INT86602

From wiki-pain
Jump to: navigation, search
Context Info
Confidence 0.36
First Reported 1999
Last Reported 2010
Negated 3
Speculated 2
Reported most in Body
Documents 14
Total Number 18
Disease Relevance 4.65
Pain Relevance 2.58

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
pore 1
oocytes 1
KCNH2 (Homo sapiens)
Pain Link Frequency Relevance Heat
local anesthetic 6 99.98 Very High Very High Very High
qutenza 12 99.84 Very High Very High Very High
agonist 237 99.78 Very High Very High Very High
opioid receptor 3 99.60 Very High Very High Very High
potassium channel 19 96.16 Very High Very High Very High
Potency 12 89.72 High High
Neuropathic pain 1 86.00 High High
Mexiletine 6 80.48 Quite High
fluoxetine 1 79.20 Quite High
antidepressant 3 77.12 Quite High
Disease Link Frequency Relevance Heat
Syndrome 179 99.48 Very High Very High Very High
Death 7 99.20 Very High Very High Very High
Nonsyndromic Deafness 2 98.80 Very High Very High Very High
Pressure Volume 2 Under Development 2 97.24 Very High Very High Very High
Cancer 29 96.72 Very High Very High Very High
Shock 8 94.24 High High
Cv General 2 Under Development 7 92.24 High High
Toxicity 5 92.00 High High
Cardiovascular Disorder Under Development 4 91.64 High High
Leukemia 2 89.12 High High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Nevertheless, given the presence of a significant component of IHERG blockade with brief depolarization and incomplete attenuation of inhibition by the Y652A and F656A mutations, we cannot exclude the possibilities that a proportion of the observed blockade with doxepin involves binding outside of the channel pore, or binding to closed HERG channels.


