INT5916

Context Info Confidence 0.67 First Reported 1990 Last Reported 2010 Negated 1 Speculated 2 Reported most in Abstract Documents 51 Total Number 53 Disease Relevance 18.27 Pain Relevance 21.38

plasma membrane (HTR1A) signal transducer activity (HTR1A)

Anatomy Link Frequency central nervous system 2 cortex 2 medulla 2 hypothalamus 2 tail 1 HTR1A (Homo sapiens)

Pain Link Frequency Relevance Heat Serotonin 215 100.00 agonist 206 100.00 antagonist 103 100.00 Dopamine 45 100.00 Raphe 17 100.00 Opioid 15 100.00 Neuropeptide 2 99.88 midbrain 3 99.86 sSRI 144 99.84 antidepressant 133 99.78

Disease Link Frequency Relevance Heat INFLAMMATION 23 99.70 Toxocariasis 14 99.68 Suicidal Behaviour 369 99.54 Hyperalgesia 28 99.08 Obsessive-compulsive Disorder 20 99.08 Depression 203 99.00 Anxiety Disorder 329 98.96 Myoclonus 4 98.94 Headache 27 98.92 Appetite Loss 2 98.68

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Protein

Mutation

Event

Anatomy

Negation

Speculation

Pain term

Disease term

This in turn activates 5-HT1A and 5-HT1B receptors resulting in inhibition of serotonin release into the synaptic cleft.

Positive_regulation (activates) of 5-HT1A in synaptic cleft associated with serotonin

1) Confidence 0.67 Published 2010 Journal Drug design, development and therapy Section Body Doc Link PMC2846147 Disease Relevance 0.47 Pain Relevance 0.52

The onset of antidepressant action of Serotonin (5HT) selective reuptake inhibitors (SSRIs) was attributed in part to the decrease in firing activity of serotonin neurons produced by the activation of raphe 5HT1A autoreceptors at the time of treatment initiation.

Positive_regulation (activation) of 5HT1A in serotonin neurons associated with antidepressant, 5ht, raphe, ssri and serotonin

2) Confidence 0.67 Published 2003 Journal Encephale Section Abstract Doc Link 14615704 Disease Relevance 0.16 Pain Relevance 0.58

The differential regulation of 5-HT1A and 5-HT1B/D agonist responses by GDP suggests that different G-protein subtypes are involved upon 5-HT1A receptor activation by 5-HT1A and 5-HT1B/D agonists.

Positive_regulation (activation) of 5-HT1A associated with agonist

3) Confidence 0.67 Published 1998 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 9650800 Disease Relevance 0 Pain Relevance 0.42

The data support the hypothesis that activation of the 5-HT1A receptor may be relevant to the mechanism of action of serotonin reuptake inhibitors.

Positive_regulation (activation) of 5-HT1A associated with serotonin

4) Confidence 0.67 Published 1998 Journal Eur. J. Pharmacol. Section Abstract Doc Link 9593591 Disease Relevance 0 Pain Relevance 0.52

In the course of that study, we found that such treatment also alleviated the pain associated with cold sensations in the legs, insomnia, anorexia, and depression, all of which are thought to be mediated through activation of the 5-HT1A receptor.

Positive_regulation (activation) of 5-HT1A in legs associated with appetite loss, pain, depression and sleep disorders

5) Confidence 0.67 Published 2005 Journal Cerebellum Section Abstract Doc Link 16147954 Disease Relevance 1.31 Pain Relevance 0.27

Activation of 5-HT1A receptors potentiates the clonidine inhibitory effect in the locus coeruleus.

Positive_regulation (Activation) of 5-HT1A in locus coeruleus associated with locus ceruleus and clonidine

6) Confidence 0.67 Published 1997 Journal Eur. J. Pharmacol. Section Title Doc Link 9314029 Disease Relevance 0.07 Pain Relevance 0.46

The excess 5-HT produced by these antidepressant drugs in the interstitial space of the midbrain raphe activates somatodendritic 5-HT1A autoreceptors, thereby attenuating terminal 5-HT release.

Positive_regulation (activates) of 5-HT1A in midbrain associated with antidepressant, midbrain and raphe

7) Confidence 0.67 Published 1996 Journal Int Clin Psychopharmacol Section Abstract Doc Link 8923121 Disease Relevance 0 Pain Relevance 0.50

Stimulation of 5-HT1A, 5-HT1B, 5-HT2A/2C, 5-HT3 and 5-HT4 receptors or 5-HT uptake inhibition: short- and long-term memory.

Positive_regulation (Stimulation) of 5-HT1A

8) Confidence 0.67 Published 2007 Journal Behav. Brain Res. Section Title Doc Link 17692935 Disease Relevance 0 Pain Relevance 0.37

Maternally deprived animals also showed a decrease in corticosteroid receptors and an increase in 5-HT 1A and 1B receptors restricted to the CA1 region of the hippocampus.

