INT65009

Context Info Confidence 0.75 First Reported 1996 Last Reported 2010 Negated 3 Speculated 6 Reported most in Abstract Documents 29 Total Number 35 Disease Relevance 8.51 Pain Relevance 10.59

transport (HTR3A) plasma membrane (HTR3A) transmembrane transport (HTR3A)

Anatomy Link Frequency N1E-115 3 chondrocytes 2 monocytes 2 neurons 2 immune system 2 HTR3A (Homo sapiens) HTR3A - A33T (1)

Pain Link Frequency Relevance Heat antagonist 172 100.00 Serotonin 48 100.00 Dorsal horn neuron 4 99.98 Spinal cord 12 99.28 antidepressant 21 99.12 tramadol 13 98.86 Dorsal horn 11 98.80 headache 16 98.54 Morphine 9 97.88 agonist 21 97.44

Disease Link Frequency Relevance Heat Neuroblastoma 4 99.56 Vomiting 850 99.54 Post-operative Nausea 8 99.28 Constipation 16 98.88 Headache 16 98.54 INFLAMMATION 21 96.92 Pain 5 93.28 Functional Bowel Disorder 7 93.04 Disease 15 89.40 Adverse Drug Reaction 18 85.60

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Effects of tramadol and O-demethyl-tramadol on human 5-HT reuptake carriers and human 5-HT3A receptors: a possible mechanism for tramadol-induced early emesis. ([3H]5-HT)-uptake and patch-clamp techniques were used to study the actions of (+) and (-) tramadol and the active metabolites of tramadol, (+) and (-) O-demethyl-tramadol on the human serotonin (5-HT) transporter and the human 5-HT3A receptor, stably expressed in HEK-293 cells.

Gene_expression (expressed) of 5-HT3A associated with tramadol, vomiting and serotonin

1) Confidence 0.75 Published 2006 Journal Eur. J. Pharmacol. Section Title Doc Link 16427041 Disease Relevance 0.10 Pain Relevance 1.14

Finally, coexpression of wild-type 5-HT3A or 5-HT3B subunits with 5-HT3A variants A33T, S253N, or M257I resulted in mixed or heteromeric receptors, characterized by significantly reduced maximal responses to 5-HT compared with the wild-type receptors.

Gene_expression (coexpression) of 5-HT3A (A33T)

2) Confidence 0.75 Published 2007 Journal Pharmacogenet. Genomics Section Body Doc Link 17496724 Disease Relevance 0 Pain Relevance 0

The 5-hydroxytryptamine 3 (5-HT3) receptor is expressed widely in the central and peripheral nervous systems, where it mediates or modulates a wide range of physiological processes.

Gene_expression (expressed) of 5-HT3 in peripheral nervous systems

3) Confidence 0.75 Published 2008 Journal Trends Pharmacol. Sci. Section Abstract Doc Link 18597859 Disease Relevance 0.25 Pain Relevance 0.08

Our data show that 5-HT3A receptors are widely expressed in cells of the immune system and that they might play an important role in inflammatory events and in the observed antiphlogistic effects of 5-HT3 receptor antagonists.

Gene_expression (expressed) of 5-HT3A in immune system associated with inflammation and antagonist

4) Confidence 0.75 Published 2004 Journal Scand. J. Rheumatol. Suppl. Section Abstract Doc Link 15515405 Disease Relevance 0.18 Pain Relevance 0.21

Expression of 5-HT3A receptors in cells of the immune system.

Gene_expression (Expression) of 5-HT3A in immune system

5) Confidence 0.75 Published 2004 Journal Scand. J. Rheumatol. Suppl. Section Title Doc Link 15515405 Disease Relevance 0.16 Pain Relevance 0.21

We found that 5-HT3A receptors are expressed in monocytes, chondrocytes, T-cells, and synovial tissue but not in dendritic cells.

Neg (not) Gene_expression (expressed) of 5-HT3A in chondrocytes

6) Confidence 0.75 Published 2004 Journal Scand. J. Rheumatol. Suppl. Section Abstract Doc Link 15515405 Disease Relevance 0.17 Pain Relevance 0.21

Therefore, we investigated the expression of the 5-HT3A receptor in primary human monocytes, chondrocytes, T-cells, dendritic cells, and synovial tissue.

Spec (investigated) Gene_expression (expression) of 5-HT3A in chondrocytes

7) Confidence 0.75 Published 2004 Journal Scand. J. Rheumatol. Suppl. Section Abstract Doc Link 15515405 Disease Relevance 0.16 Pain Relevance 0.20

Receptor binding (inhibition of [3H]-GR65630 binding) and agonist effects (stimulation of [14C]-guanidinium influx) at 5-HT3 receptors were studied in murine neuroblastoma N1E-115 cells, which express functional 5-HT3 receptors.

Gene_expression (express) of 5-HT3 in N1E-115 associated with neuroblastoma and agonist

8) Confidence 0.75 Published 2000 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 10651152 Disease Relevance 0.26 Pain Relevance 0.43

Enkephalinergic neurons express 5-HT3 receptors in the spinal cord dorsal horn: single cell RT-PCR analysis.

