INT9231

Context Info Confidence 0.47 First Reported 1990 Last Reported 2009 Negated 3 Speculated 0 Reported most in Abstract Documents 27 Total Number 27 Disease Relevance 7.29 Pain Relevance 13.04

plasma membrane (Htr3a) cytoplasm (Htr3a)

Anatomy Link Frequency brain 2 neurons 2 ileum 1 visceral 1 vagus nerve 1 Htr3a (Rattus norvegicus)

Pain Link Frequency Relevance Heat antagonist 68 100.00 agonist 52 100.00 Serotonin 44 100.00 5HT 23 100.00 opiate 3 100.00 nMDA receptor 1 100.00 mu opioid receptor 1 100.00 Pain 15 99.64 trigeminal ganglion 1 99.48 noradrenaline 14 99.44

Disease Link Frequency Relevance Heat Frailty 4 99.68 Pain 12 99.64 Amnesia 3 99.26 Ganglion Cysts 2 99.04 Depression 50 99.00 Irritable Bowel Syndrome / Irritable Bowel Syndrome Super 20 98.90 Post-operative Nausea 4 98.40 Irritable Bowel Syndrome / Irritable Bowel Syndrome Super / Visceral Pain 1 98.08 Stress 9 97.40 Sleep Disorders 3 97.36

Sentences Mentioned In

Key:

Protein

Mutation

Event

Anatomy

Negation

Speculation

Pain term

Disease term

Numerous works have demonstrated an interaction between 5-HT3 receptor antagonists and some of the effects of ethanol (EtOH) using biochemical, electrophysiological, and behavioral techniques.

5-HT3 Binding (interaction) of associated with antagonist

1) Confidence 0.47 Published 1997 Journal Alcohol Section Abstract Doc Link 9014026 Disease Relevance 0.21 Pain Relevance 0.24

Interaction between opiate and 5-HT3 receptor antagonists in the regulation of alcohol intake.

5-HT3 Binding (Interaction) of associated with antagonist, opiate and alcohol

2) Confidence 0.47 Published 1994 Journal Alcohol Alcohol Suppl Section Title Doc Link 8974381 Disease Relevance 0 Pain Relevance 0.47

From these results, 10e appears to interact selectively with 5-HT3 receptors in the gastrointestinal system and might be effective in the therapy of irritable bowel syndrome (IBS).

5-HT3 Binding (interact) of in gastrointestinal system associated with spastic colon

3) Confidence 0.47 Published 1993 Journal J. Med. Chem. Section Abstract Doc Link 8230119 Disease Relevance 0.66 Pain Relevance 0.34

This study examined whether the antinociception produced following the intrathecal (i.t.) administration of serotonin (5-hydroxytryptamine, 5-HT) and other 5-HT receptor agonists in a model of visceral pain that utilizes colorectal distension (CRD) as the noxious visceral stimulus is mediated through interaction with spinal 5-HT1, 5-HT2, or 5-HT3 receptor subtypes.

5-HT3 Binding (interaction) of in visceral associated with antinociception, visceral pain, agonist, serotonin and intrathecal

4) Confidence 0.47 Published 1991 Journal Brain Res. Section Abstract Doc Link 2018933 Disease Relevance 0 Pain Relevance 0.59

Behavioral evidence suggests that 5-HT3 receptors interact with mesolimbic dopamine (DA) systems and that 5-HT3 antagonists can interfere with the hyperlocomotive effects of amphetamine and cocaine and the rewarding and stimulus effects of morphine, nicotine and ethanol.

5-HT3 Binding (interact) of associated with dopamine, nicotine, antagonist, morphine and cocaine

5) Confidence 0.47 Published 1991 Journal Psychopharmacology (Berl.) Section Abstract Doc Link 1780417 Disease Relevance 0 Pain Relevance 0.84

In-vitro binding studies revealed that alverine citrate had a high affinity for 5-HT1A receptors and a weak affinity for 5-HT3 and 5-HT4 subtypes.

5-HT3 Binding (affinity) of

6) Confidence 0.47 Published 2001 Journal J. Pharm. Pharmacol. Section Abstract Doc Link 11697552 Disease Relevance 0.30 Pain Relevance 0.37

Chronic citalopram or fluoxetine did not significantly affect the binding of [3H]BRL-43694 to 5-HT3 receptors in the rat brain cortex.

5-HT3 Binding (binding) of in brain associated with fluoxetine

7) Confidence 0.47 Published 1997 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 9228186 Disease Relevance 0 Pain Relevance 0.47

Serotonin3 (5-HT3) receptors can affect motor control through an interaction with the nigrostriatal dopamine (DA) neurons, but the neurochemical basis for this interaction remains controversial.

5-HT3 Binding (interaction) of in neurons associated with dopamine

8) Confidence 0.36 Published 2003 Journal Eur. J. Neurosci. Section Abstract Doc Link 12603267 Disease Relevance 0 Pain Relevance 0.41

Ibogaine and its metabolite noribogaine have low microM affinities for kappa and mu opioid receptors, NMDA receptors, 5HT-3 receptors, sigma-2 sites, sodium channels and the serotonin transporter. 18-MC has low microM affinities at all three opioid receptors and at 5HT-3 receptors but much lower or no affinities for NMDA and sigma-2 receptors, sodium channels, and the 5HT transporter.

