The neuronal 5-HT3 receptor network after 20 years of research — Evolving concepts in management of pain and inflammation

Faerber, Lothar; Drechsler, S.; Ladenburger, S.; Gschaidmeier, Harald; Fischer, Wolfgang B.

doi:10.1016/j.ejphar.2007.01.028

Cited by 192 publications

(175 citation statements)

References 65 publications

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“…It is known that 5-HT 2A/2C and 5-HT 3 receptors are the main subtype receptors that mediate 5-HT-evoked glutamate release (Aghajanian and Marek, 1997;Faerber et al, 2007). This statement was confirmed by our result that the application of a combination of the 5-HT 2A/2C and 5-HT 3 receptor antagonists could abolish the effect of 5-HT on glutamate release.…”

Section: Discussionsupporting

confidence: 88%

“…5-HT 3 receptors are found in the brain, predominantly in presynaptic sites except for the hippocampus, where they are mostly postsynaptic receptors (Miquel et al, 2002). The preferential localization on nerve endings is consistent with a physiological role of 5-HT 3 receptors in the control of neurotransmitter release (Faerber et al, 2007). Activation of presynaptic 5-HT 3 receptors followed by rapid depolarization causes a rapid rise in cytosolic Ca 2ϩ concentration by inducing Ca 2ϩ influx and mobilization of intracellular Ca 2ϩ stores, thereby modulating the release of various neurotransmitters (Faerber et al, 2007).…”

Section: Discussionsupporting

confidence: 70%

“…It has been known that 5-HT induces glutamate release via activation of different 5-HT receptor subtypes, especially 5-HT 2A/2C and 5-HT 3 subtypes (Aghajanian and Marek, 1997;Faerber et al, 2007). To study which 5-HT receptor subtypes were inhibited by DHEAS, we observed the effect of DHEAS on the 5-HT subtype receptor agonist-evoked increase in the frequency of sEPSCs.…”

Section: Dheas Inhibits 5-ht-evoked Glutamate Release But Has No Effementioning

confidence: 99%

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Neuroactive Steroid Dehydroepiandrosterone Sulfate Inhibits 5-Hydroxytryptamine (5-HT)-Evoked Glutamate Release via Activation of σ-1 Receptors and Then Inhibition of 5-HT₃Receptors in Rat Prelimbic Cortex

Dong

Zhu²,

Dong³

et al. 2009

J Pharmacol Exp Ther

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Dehydroepiandrosterone sulfate (DHEAS) is one of the most important neuroactive steroids. The present study examined the effect of DHEAS on spontaneous and evoked glutamate release in the pyramidal cells of layers V and VI of the rat prelimbic cortex by using whole-cell patch-clamp recordings in slices and further investigated its mechanism. The results showed that DHEAS at 1 M had no effect on spontaneous glutamate release but inhibited 5-hydroxytryptaime (5-HT)-evoked glutamate release. The concentration-response relationship of this effect of DHEAS was U-shaped with a maximum at 1 M, and this inhibition seemed to have some extent of selectivity for the 5-HT-evoked glutamate release because it had no effects on high K ϩ -, electrical stimulus-, and dopamineevoked releases. Further study showed that DHEAS inhibited the 5-HT 3 receptor agonist evoked-glutamate release but had no effect on the 5-HT 2A/2C receptor agonist-evoked release. Moreover, the 5-HT 3 receptor antagonist could block the effect of DHEAS on the 5-HT-evoked glutamate release. The mechanism study showed that the -1 receptor antagonist could block the effect of DHEAS and that the -1 receptor agonist could mimic the effect of DHEAS on 5-HT 3 receptor agonistevoked glutamate release and intrasynaptosomal Ca 2ϩ increase. These results suggest that DHEAS can inhibit 5-HTevoked glutamate release via activation of the -1 receptor and then inhibition of the 5-HT 3 receptor in the pyramidal cells of the prelimbic cortex.

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Section: Discussionsupporting

confidence: 88%

Section: Discussionsupporting

confidence: 70%

Section: Dheas Inhibits 5-ht-evoked Glutamate Release But Has No Effementioning

confidence: 99%

See 1 more Smart Citation

Neuroactive Steroid Dehydroepiandrosterone Sulfate Inhibits 5-Hydroxytryptamine (5-HT)-Evoked Glutamate Release via Activation of σ-1 Receptors and Then Inhibition of 5-HT₃Receptors in Rat Prelimbic Cortex

Dong

Zhu²,

Dong³

et al. 2009

J Pharmacol Exp Ther

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show abstract

“…The 5-HT3 receptor is a pentameric ligand-gated cation channel located in CNS regions integrating reward and anxiety control as well as emetic and pain processing. 24 The physiological role of 5-HT3 receptors encompasses responses to serotonin, dopamine, glutamate, GABA, and substance P. The novel physiogenomic association of HTR3A found here is thus plausible.…”