Gene_expression (express) of 5-HT3 in spinal cord dorsal horn associated with dorsal horn and spinal cord

9) Confidence 0.75 Published 1999 Journal Neuroreport Section Title Doc Link 10511434 Disease Relevance 0 Pain Relevance 0.91

However, that at least some airway-specific neurons express 5-HT3 receptors is supported by electrophysiologic studies [4] that showed that 10 out of 12 neurons that were retrogradely labeled by fluorescent dye injection into guinea pig airways depolarized an average of over 8 mV in response to 10 ?

Gene_expression (express) of 5-HT3 in neurons

10) Confidence 0.75 Published 2001 Journal Respir Res Section Body Doc Link PMC59581 Disease Relevance 0.05 Pain Relevance 0.28

This prompted us to examine whether enkephalinergic dorsal horn neurons express 5-HT3 receptors.

Spec (whether) Gene_expression (express) of 5-HT3 in dorsal horn associated with dorsal horn neuron

11) Confidence 0.75 Published 1999 Journal Neuroreport Section Abstract Doc Link 10511434 Disease Relevance 0 Pain Relevance 0.90

Naturally occurring variations in the human 5-HT3A gene profoundly impact 5-HT3 receptor function and expression.

Gene_expression (expression) of 5-HT3A

12) Confidence 0.65 Published 2007 Journal Pharmacogenet. Genomics Section Title Doc Link 17496724 Disease Relevance 0.37 Pain Relevance 0.14

Radioligand-binding studies with the 5-HT3 receptor antagonist [H]GR65630 were carried out to determine expression levels of heteromeric 5-HT3A/B receptors.

Spec (determine) Gene_expression (expression) of 5-HT3A

13) Confidence 0.65 Published 2008 Journal Pharmacogenet. Genomics Section Body Doc Link 18698232 Disease Relevance 0 Pain Relevance 0

These targets were subsequently classified in the 5-HT1, 5-HT2, and 5-HT3 families using specific and distinguishing agonism and especially antagonism by drugs like Bemestron and Tropisetron (for the 5-HT3 family).

Gene_expression (classified) of 5-HT3

14) Confidence 0.65 Published 2010 Journal Biochemistry Section Body Doc Link PMC2994275 Disease Relevance 0.06 Pain Relevance 0.25

The variant p.V183I decreased surface expression, whereas p.Y129S and p.S156R led to pronounced increases of 5-HT maximum responses, despite nearly unaltered surface expression levels of heteromeric 5-HT3A/B receptors.

Gene_expression (expression) of 5-HT3A

15) Confidence 0.65 Published 2008 Journal Pharmacogenet. Genomics Section Body Doc Link 18698232 Disease Relevance 0 Pain Relevance 0

Do variations in the 5-HT3A and 5-HT3B serotonin receptor genes (HTR3A and HTR3B) influence the occurrence of postoperative vomiting?

Gene_expression (genes) of 5-HT3A associated with post-operative nausea and serotonin

16) Confidence 0.65 Published 2009 Journal Anesth. Analg. Section Title Doc Link 19713259 Disease Relevance 0.47 Pain Relevance 0.32

Whole-cell patches from HEK-293 cells stably transfected with the human 5-HT3A receptor cDNA were used to determine the effects of morphine on the 5-HT-induced currents using the patch clamp technique.

Gene_expression (transfected) of 5-HT3A associated with morphine

17) Confidence 0.65 Published 2006 Journal Anesth. Analg. Section Abstract Doc Link 16931691 Disease Relevance 0.19 Pain Relevance 0.73

Quantitative autoradiography with selective radioligands was used to establish the respective distribution of serotonin 5-HT1A, 5-HT1D, 5-HT2A and 5-HT3 receptors at the cervical, thoracic and lumbar levels of the spinal cord from subjects who died at 81-94 years.

Gene_expression (distribution) of 5-HT3 in spinal cord associated with serotonin and spinal cord

18) Confidence 0.65 Published 1996 Journal J. Chem. Neuroanat. Section Abstract Doc Link 8841890 Disease Relevance 0 Pain Relevance 0.27

To further investigate the mechanisms underlying the noncompetitive inhibition of the serotonin-evoked cation current, we quantified the concentrations of different types of antidepressants and antipsychotics in fractions of sucrose flotation gradients isolated from HEK293 (human embryonic kidney 293) cells stably transfected with the 5-HT3A receptor and of N1E-115 neuroblastoma cells in relation to the localization of the 5-HT3 receptor protein within the cell membrane.

Gene_expression (transfected) of 5-HT3A in N1E-115 associated with neuroblastoma, antidepressant and serotonin

19) Confidence 0.65 Published 2005 Journal J. Neurosci. Section Abstract Doc Link 16267227 Disease Relevance 0.10 Pain Relevance 0.39

[Prevention of postoperative nausea and vomiting with highly selective 5-HT3 serotonin receptors antagonists during different types of surgery].

Gene_expression (antagonists) of 5-HT3 associated with post-operative nausea, antagonist, vomiting and serotonin

20) Confidence 0.65 Published 2002 Journal Anesteziol Reanimatol Section Title Doc Link 12611303 Disease Relevance 0.61 Pain Relevance 0.28

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