INT93129

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Context Info
Confidence 0.54
First Reported 2001
Last Reported 2010
Negated 1
Speculated 1
Reported most in Abstract
Documents 42
Total Number 43
Disease Relevance 9.63
Pain Relevance 10.85

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

nuclear envelope (KCNH2) plasma membrane (KCNH2) transmembrane transport (KCNH2)
cytoplasm (KCNH2)
Anatomy Link Frequency
tail 2
margin 1
papillary muscles 1
pore 1
heart 1
KCNH2 (Homo sapiens)
Pain Link Frequency Relevance Heat
potassium channel 47 100.00 Very High Very High Very High
methadone 32 99.98 Very High Very High Very High
qutenza 20 99.98 Very High Very High Very High
Oxycodone 1 99.90 Very High Very High Very High
fluoxetine 27 99.86 Very High Very High Very High
Action potential 118 99.66 Very High Very High Very High
Buprenorphine 3 99.62 Very High Very High Very High
spastic colon 5 99.56 Very High Very High Very High
antidepressant 30 99.54 Very High Very High Very High
agonist 90 99.36 Very High Very High Very High
Disease Link Frequency Relevance Heat
Syndrome 86 99.92 Very High Very High Very High
Toxicity 12 99.68 Very High Very High Very High
Irritable Bowel Syndrome /

Irritable Bowel Syndrome Super

6 99.56 Very High Very High Very High
Cardiovascular Disorder Under Development 10 99.50 Very High Very High Very High
Functional Bowel Disorder 7 99.36 Very High Very High Very High
Arrhythmogenic Right Ventricular Dysplasia 17 98.68 Very High Very High Very High
Ovarian Cancer 62 96.88 Very High Very High Very High
Increased Venous Pressure Under Development 2 95.76 Very High Very High Very High
Arrhythmia Under Development 58 95.68 Very High Very High Very High
Vomiting 17 95.68 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Several therapeutic compounds have been identified that reduce hERG/I(Kr) currents not by direct block but by inhibition of hERG/I(Kr) trafficking to the cell surface.
Neg (not) Negative_regulation (reduce) of hERG
1) Confidence 0.54 Published 2007 Journal Biochem. Soc. Trans. Section Abstract Doc Link 17956279 Disease Relevance 0.59 Pain Relevance 0.14
We conclude that HERG current inhibition might be an explanation for the arrhythmogenic side effects of this drug.
Negative_regulation (inhibition) of HERG associated with arrhythmogenic right ventricular dysplasia
2) Confidence 0.51 Published 2002 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 11805215 Disease Relevance 0.28 Pain Relevance 0.80
Inhibition of HERG tail currents by bupivacaine (300 microm) was reduced by all mutations (P < 0.001).
Negative_regulation (Inhibition) of HERG in tail
3) Confidence 0.51 Published 2007 Journal Anesthesiology Section Body Doc Link 17325511 Disease Relevance 0 Pain Relevance 0
These observations indicate the IHERG blockade by doxepin was not highly sensitive to attenuation of HERG channel inactivation.


