INT89925

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Context Info
Confidence 0.75
First Reported 2000
Last Reported 2010
Negated 1
Speculated 0
Reported most in Body
Documents 22
Total Number 24
Disease Relevance 9.63
Pain Relevance 4.21

This is a graph with borders and nodes. Maybe there is an Imagemap used so the nodes may be linking to some Pages.

nucleoplasm (NR1I2) signal transduction (NR1I2) nucleus (NR1I2)
Anatomy Link Frequency
liver 3
CAR 2
kidney 2
intestine 2
brain 1
NR1I2 (Homo sapiens)
Pain Link Frequency Relevance Heat
antagonist 12 100.00 Very High Very High Very High
nerve block 1 99.80 Very High Very High Very High
dexamethasone 4 99.44 Very High Very High Very High
Inflammation 16 99.28 Very High Very High Very High
Analgesic 14 98.84 Very High Very High Very High
agonist 27 98.48 Very High Very High Very High
cINOD 54 97.52 Very High Very High Very High
Acute pain 1 96.60 Very High Very High Very High
adenocard 6 95.60 Very High Very High Very High
Pain 11 95.40 Very High Very High Very High
Disease Link Frequency Relevance Heat
Colon Cancer 155 99.80 Very High Very High Very High
INFLAMMATION 28 99.28 Very High Very High Very High
Fever 23 98.92 Very High Very High Very High
Nicotine Addiction 267 98.76 Very High Very High Very High
Pain 14 96.60 Very High Very High Very High
Nociception 1 93.80 High High
Osteoporosis 186 93.40 High High
Hypercalcemia 90 88.80 High High
Hemorrhage 1 85.48 High High
Heart Disease 1 84.40 Quite High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
We report the synthesis and SAR of a series of novel azaindole CB(2) agonists. 6-Azaindole 18 showed activity in an acute pain model but was inactive in a chronic model. 18 is a Pgp substrate with low brain penetration.
Gene_expression (synthesis) of SAR in brain associated with acute pain and agonist
1) Confidence 0.75 Published 2009 Journal J. Med. Chem. Section Abstract Doc Link 19743867 Disease Relevance 0.17 Pain Relevance 0.37
The synthesis and SAR of a series of indazole TRPV1 antagonists leading to the discovery of 21 (ABT-116) is described.
Gene_expression (synthesis) of SAR associated with antagonist
2) Confidence 0.75 Published 2010 Journal Bioorg. Med. Chem. Lett. Section Abstract Doc Link 20457518 Disease Relevance 0 Pain Relevance 0.16
We found no statistically significant associations between the PXR and LXR polymorphisms and CRC risk, and no interaction with smoking status, use of NSAID, or intake of red and processed meat.
Gene_expression (polymorphisms) of PXR associated with nicotine addiction, colon cancer and cinod
3) Confidence 0.67 Published 2010 Journal BMC Cancer Section Body Doc Link PMC2949803 Disease Relevance 0.79 Pain Relevance 0.10
The expression of human MDR1 is regulated by pregnane X receptor (PXR) and nuclear factor-?
Gene_expression (pregnane) of PXR
4) Confidence 0.67 Published 2010 Journal BMC Cancer Section Body Doc Link PMC2949803 Disease Relevance 1.21 Pain Relevance 0.26
Herein, we describe the design, synthesis, SAR studies, biological data, physicochemical properties and pharmacokinetics of this 4-piperidinylaniline series.
Gene_expression (synthesis) of SAR
5) Confidence 0.65 Published 2000 Journal Drug Des Discov Section Abstract Doc Link 10928451 Disease Relevance 0 Pain Relevance 0.16
The synthesis and SAR of a series of indazole TRPV1 antagonists leading to the discovery of 21 (ABT-116) is described.
Gene_expression (described) of SAR associated with antagonist
6) Confidence 0.65 Published 2010 Journal Bioorg. Med. Chem. Lett. Section Abstract Doc Link 20457518 Disease Relevance 0 Pain Relevance 0.17
This review focuses on the A(1) adenosine receptor (A(1)AR) ligands, both agonists and antagonists, appeared in the literature in the last few years, together with their potential therapeutic application, pointing the attention on their chemical structures and SAR (Structure Activity Relationship) and also reporting new findings on preclinical or clinical trials of some important A(1)AR ligands synthesized in the past.
Gene_expression (synthesized) of SAR associated with adenocard, antagonist and agonist
7) Confidence 0.65 Published 2010 Journal Curr Top Med Chem Section Abstract Doc Link 20370661 Disease Relevance 0.46 Pain Relevance 0.59
Structure-based design of benzimidazole sugar conjugates: synthesis, SAR and in vivo anti-inflammatory and analgesic activities.
Gene_expression (synthesis) of SAR associated with inflammation and analgesic