Section: Discussionmentioning

confidence: 57%

Physiogenomic Analysis of Localized fMRI Brain Activity in Schizophrenia

et al. 2008

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The search for genetic factors associated with disease is complicated by the complexity of the biological pathways linking genotype and phenotype. This analytical complexity is particularly concerning in diseases historically lacking reliable diagnostic biological markers, such as schizophrenia and other mental disorders. We investigate the use of functional magnetic resonance imaging (fMRI) as an intermediate phenotype (endophenotype) to identify physiogenomic associations to schizophrenia. We screened 99 subjects, 30 subjects diagnosed with schizophrenia, 13 unaffected relatives of schizophrenia patients, and 56 unrelated controls, for gene polymorphisms associated with fMRI activation patterns at two locations in temporal and frontal lobes previously implied in schizophrenia. A total of 22 single nucleotide polymorphisms (SNPs) in 15 genes from the dopamine and serotonin neurotransmission pathways were genotyped in all subjects. We identified three SNPs in genes that are significantly associated with fMRI activity. SNPs of the dopamine beta-hydroxylase (DBH) gene and of the dopamine receptor D4 (DRD4) were associated with activity in the temporal and frontal lobes, respectively. One SNP of serotonin-3A receptor (HTR3A) was associated with temporal lobe activity. The results of this study support the physiogenomic analysis of neuroimaging data to discover associations between genotype and disease-related phenotypes.

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“…Central to the pharmacodynamic hypothesis to explain this interaction is the pharmacology of serotonin and its receptors with respect to nociception and analgesia, which remains a complex and incompletely understood area. Postulated roles for the 5-HT 3 receptor in pain signalling include: mediating pronociceptive signalling via excitatory effects on peripheral nerve endings, and on presynaptic terminals of primary afferent nerve fibres; and participation in both descending facilitatory and inhibitory pathways [18][19][20]. Increased serotonin resulting from tramadol-mediated serotonin release and inhibition of serotonin re-uptake, in combination with antagonism of 5-HT 3 receptors, could result in increased analgesic requirements of tramadol in the acute postoperative period.…”

Section: Discussionmentioning

confidence: 99%

The effect of ondansetron on the efficacy of postoperative tramadol: a systematic review and meta-analysis of a drug interaction

2014

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SummarySeveral studies have investigated the presence of a drug interaction between tramadol and ondansetron that reduced the efficacy of tramadol postoperatively. Most of these studies were small and the results inconsistent, so we performed a systematic review and meta-analysis of randomised controlled trials comparing the cumulative dose of tramadol administered by patient-controlled analgesia within the first 24 h after surgery between subjects receiving tramadol alone and those who received tramadol with ondansetron. Six studies, with a total of 340 participants, met the selection criteria and were included in the meta-analysis. There was an increased tramadol requirement in patients receiving ondansetron. The standardised mean difference in tramadol requirements, expressed in terms of standard deviations (95% CI), was 1.03 (0.54-

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The neuronal 5-HT3 receptor network after 20 years of research — Evolving concepts in management of pain and inflammation

Cited by 192 publications

References 65 publications

Neuroactive Steroid Dehydroepiandrosterone Sulfate Inhibits 5-Hydroxytryptamine (5-HT)-Evoked Glutamate Release via Activation of σ-1 Receptors and Then Inhibition of 5-HT₃Receptors in Rat Prelimbic Cortex

Neuroactive Steroid Dehydroepiandrosterone Sulfate Inhibits 5-Hydroxytryptamine (5-HT)-Evoked Glutamate Release via Activation of σ-1 Receptors and Then Inhibition of 5-HT₃Receptors in Rat Prelimbic Cortex

Physiogenomic Analysis of Localized fMRI Brain Activity in Schizophrenia

The effect of ondansetron on the efficacy of postoperative tramadol: a systematic review and meta-analysis of a drug interaction

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The neuronal 5-HT3 receptor network after 20 years of research — Evolving concepts in management of pain and inflammation

Cited by 192 publications

References 65 publications

Neuroactive Steroid Dehydroepiandrosterone Sulfate Inhibits 5-Hydroxytryptamine (5-HT)-Evoked Glutamate Release via Activation of σ-1 Receptors and Then Inhibition of 5-HT3Receptors in Rat Prelimbic Cortex

Neuroactive Steroid Dehydroepiandrosterone Sulfate Inhibits 5-Hydroxytryptamine (5-HT)-Evoked Glutamate Release via Activation of σ-1 Receptors and Then Inhibition of 5-HT3Receptors in Rat Prelimbic Cortex

Physiogenomic Analysis of Localized fMRI Brain Activity in Schizophrenia

The effect of ondansetron on the efficacy of postoperative tramadol: a systematic review and meta-analysis of a drug interaction

Contact Info

Product

Resources

About

Neuroactive Steroid Dehydroepiandrosterone Sulfate Inhibits 5-Hydroxytryptamine (5-HT)-Evoked Glutamate Release via Activation of σ-1 Receptors and Then Inhibition of 5-HT₃Receptors in Rat Prelimbic Cortex

Neuroactive Steroid Dehydroepiandrosterone Sulfate Inhibits 5-Hydroxytryptamine (5-HT)-Evoked Glutamate Release via Activation of σ-1 Receptors and Then Inhibition of 5-HT₃Receptors in Rat Prelimbic Cortex