Negative_regulation (inactivation) of HERG
4) Confidence 0.44 Published 2007 Journal Biochem Pharmacol Section Body Doc Link PMC1920586 Disease Relevance 0 Pain Relevance 0
The therapeutic potential of blocking Eag and HERG channels non-specifically may be limited by cardiotoxicity toxicity resulting from impaired HERG channel activity in the heart.
Negative_regulation (impaired) of HERG in heart associated with toxicity and cardiovascular disorder under development
5) Confidence 0.43 Published 2010 Journal Diagn Pathol Section Body Doc Link PMC3016344 Disease Relevance 0.95 Pain Relevance 0
MA-2029 inhibited the human ether-a-go-go-related gene (hERG) current at 100 microg/ml, but shortened action potential duration (APD) in isolated guinea pig papillary muscles at 10 and 100 microg/ml and the corrected QT (QTc) interval after oral administration of 30 and 300 mg/kg in conscious telemetered dogs.
Negative_regulation (inhibited) of hERG in papillary muscles associated with action potential duration
6) Confidence 0.41 Published 2008 Journal J Toxicol Sci Section Abstract Doc Link 19043284 Disease Relevance 0.10 Pain Relevance 0.44
M (shown in Fig. 1 to produce extensive inhibition of WT IHERG with a standard [K+]e).
Negative_regulation (inhibition) of HERG
7) Confidence 0.41 Published 2007 Journal Biochem Pharmacol Section Body Doc Link PMC1920586 Disease Relevance 0 Pain Relevance 0
These results suggest that 1) bupivacaine and IQB-9302 block the open state of hKv1.5, Kv2.1, Kv4.3, and HERG channels; and 2) small differences at the N-substituent of these drugs do not affect the drug-induced block of Kv2.1, Kv4.3, or HERG, but specifically modify block of hKv1.5 channels.
Negative_regulation (block) of HERG
8) Confidence 0.41 Published 2001 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 11160646 Disease Relevance 0 Pain Relevance 0.07
The cardiotoxicity associated with unintended hERG block has prompted pharmaceutical companies to screen developmental compounds for hERG blockade and made hERG a major target in drug safety programmes.
Negative_regulation (blockade) of hERG associated with toxicity and cardiovascular disorder under development
9) Confidence 0.39 Published 2007 Journal Biochem. Soc. Trans. Section Abstract Doc Link 17956279 Disease Relevance 0.59 Pain Relevance 0.12
Direct block of hERG/I(Kr) channels by a large number of therapeutic compounds produces acLQTS [acquired LQTS (long QT syndrome)] characterized by drug-induced QT prolongation and torsades de pointes arrhythmias.
Negative_regulation (block) of hERG associated with syndrome and arrhythmia under development
10) Confidence 0.39 Published 2007 Journal Biochem. Soc. Trans. Section Abstract Doc Link 17956279 Disease Relevance 0.42 Pain Relevance 0.05
We conclude that the proarrhythmic effects of l-alpha-acetylmethadol are due to specific blockade of the HERG cardiac K(+) channel and that its active metabolite noracetylmethadol may provide a safer alternative in the treatment of opiate addiction.
Negative_regulation (blockade) of HERG associated with addiction and opiate
11) Confidence 0.39 Published 2003 Journal Eur. J. Pharmacol. Section Abstract Doc Link 12498903 Disease Relevance 0.23 Pain Relevance 0.30
These results demonstrate that LAAM and methadone can block I(HERG) in transfected cells at clinically relevant concentrations, thereby providing a plausible mechanism for the adverse cardiac effects observed in some patients receiving LAAM or methadone.
Negative_regulation (block) of HERG associated with methadone
12) Confidence 0.38 Published 2002 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 12388652 Disease Relevance 0 Pain Relevance 0.69
RESULTS: At concentrations of 0.01, 0.03, 0.1, 1 and 3 mM, r/s-methadone produced a dose-dependent inhibition of HERG by 17 +/- 5, 23 +/- 4, 40 +/- 4, 57 +/- 3, 69 +/- 3 and 80 +/- 1%, respectively.
Negative_regulation (inhibition) of HERG
13) Confidence 0.38 Published 2009 Journal Cardiology Section Body Doc Link 18984955 Disease Relevance 0 Pain Relevance 0
The antidepressant drug fluoxetine is an inhibitor of human ether-a-go-go-related gene (HERG) potassium channels.
Negative_regulation (inhibitor) of ether-a-go-go-related gene associated with antidepressant, potassium channel and fluoxetine
14) Confidence 0.38 Published 2002 Journal J. Pharmacol. Exp. Ther. Section Title Doc Link 11805215 Disease Relevance 0.24 Pain Relevance 0.90
The antidepressant drug fluoxetine is an inhibitor of human ether-a-go-go-related gene (HERG) potassium channels.
Negative_regulation (inhibitor) of HERG associated with antidepressant, potassium channel and fluoxetine
15) Confidence 0.38 Published 2002 Journal J. Pharmacol. Exp. Ther. Section Title Doc Link 11805215 Disease Relevance 0.24 Pain Relevance 0.90
CONCLUSIONS: The authors' results indicate that not only the aromatic residues Y652 and F656 but also residues residing deeper within the pore and close to the selectivity filter of HERG channels are involved in inhibition of HERG channels by the low-affinity blocker bupivacaine.


Negative_regulation (inhibition) of HERG in pore
16) Confidence 0.38 Published 2007 Journal Anesthesiology Section Body Doc Link 17325511 Disease Relevance 0 Pain Relevance 0
The mutations resulted in a change of the stereoselectivity of HERG channel block by ropivacaine.
Negative_regulation (block) of HERG
17) Confidence 0.38 Published 2005 Journal Anesthesiology Section Body Doc Link 15983462 Disease Relevance 0 Pain Relevance 0
Inhibition of the HERG channel by droperidol depends on channel gating and involves the S6 residue F656.
Negative_regulation (Inhibition) of HERG
18) Confidence 0.38 Published 2008 Journal Anesth. Analg. Section Title Doc Link 18349188 Disease Relevance 0.36 Pain Relevance 0.20
Additional studies demonstrated prominent (>50%) hERG inhibition with most (9/10) drugs despite wide APD changes (158% prolongation - 16% shortening), consistent with multi-channel block.
Negative_regulation (inhibition) of hERG
19) Confidence 0.38 Published 2004 Journal J. Cardiovasc. Pharmacol. Section Abstract Doc Link 15076220 Disease Relevance 0.06 Pain Relevance 0.13
The present study identifies doxepin as both an IHERG-blocker for which channel inactivation does not play a major role in drug binding and as an additional drug that is an effective inhibitor of N588K–HERG.
Negative_regulation (inhibitor) of HERG
20) Confidence 0.37 Published 2007 Journal Biochem Pharmacol Section Body Doc Link PMC1920586 Disease Relevance 0.18 Pain Relevance 0

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