8) Confidence 0.65 Published 2009 Journal Med Chem Section Title Doc Link 19673695 Disease Relevance 0.10 Pain Relevance 0.64
Exposure of cell lines expressing PAR(2) and PAR(4) to trypsin IV increased [Ca(2+)](i) and strongly desensitized cells to PAR agonists, whereas there were no responses in cells lacking these receptors.
Gene_expression (expressing) of PAR associated with agonist
9) Confidence 0.58 Published 2004 Journal J. Biol. Chem. Section Abstract Doc Link 14726524 Disease Relevance 0.10 Pain Relevance 0.27
The SAR leading to the discovery of 6 is presented in this report.
Gene_expression (presented) of SAR
10) Confidence 0.58 Published 2008 Journal Bioorg. Med. Chem. Section Abstract Doc Link 18722778 Disease Relevance 0.27 Pain Relevance 0.51
The expression of human MDR1 is regulated by pregnane X receptor (PXR) and nuclear factor-?
Gene_expression (pregnane) of X receptor
11) Confidence 0.58 Published 2010 Journal BMC Cancer Section Body Doc Link PMC2949803 Disease Relevance 1.16 Pain Relevance 0.26
We consider that evaluation of the necessary precautions, such as the obturator nerve block, for the prevention of the ONR is important even in the surgery using the TURis system.
Neg (prevention) Gene_expression (prevention) of ONR in obturator nerve associated with nerve block
12) Confidence 0.58 Published 2010 Journal Masui Section Abstract Doc Link 20229762 Disease Relevance 0.22 Pain Relevance 0.17
The PXR shares 60% homology in their DNA binding domains with the vitamin D receptor (VDRs) and is expressed in intestine, kidney and liver.
Gene_expression (expressed) of PXR in liver
13) Confidence 0.47 Published 2006 Journal Nutr Metab (Lond) Section Body Doc Link PMC1586194 Disease Relevance 0.50 Pain Relevance 0.08
In patients with equivocal results a repeat SXR was made 48 hours later unless the fever had resolved or another cause of fever had been found.
Gene_expression (made) of SXR associated with fever
14) Confidence 0.43 Published 2005 Journal Crit Care Section Body Doc Link PMC1297630 Disease Relevance 0.43 Pain Relevance 0
The PXR shares 60% homology in their DNA binding domains with the vitamin D receptor (VDRs) and is expressed in intestine, kidney and liver.
Gene_expression (expressed) of PXR in liver
15) Confidence 0.40 Published 2006 Journal Nutr Metab (Lond) Section Body Doc Link PMC1586194 Disease Relevance 0.50 Pain Relevance 0.08
Gene expression of LXR (p < 0.001) and GR (p < 0.01) in BAL cells of smokers (Figure 2) was up to three times that of nonsmokers, whereas expression of the cytosolic AHR and PXR was similar.
Gene_expression (expression) of PXR associated with nicotine addiction
16) Confidence 0.28 Published 2006 Journal Environ Health Perspect Section Body Doc Link PMC1665420 Disease Relevance 0.54 Pain Relevance 0
GR-activating concentrations of glucocorticoid transactivated SULT2A transcription indirectly, through intermediary steps involving GR-inducible liver-enriched CCAAT enhancer binding protein [128], while pharmacological concentrations of dexamethasone induced rat hepatic SULT2A expression via a PXR-mediated mechanism [127].
Gene_expression (expression) of PXR in liver associated with dexamethasone
17) Confidence 0.24 Published 2009 Journal PPAR Research Section Body Doc Link PMC2724710 Disease Relevance 0 Pain Relevance 0.08
The expression of AHR, LXR, PXR and GR was not different in BBs of both study groups.
Gene_expression (expression) of PXR
18) Confidence 0.22 Published 2006 Journal Environ Health Perspect Section Body Doc Link PMC1665420 Disease Relevance 0.58 Pain Relevance 0
We therefore studied expression of the aryl hydrocarbon receptor (AHR), constitutive androstane receptor (CAR), pregnane X receptor (PXR), liver X receptor (LXR), and glucocorticoid receptor (GR) (Gibson et al. 2002; Tirona et al. 2003) for their established role in CYP gene regulation in BAL cells and BBs derived from smokers and nonsmokers.
Gene_expression (expression) of PXR in CAR associated with nicotine addiction
19) Confidence 0.22 Published 2006 Journal Environ Health Perspect Section Body Doc Link PMC1665420 Disease Relevance 0.56 Pain Relevance 0
The PXR shares 60% homology in their DNA binding domains with the vitamin D receptor (VDRs) and is expressed in intestine, kidney and liver.
Gene_expression (expressed) of PXR in kidney
20) Confidence 0.16 Published 2006 Journal Nutr Metab (Lond) Section Body Doc Link PMC1586194 Disease Relevance 0.50 Pain Relevance 0.08

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