HERG Binding (binding) of in pore
1) Confidence 0.36 Published 2007 Journal Biochem Pharmacol Section Body Doc Link PMC1920586 Disease Relevance 0.07 Pain Relevance 0.03
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.
hERG Binding (trafficking) of
2) Confidence 0.34 Published 2007 Journal Biochem. Soc. Trans. Section Abstract Doc Link 17956279 Disease Relevance 0.59 Pain Relevance 0.15
This has led both LQT2 (also at risk while resting) and LQT3 patients to be saved by a family member, such as the spouse sleeping in the same bed.
LQT2 Binding (saved) of
3) Confidence 0.33 Published 2008 Journal Orphanet J Rare Dis Section Body Doc Link PMC2474834 Disease Relevance 0.41 Pain Relevance 0.14
BACKGROUND: Local anesthetics interact with human ether-a-go-go-related gene (HERG) channels via the aromatic amino acids Y652 and F656 in the S6 region.
HERG Binding (interact) of associated with local anesthetic
4) Confidence 0.31 Published 2007 Journal Anesthesiology Section Abstract Doc Link 17325511 Disease Relevance 0 Pain Relevance 0.10
BACKGROUND: Local anesthetics interact with human ether-a-go-go-related gene (HERG) channels via the aromatic amino acids Y652 and F656 in the S6 region.
ether-a-go-go-related gene Binding (interact) of associated with local anesthetic
5) Confidence 0.31 Published 2007 Journal Anesthesiology Section Abstract Doc Link 17325511 Disease Relevance 0 Pain Relevance 0.10
Local anesthetic interaction with human ether-a-go-go-related gene (HERG) channels: role of aromatic amino acids Y652 and F656.
ether-a-go-go-related gene Binding (interaction) of associated with local anesthetic
6) Confidence 0.31 Published 2005 Journal Anesthesiology Section Title Doc Link 15983462 Disease Relevance 0 Pain Relevance 0.24
Local anesthetic interaction with human ether-a-go-go-related gene (HERG) channels: role of aromatic amino acids Y652 and F656.
HERG Binding (interaction) of associated with local anesthetic
7) Confidence 0.31 Published 2005 Journal Anesthesiology Section Title Doc Link 15983462 Disease Relevance 0 Pain Relevance 0.24
However, recently a monoclonal Eag antibody has been developed which specifically inhibits proliferation based on its Eag blockade with no interaction with HERG channels and has been postulated as a potential therapeutic for the treatment of cancer [22].
HERG Neg (no) Binding (interaction) of associated with cancer
8) Confidence 0.27 Published 2010 Journal Diagn Pathol Section Body Doc Link PMC3016344 Disease Relevance 0.98 Pain Relevance 0
Indeed, QT interval duration, genotype and gender are significantly associated with the outcome with a QTc interval >500ms, and a LQT2 or LQT3 genotype determining the worst prognosis.
LQT2 Spec (determining) Binding (associated) of
9) Confidence 0.25 Published 2008 Journal Indian Pacing and Electrophysiology Journal Section Body Doc Link PMC2363724 Disease Relevance 0.92 Pain Relevance 0
In conclusion, capsaicin blocks hERG channels by binding to both the closed and open channel states.Y652 was important as a molecular determinant of blockade.
hERG Spec (determinant) Binding (binding) of associated with qutenza
10) Confidence 0.22 Published 2010 Journal Eur. J. Pharmacol. Section Abstract Doc Link 19903464 Disease Relevance 0 Pain Relevance 0.79
METHODS: Using the 2-microelectrode voltage clamp technique we investigated the interaction of P and NP with HERG channels, expressed in Xenopus oocytes.
HERG Binding (interaction) of in oocytes
11) Confidence 0.15 Published 1999 Journal Cardiovasc. Res. Section Body Doc Link 10690289 Disease Relevance 0 Pain Relevance 0
It was selective for the sigma1 receptor over more than 60 other receptors, ion channels and neurotransmitter transporters, and did not interact with the human ether-a-go-go-related gene (hERG) cardiac potassium channel.
hERG Neg (not) Binding (interact) of
12) Confidence 0.08 Published 2009 Journal J. Pharm. Pharmacol. Section Body Doc Link 19406002 Disease Relevance 0 Pain Relevance 0
It was selective for the sigma1 receptor over more than 60 other receptors, ion channels and neurotransmitter transporters, and did not interact with the human ether-a-go-go-related gene (hERG) cardiac potassium channel.
ether-a-go-go-related Neg (not) Binding (interact) of
13) Confidence 0.07 Published 2009 Journal J. Pharm. Pharmacol. Section Body Doc Link 19406002 Disease Relevance 0 Pain Relevance 0
In addition, two homozygous HERG mutations have been associated with severe LQTS with functional atrioventricular conduction anomalies in young children.
HERG Binding (associated) of associated with syndrome
14) Confidence 0.05 Published 2001 Journal Circ. Res. Section Abstract Doc Link 11463728 Disease Relevance 1.13 Pain Relevance 0
The advantage of compound 7aa was that it showed the potential for an improved cardiosafety profile due to its low affinity for hERG.
hERG Binding (affinity) of
15) Confidence 0.03 Published 2010 Journal The Open Medicinal Chemistry Journal Section Body Doc Link PMC3023065 Disease Relevance 0.06 Pain Relevance 0.17
7 nAChR agonist.‡ This compound showed low affinity for hERG (IC50=40,000 nM) and high affinity binding to ?
hERG Binding (affinity) of associated with agonist
16) Confidence 0.02 Published 2010 Journal The Open Medicinal Chemistry Journal Section Body Doc Link PMC3023065 Disease Relevance 0.20 Pain Relevance 0.19
7 nAChR agonist.‡ This compound showed low affinity for hERG (IC50=40,000 nM) and high affinity binding to ?
hERG Binding (affinity) of associated with agonist
17) Confidence 0.02 Published 2010 Journal The Open Medicinal Chemistry Journal Section Body Doc Link PMC3023065 Disease Relevance 0.20 Pain Relevance 0.16
2,4-Diaminopyridine delta-opioid receptor agonists and their associated hERG pharmacology.
hERG Binding (associated) of associated with agonist and opioid receptor
18) Confidence 0.01 Published 2009 Journal Bioorg. Med. Chem. Lett. Section Title Doc Link 19231185 Disease Relevance 0.09 Pain Relevance 0.28

General Comments

This test has worked.

Personal tools
Namespaces

Variants
Actions
Navigation
Toolbox