grippa and Franco Borsini},
  journal={European Neuropsychopharmacology},
  year={1999},
  volume={10},
  pages={63-67}
}
In male rats, the effects of the administration of the novel serotonergic agent flibanserin on the synthesis of 5-HT were evaluated in the frontal cortex (FC), hippocampus (Hip) and brainstem (Br). The selective serotonergic uptake blocker, fluoxetine, and two serotonin1A (5-HT1A) agonists, 8-hydroxy-2-(di-n-propylamino)tetraline (8-OH-DPAT) and buspirone, were used as reference compounds. The synthesis of 5-HT was assessed by measuring the accumulation of 5-hydroxytryptophan (5-HTP) after… Expand
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References

SHOWING 1-10 OF 25 REFERENCES
Antidepressant-like action of 8-OH-DPAT, a 5-HT1A agonist, in the learned helplessness paradigm: evidence for a postsynaptic mechanism
TLDR
The results suggest that the ability of 8-OH-DPAT to reverse helpless behaviour probably involved the stimulation of postsynaptic rather than presynaptic 5-HT1A receptors. Expand
Receptor reserve for 5-hydroxytryptamine1A-mediated inhibition of serotonin synthesis: possible relationship to anxiolytic properties of 5-hydroxytryptamine1A agonists.
TLDR
The results suggest that 5- HT1A receptor-mediated regulation of 5-HT synthesis appears to be mediated by somatodendritic autoreceptors on5-HT neurons in the midbrain raphé nuclei, and suggest that these autoreceptor possess a large receptor reserve for agonists. Expand
Influence of repeated treatment with buspirone on central 5-hydroxytryptamine and dopamine synthesis
TLDR
It is suggested that repeated treatment with buspirone reduces the synthesis of dopamine in the striatum but that the synthesisof 5-HT is unaffected. Expand
Central pre- and postsynaptic 5-HT1A receptors in rats treated chronically with a novel antidepressant, cericlamine.
TLDR
The idea that postsynaptic and somatodendritic 5-HT1A receptors are differently regulated in the rat brain is supported, because only the latter receptors desensitized after a long-term blockade of serotonin reuptake by cericlamine is suggested. Expand
The 5-HT1A receptor agonist, 8-OH-DPAT, preferentially activates cell body 5-HT autoreceptors in rat brain in vivo
SummaryThe present study was undertaken in an attempt to assess whether the effects of the potent and selective 5HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino)tetralin, 8-OH-DPAT, on cerebralExpand
Modulation of the activity of central serotoninergic neurons by novel serotonin1A receptor agonists and antagonists: a comparison to adrenergic and dopaminergic neurons in rats.
TLDR
With the exception of (-)-tertatolol, which behaved as a weak agonist, a very similar pattern of inhibition of 5-HT turnover was seen in the striatum, the hippocampus and the hypothalamus (DRN and median raphe nucleus) and the spinal cord, with the Striatum displaying the greatest sensitivity. Expand
Inhibition of serotonergic dorsal raphe neurons by systemic and iontophoretic administration of buspirone, a non-benzodiazepine anxiolytic drug.
TLDR
The present study supports the notion that central serotonergic systems may be involved in the therapeutic effects of anxiolytic drugs by concluding that buspirone potently and directly inhibits the firing of Serotonergic dorsal raphe neurons in the rat. Expand
Sex differences in neurochemical and behavioural effects of 8-hydroxy-2-(di-n-propylamino) tetralin.
TLDR
The present article integrates research on neurochemical and behavioural effects of 8-OH-DPAT in male and female rats, in order to investigate sex-related differences in 5-HT-1A receptor dependent functions. Expand
Effects of a selective 5‐HT2 agonist, DOI, on 5‐HT neuronal firing in the dorsal raphe nucleus and 5‐HT release and metabolism in the frontal cortex
TLDR
The results demonstrate that DOI is a potent inhibitor of 5‐HT neuronal firing and terminal release and that the effects on release are not mediated by an action within the terminal region. Expand
The effect of BIMT 17, a new potential antidepressant, in the forced swimming test in mice
TLDR
Neither the reduction of 5-HT synthesis brought about by p-chlorophenylalanine nor the selective destruction of5-HT containing neurons by 5,7-dihydroxytryptamine reduced the BIMT 17 effect, suggesting that BIMM 17 acts postsynaptically in increasing struggling behaviour. Expand
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