INT74075

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Context Info
Confidence 0.59
First Reported 1998
Last Reported 2010
Negated 1
Speculated 0
Reported most in Abstract
Documents 20
Total Number 21
Disease Relevance 4.68
Pain Relevance 8.64

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

transmembrane transport (Kcna3)
Anatomy Link Frequency
neurons 4
L929 1
PASM 1
DRG 1
Kcna3 (Rattus norvegicus)
Pain Link Frequency Relevance Heat
dorsal root ganglion 22 100.00 Very High Very High Very High
fluoxetine 75 99.98 Very High Very High Very High
tetrodotoxin 7 99.86 Very High Very High Very High
intrathecal 2 99.84 Very High Very High Very High
Spinal nerve ligature 2 99.36 Very High Very High Very High
Neuropathic pain 6 98.58 Very High Very High Very High
Glutamate receptor 2 98.16 Very High Very High Very High
qutenza 2 97.36 Very High Very High Very High
addiction 18 96.16 Very High Very High Very High
Serotonin 4 92.68 High High
Disease Link Frequency Relevance Heat
Ganglion Cysts 22 100.00 Very High Very High Very High
Hypoxia 12 99.14 Very High Very High Very High
Diabetes Mellitus 6 99.12 Very High Very High Very High
Neuropathic Pain 6 98.58 Very High Very High Very High
Hypersensitivity 6 96.40 Very High Very High Very High
Nociception 4 93.84 High High
Targeted Disruption 4 83.24 Quite High
Pain 6 78.00 Quite High
Increased Venous Pressure Under Development 2 76.32 Quite High
Diabetic Neuropathy 2 75.00 Quite High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Inhibition of Kv3.1 by fluoxetine was use-dependent.
Negative_regulation (Inhibition) of Kv3 associated with fluoxetine
1) Confidence 0.59 Published 2008 Journal J. Pharmacol. Sci. Section Abstract Doc Link 18187934 Disease Relevance 0 Pain Relevance 0.88
It is concluded that at clinically relevant concentrations, both fluoxetine and its major metabolite norfluoxetine inhibit Kv3.1, and that norfluoxetine directly inhibits Kv3.1 as an open channel blocker.
Negative_regulation (inhibits) of Kv3 associated with fluoxetine
2) Confidence 0.58 Published 2001 Journal Neuropharmacology Section Abstract Doc Link 11543764 Disease Relevance 0 Pain Relevance 0.28
The degree of inhibition of Kv3.1 by norfluoxetine was voltage-dependent.
Negative_regulation (inhibition) of Kv3
3) Confidence 0.58 Published 2001 Journal Neuropharmacology Section Abstract Doc Link 11543764 Disease Relevance 0 Pain Relevance 0.37
Norfluoxetine produced use-dependent inhibition of Kv3.1 at a frequency of 1 Hz and slowed the recovery from inactivation.
Negative_regulation (inhibition) of Kv3
4) Confidence 0.58 Published 2001 Journal Neuropharmacology Section Abstract Doc Link 11543764 Disease Relevance 0 Pain Relevance 0.28
It is concluded that at clinically relevant concentrations, both fluoxetine and its major metabolite norfluoxetine inhibit Kv3.1, and that norfluoxetine directly inhibits Kv3.1 as an open channel blocker.
Negative_regulation (inhibit) of Kv3 associated with fluoxetine
5) Confidence 0.51 Published 2001 Journal Neuropharmacology Section Abstract Doc Link 11543764 Disease Relevance 0 Pain Relevance 0.29
Fluoxetine accelerated the decay rate of inactivation of Kv3.1 currents without modifying the kinetics of current activation.
Negative_regulation (inactivation) of Kv3 associated with fluoxetine
6) Confidence 0.43 Published 2008 Journal J. Pharmacol. Sci. Section Abstract Doc Link 18187934 Disease Relevance 0 Pain Relevance 0.61
The binding (k(+1)) and dissociation (k(-1)) rate constants for fluoxetine-induced block of Kv3.1 were 5.7 microM(-1)s(-1) and 53.5 s(-1), respectively.
Negative_regulation (block) of Kv3 associated with fluoxetine
7) Confidence 0.43 Published 2008 Journal J. Pharmacol. Sci. Section Abstract Doc Link 18187934 Disease Relevance 0 Pain Relevance 0.86
In inside-out patches, norfluoxetine applied to the cytoplasmic surface inhibited Kv3.1 with an IC(50) value of 0.19+/-0.01 microM.
Negative_regulation (inhibited) of Kv3
8) Confidence 0.43 Published 2001 Journal Neuropharmacology Section Abstract Doc Link 11543764 Disease Relevance 0 Pain Relevance 0.40
The inhibition of Kv3.1 currents by both drugs was characterized by an acceleration in the apparent rate of current decay, without modification of the activation time course and with relatively fewer effects on peak amplitude.
Negative_regulation (inhibition) of Kv3