5HT-3 Binding (affinities) of associated with nmda receptor, sodium channel, 5ht, mu opioid receptor, opioid receptor and serotonin

9) Confidence 0.36 Published 2000 Journal Ann. N. Y. Acad. Sci. Section Abstract Doc Link 10911925 Disease Relevance 0.31 Pain Relevance 1.01

The present study aimed to investigate the interaction between the coexistent SP receptor and 5-HT3 receptor in trigeminal ganglion (TG) neurons using whole-cell patch clamp technique.

5-HT3 Binding (interaction) of in neurons associated with ganglion cysts and trigeminal ganglion

10) Confidence 0.36 Published 2004 Journal Neurosci. Lett. Section Abstract Doc Link 15245797 Disease Relevance 0.17 Pain Relevance 0.20

Differential mediation of descending pain facilitation and inhibition by spinal 5HT-3 and 5HT-7 receptors.

5HT-3 Neg (inhibition) Binding (inhibition) of in spinal associated with pain and 5ht

11) Confidence 0.36 Published 2009 Journal Brain Res. Section Title Doc Link 19427839 Disease Relevance 0.45 Pain Relevance 1.56

The receptors contributing to 5-hydroxytryptamine (5-HT)-induced secretion by rat ileum were investigated in-vitro using selective agonists and antagonists. 5-HT induced a dose-dependent increase in the short-circuit current (SCC) generated by both intact and stripped sheets of rat ileum. 1-Phenylbiguanide, a selective 5-HT3 agonist, and 5-methoxytryptamine, an agonist that lacks affinity for 5-HT3 receptors, also increased the SCC.

5-HT3 Binding (affinity) of in ileum associated with antagonist and agonist

12) Confidence 0.36 Published 1997 Journal J. Pharm. Pharmacol. Section Abstract Doc Link 9401948 Disease Relevance 0 Pain Relevance 0.33

In both intact and stripped jejunum 5-HT and 5-methoxytryptamine, an agonist that lacks affinity for 5-HT3 receptors, induced concentration-dependent increases in the short-circuit current (SCC), although 5-methoxytryptamine induced a smaller maximum response.

5-HT3 Binding (affinity) of in jejunum associated with agonist

13) Confidence 0.36 Published 1998 Journal J. Pharm. Pharmacol. Section Abstract Doc Link 9643448 Disease Relevance 0 Pain Relevance 0.31

1-(m-Chlorophenyl)-biguanide (mCPBG) was examined and compared with three 5-HT3 receptor agonists in three 5-HT3 receptor models. mCPBG inhibited [3H]GR67330 binding to 5-HT3 receptors with high affinity (IC50 1.5 nM). mCPBG depolarized the rat vagus nerve with an EC50 one tenth of that for 5-HT (0.05 vs. 0.46 microM); the maximum depolarization was approximately half that for 5-HT.

5-HT3 Binding (binding) of in vagus nerve associated with agonist and vagus nerve

14) Confidence 0.36 Published 1990 Journal Eur. J. Pharmacol. Section Abstract Doc Link 2144822 Disease Relevance 0 Pain Relevance 0.20

Interestingly, amoxapine binds with a good affinity (IC50 = 0.30 microM) to 5-HT3 receptors labelled by [3H]zacopride in cortical membranes.

5-HT3 Binding (binds) of

15) Confidence 0.36 Published 1991 Journal Encephale Section Abstract Doc Link 1666997 Disease Relevance 0 Pain Relevance 0.38

The 5-HT1A and 5-HT3 agonists, 8-OH-DPAT and 2-methyl-5-HT, respectively, produced only transient responses by themselves and did not interact with PGE2 or NA.

5-HT3 Binding (interact) of in PGE2 associated with noradrenaline and agonist

16) Confidence 0.35 Published 1996 Journal Neuropharmacology Section Abstract Doc Link 8684602 Disease Relevance 0.48 Pain Relevance 0.89

In radioligand binding assays, brofaromine exhibited weak or no interaction with alpha 1- and alpha 2-noradrenergic, 5-HT1, 5-HT2, 5-HT3, cholinergic, histamine H1 and H2, mu-opiate, GABAA, benzodiazepine, adenosine, neurotensin, and substance P receptors.

5-HT3 Neg (no) Binding (interaction) of associated with adenocard, opiate and substance p

17) Confidence 0.35 Published 1993 Journal Clin Neuropharmacol Section Abstract Doc Link 8313393 Disease Relevance 0 Pain Relevance 0.40

In-vitro binding studies revealed that alverine citrate had a high affinity for 5-HT1A receptors and a weak affinity for 5-HT3 and 5-HT4 subtypes.

5-HT3 Binding (affinity) of

18) Confidence 0.35 Published 2001 Journal J. Pharm. Pharmacol. Section Abstract Doc Link 11697552 Disease Relevance 0.24 Pain Relevance 0.31

Overall, these results suggest that the increase in AmPFc DA levels by NMQ is probably not mediated by its interaction with the 5-HT3 receptor.

5-HT3 receptor Binding (interaction) of associated with dopamine

19) Confidence 0.32 Published 1996 Journal Synapse Section Abstract Doc Link 10638822 Disease Relevance 0 Pain Relevance 0.47

Ligand binding at the 5-HT3-receptor causes manifold effects on other neurotransmitter and neuropeptide systems.

5-HT3-receptor Binding (binding) of associated with neurotransmitter and neuropeptide

20) Confidence 0.30 Published 2000 Journal Scand. J. Rheumatol. Suppl. Section Abstract Doc Link 11028830 Disease Relevance 1.11 Pain Relevance 1.00

General Comments

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