5-HT3 receptors and neurotransmitter release in the CNS: a nerve ending story?

@article{Hooft20005HT3RA,
  title={5-HT3 receptors and neurotransmitter release in the CNS: a nerve ending story?},
  author={Johannes A. van Hooft and Henk P. M. Vijverberg},
  journal={Trends in Neurosciences},
  year={2000},
  volume={23},
  pages={605-610}
}
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TLDR
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5‐HT3 (serotonin type 3) receptors are targets of antiemetics, antipsychotics, and antidepressants and are believed to play a role in cognition. Nevertheless, contrasting results have been obtained
Antipsychotic drugs antagonize human serotonin type 3 receptor currents in a noncompetitive manner
TLDR
Since 5-HT3 receptors modulate mesolimbic and mesocortical dopaminergic activity, the functional antagonism of neuroleptics at 5- HT3 receptors may contribute to their antipsychotic efficacy and may constitute a not yet recognized pharmacological principle of these drugs.
Dopamine and Serotonin Crosstalk Within the Dopaminergic and Serotonergic Systems
TLDR
This work has shown that under circumstances that elevate extracellular 5-HT (such as treatment with antidepressants that block SERTs), DATs expressed on the dense DA terminals of the striatum uptake5-HT, and this process induces DA and 5- HT co-signaling mechanisms that have important implications for neuropsychiatric disorders and their treatments.
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References

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The 5-HT3 Receptor Channel: Function, Activation and Regulation
TLDR
The activation of the 5-HT3R opens a cationic ion channel that depolarizes the membrane, thereby activating a rapid excitatory response in a variety of central and peripheral nervous system (CNS and PNS) preparations.
5-HT3 receptors are membrane ion channels
TLDR
The first recordings of currents through single ion channels activated by 5-HT3 receptors are reported, in excised membrane patches from neurons of the guinea pig submucous plexus, implying a role for 5- HT, and perhaps other amines, as a 'fast' synaptic transmitter.
Central and peripheral 5-HT3 receptors
TLDR
The role of peripheral and central 5- HT3 receptors in the control of nociceptive messages and the clinical perspectives of drugs acting at 5-HT3 receptors are discussed.
5-HT3 receptors mediate inhibition of acetylcholine release in cortical tissue
TLDR
Evidence that a reduction in cortical cholinergic function can be effected in vitro by 5-HT3 receptors is provided and Radioligand binding studies show a high density of 5- HT3 receptors in theCholinergic-rich entorhinal cortex.
5-Hydroxytryptamine2 receptor facilitates GABAergic neurotransmission in rat hippocampus.
  • R. ShenR. Andrade
  • Biology
    The Journal of pharmacology and experimental therapeutics
  • 1998
TLDR
Results interpret these results to indicate that 5-HT2 receptors activate GABAergic interneurons in the slice, leading to an increase in GABAergic synaptic activity onto pyramidal cells of the CA1 region.
Primary structure and functional expression of the 5HT3 receptor, a serotonin-gated ion channel.
TLDR
A complementary DNA clone containing the coding sequence of one of these rapidly responding channels, a 5HT3 subtype of the serotonin receptor, has been isolated by screening a neuroblastoma expression library for functional expression of serotonin-gated currents in Xenopus oocytes.
5-HT3 serotonin hetero-receptors inhibit [3H]acethylcholine release in rat cortical synaptosomes.
TLDR
The data suggest that 5-HT3 hetero-receptors are located on cortical nerve endings where they directly inhibit acethylcholine release, but they do not seem to be located on serotonergic and dopaminergic nerve endings in the brain regions studied, probably having an indirect effect on these neurotransmitters release in rat brain.
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