9) Confidence 0.43 Published 2001 Journal Neuropharmacology Section Abstract Doc Link 11543764 Disease Relevance 0 Pain Relevance 0.39
Quantitative RT-PCR analysis revealed that the mRNA levels of IA subunits, including Kv1.4, Kv3.4, Kv4.2, and Kv4.3, in the DRG were reduced approximately 50% in diabetic rats compared with those in control rats.
Negative_regulation (reduced) of Kv3 in DRG associated with dorsal root ganglion and diabetes mellitus
10) Confidence 0.42 Published 2010 Journal J. Neurochem. Section Abstract Doc Link 20557422 Disease Relevance 1.11 Pain Relevance 0.62
The association (k(+1)) and dissociation (k(-1)) rate constants for norfluoxetine-induced inhibition of Kv3.1 were 21.70+/-3.39 microM(-1) s(-1) and 14.68+/-3.94 s(-1), respectively.
Negative_regulation (inhibition) of Kv3
11) Confidence 0.38 Published 2001 Journal Neuropharmacology Section Abstract Doc Link 11543764 Disease Relevance 0 Pain Relevance 0.31
Fluoxetine reduced Kv3.1 whole-cell currents in a reversible, concentration-dependent manner, with an IC(50) value and a Hill coefficient of 13.4 muM and 1.4, respectively.
Negative_regulation (reduced) of Kv3 associated with fluoxetine
12) Confidence 0.37 Published 2008 Journal J. Pharmacol. Sci. Section Abstract Doc Link 18187934 Disease Relevance 0 Pain Relevance 0.48
In a neuropathic pain model induced by spinal nerve ligation in rats, the protein levels of Kv3.4 and Kv4.3 in the DRG neurons were greatly reduced.
Negative_regulation (reduced) of Kv3 in neurons associated with dorsal root ganglion, spinal nerve ligature and neuropathic pain
13) Confidence 0.35 Published 2007 Journal J. Neurosci. Section Abstract Doc Link 17855600 Disease Relevance 1.23 Pain Relevance 1.04
After Kv3.4 or Kv4.3 expression in lumbar DRG neurons was suppressed by intrathecal injections of antisense oligodeoxynucleotides, mechanical but not thermal hypersensitivity developed.
Negative_regulation (suppressed) of Kv3 in neurons associated with dorsal root ganglion, hypersensitivity and intrathecal
14) Confidence 0.35 Published 2007 Journal J. Neurosci. Section Abstract Doc Link 17855600 Disease Relevance 1.22 Pain Relevance 1.03
Hypoxia failed to inhibit any Kv1 channel, but it inhibited Kv3.1b channels expressed in L929 cells, as shown by a reduction of whole-cell current and single-channel activity, without affecting unitary conductance.
Negative_regulation (inhibited) of Kv3 in L929 associated with hypoxia
15) Confidence 0.20 Published 2000 Journal Circ. Res. Section Abstract Doc Link 10720415 Disease Relevance 0.56 Pain Relevance 0.06
Activity deprivation by glutamate receptor blockade from 10 to 20 DIV reduced both mRNAs, whereas deprivation with tetrodotoxin (TTX) reduced both mRNAs and the Kv3.2 protein.
Negative_regulation (reduced) of Kv3 associated with tetrodotoxin and glutamate receptor
16) Confidence 0.19 Published 2008 Journal Neuroscience Section Abstract Doc Link 18775767 Disease Relevance 0.08 Pain Relevance 0.25
However, chronic activity deprivation failed to alter Kv3.1b and marginally delayed Kv3.2 protein expression.
Neg (failed) Negative_regulation (delayed) of Kv3
17) Confidence 0.19 Published 2008 Journal Neuroscience Section Abstract Doc Link 18775767 Disease Relevance 0.08 Pain Relevance 0.25
Moreover, hypoxia inhibited a K(+) current in rabbit PASM cells in the presence of charybdotoxin and capsaicin, which preserve Kv3.1b while blocking most other Kv channels, but not in the presence of millimolar tetraethylammonium ions, which abolish Kv3.1b current.
Negative_regulation (abolish) of Kv3 in PASM associated with qutenza and hypoxia
18) Confidence 0.17 Published 2000 Journal Circ. Res. Section Abstract Doc Link 10720415 Disease Relevance 0.34 Pain Relevance 0.10
In COS-transfected cells, the Kv3.4 current was inhibited in a reversible manner by BDS-I, with an IC50 value of 47 nM.
Negative_regulation (inhibited) of Kv3
19) Confidence 0.04 Published 1998 Journal J. Biol. Chem. Section Abstract Doc Link 9506974 Disease Relevance 0.05 Pain Relevance 0.14
Blocking Kv3.1b and Kv3.2 currents prevents the daily rhythm in firing of SCN neurons [21].
Negative_regulation (Blocking) of Kv3 in neurons
20) Confidence 0.04 Published 2008 Journal PLoS ONE Section Body Doc Link PMC2386553 Disease Relevance 0 Pain Relevance 0

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