Positive_regulation (increase) of 5-HT 1A in hippocampus associated with corticosteroid and hippocampus

9) Confidence 0.67 Published 2002 Journal Psychoneuroendocrinology Section Abstract Doc Link 11750782 Disease Relevance 0.47 Pain Relevance 0.30

Although activation of the 5-HT1a receptor exhibits proejaculatory effects, activation of the 5-HT1b and 5-HT2c receptors are involved in the process of delaying ejaculation.16,17 It has been hypothesized that altered levels of serotonin or serotonin receptor sensitivity in the ejaculatory modulating centers of the central nervous system are the pathophysiologic basis of ejaculatory disorders.17 Current treatments for PE

Positive_regulation (activation) of 5-HT1a in central nervous system associated with premature ejaculation, central nervous system and serotonin

10) Confidence 0.67 Published 2009 Journal Neuropsychiatric Disease and Treatment Section Body Doc Link PMC2695237 Disease Relevance 0.64 Pain Relevance 0.31

No differences in magnitude of the effect of the two receptor subtypes were found, indicating that stimulation of either 5-HT1A or 5-HT1B receptors was equipotent in producing the antinociceptive tail-flick response.

Positive_regulation (stimulation) of 5-HT1A in tail associated with tail-flick and antinociceptive

11) Confidence 0.67 Published 1992 Journal Psychopharmacology (Berl.) Section Abstract Doc Link 1410132 Disease Relevance 0.30 Pain Relevance 0.40

Selective activation of 5-HT1A receptors seems to cause anxiolytic and possibly antidepressive effects.

Positive_regulation (activation) of 5-HT1A associated with anxiety disorder

12) Confidence 0.67 Published 1991 Journal J Clin Psychiatry Section Abstract Doc Link 1674251 Disease Relevance 0.94 Pain Relevance 0.64

Stimulation of 5-HT1A receptors causes central sympathoinhibition and an increase in cardiac vagal drive, which results in a profound fall in blood pressure.

Positive_regulation (Stimulation) of 5-HT1A in blood associated with pressure volume 2 under development

13) Confidence 0.67 Published 1990 Journal J. Cardiovasc. Pharmacol. Section Abstract Doc Link 1702490 Disease Relevance 0.10 Pain Relevance 0.24

The use of agonists and antagonists known to discriminate among different subtypes of serotonin receptors indicated that the hyperpolarizations were produced by activation of 5-HT1A receptors and the depolarizations were generated by activation of 5-HT2 and/or 5-HT1C receptors.

Positive_regulation (activation) of 5-HT1A associated with antagonist, agonist and serotonin

14) Confidence 0.67 Published 1990 Journal Neuroscience Section Abstract Doc Link 2141111 Disease Relevance 0 Pain Relevance 0.65

The observations suggest that the sumatriptan-induced contraction of the dural artery is mediated via activation of 5-HT1D or 5-HT1-like receptors, whereas it does not appear to activate the 5-HT2 receptors.

Positive_regulation (activation) of 5-HT1-like in artery associated with sumatriptan

15) Confidence 0.64 Published 1992 Journal Cephalalgia Section Abstract Doc Link 1326402 Disease Relevance 0.17 Pain Relevance 0.50

CONCLUSIONS: This study suggests that buspirone, but not sumatriptan, the selective agonist of 5-HT1-like receptors, causes miosis in humans by activation of 5-HT1A receptors, possibly located in the central nervous system where they inhibit iris sympathetic pathways.

Positive_regulation (activation) of 5-HT1A in iris

16) Confidence 0.59 Published 1995 Journal Clin. Pharmacol. Ther. Section Body Doc Link 7697953 Disease Relevance 0 Pain Relevance 0

Opioid or 5-HT1A receptor stimulation in the RVLM, but not in the CVLM, attenuates cardiovascular responses to muscle contraction.

Positive_regulation (stimulation) of 5-HT1A in RVLM associated with toxocariasis and opioid

17) Confidence 0.49 Published 1998 Journal Neurosci Biobehav Rev Section Abstract Doc Link 9861613 Disease Relevance 1.22 Pain Relevance 0.59

Anandamide (AEA) potentiates 5-HT1A and inhibits 5-HT2A receptors supporting therapeutic efficacy in acute and preventive migraine treatment.

Positive_regulation (potentiates) of 5-HT1A

18) Confidence 0.49 Published 2004 Journal Neuro Endocrinol. Lett. Section Body Doc Link 15159679 Disease Relevance 0.26 Pain Relevance 0

The effect of 5-HT on ERK activation appeared to be mediated through the activation of 5-HT1A receptors since similar results were obtained with R-+-8-hydroxy-DPAT, a selective 5-HT1A receptor agonist and WAY100635, a selective 5-HT1A receptor antagonist, reversed the 5-HT and the R-+-8-hydroxy-DPAT effects.

Positive_regulation (activation) of 5-HT1A associated with antagonist and agonist

19) Confidence 0.49 Published 2004 Journal Life Sci. Section Abstract Doc Link 15530505 Disease Relevance 0 Pain Relevance 0.24

Building on a set-point model described previously for the hypothermic effect of 5-HT agonists, we have developed a model based on the concept of homeostatic control mechanisms, in which SSRIs exert their antidepressant effect by increasing the transduction set-point of the postsynaptic 5-HT1A receptor, and pindolol exerts its effect by increasing the rate of feedback mechanisms.

Positive_regulation (increasing) of 5-HT1A associated with antidepressant, agonist and ssri

20) Confidence 0.49 Published 2005 Journal J Pharmacokinet Pharmacodyn Section Abstract Doc Link 16307210 Disease Relevance 0 Pain Relevance 0.47

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