INT23675

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Context Info
Confidence 0.37
First Reported 1983
Last Reported 1998
Negated 0
Speculated 0
Reported most in Abstract
Documents 18
Total Number 19
Disease Relevance 0.50
Pain Relevance 10.74

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

signal transduction (Chrna7) plasma membrane (Chrna7) cytoplasm (Chrna7)
Anatomy Link Frequency
cerebral cortex 2
Chrna7 (Rattus norvegicus)
Pain Link Frequency Relevance Heat
local anesthetic 78 99.84 Very High Very High Very High
lidocaine 18 99.84 Very High Very High Very High
tetrodotoxin 15 99.10 Very High Very High Very High
Opioid 6 98.76 Very High Very High Very High
sodium channel 54 98.60 Very High Very High Very High
Potency 12 98.24 Very High Very High Very High
cerebral cortex 10 97.16 Very High Very High Very High
addiction 1 94.16 High High
antagonist 8 88.96 High High
cocaine 6 85.00 Quite High
Disease Link Frequency Relevance Heat
Overactive Bladder 6 100.00 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Another ligand specific for the BTX sodium channel receptor, batrachotoxinin-A 20-alpha-benzoate (BTX-B), competitively inhibited the specific binding of [3H]BTX-OAB.
Negative_regulation (inhibited) of BTX-OAB Binding (binding) of associated with sodium channel and overactive bladder
1) Confidence 0.37 Published 1993 Journal Toxicon Section Abstract Doc Link 8266344 Disease Relevance 0.50 Pain Relevance 0.35
These sites could be differentiated by means of the divalent cations Mg2+ and Ca2+, that inhibit BTX-B binding completely.
Negative_regulation (inhibit) of BTX-B Binding (binding) of
2) Confidence 0.35 Published 1988 Journal Eur. J. Pharmacol. Section Abstract Doc Link 2450762 Disease Relevance 0 Pain Relevance 0.38
The rank order and relative potency of the local anesthetics tested in both paradigms were similar with the exception of lidocaine ethiodide, which was 18 times more potent as an inhibitor of binding of [3H]BTX-B than it was as an inhibitor of BTX-elicited depolarization.
Negative_regulation (inhibitor) of BTX-B Binding (binding) of associated with lidocaine, local anesthetic and potency
3) Confidence 0.34 Published 1983 Journal Mol. Pharmacol. Section Abstract Doc Link 6300644 Disease Relevance 0 Pain Relevance 0.83
A series of 14 local anesthetics was shown to inhibit the specific binding of [3H]BTX-B with Ki values ranging from 0.6 microM for dibucaine to 400 microM for benzocaine.
Negative_regulation (inhibit) of BTX-B Binding (binding) of associated with local anesthetic
4) Confidence 0.34 Published 1983 Journal Mol. Pharmacol. Section Abstract Doc Link 6300644 Disease Relevance 0 Pain Relevance 0.91
Compounds with local anesthetic activity inhibit the binding of [3H]BTX-B by a mutually exclusive, allosteric mechanism.
Negative_regulation (inhibit) of BTX-B Binding (binding) of associated with local anesthetic
5) Confidence 0.25 Published 1985 Journal Neuropeptides Section Abstract Doc Link 2582303 Disease Relevance 0 Pain Relevance 0.84
The potential local anesthetic potency of a series of 23 opioids and phencyclidine-like compounds has been estimated by their inhibition of [3H]BTX-B binding to Na+ channels in a preparation of synaptoneurosomes from guinea pig cerebral cortex.
Negative_regulation (inhibition) of BTX-B Binding (binding) of in cerebral cortex associated with cerebral cortex, opioid, potency and local anesthetic
6) Confidence 0.25 Published 1985 Journal Neuropeptides Section Abstract Doc Link 2582303 Disease Relevance 0 Pain Relevance 0.98
Ethanol inhibited the specific binding of [3H]BTX-B in a vesicular preparation with an IC50 value of 310 mM and a Hill number of 1.0.
Negative_regulation (inhibited) of BTX-B Binding (binding) of
7) Confidence 0.21 Published 1988 Journal Eur. J. Pharmacol. Section Abstract Doc Link 2450767 Disease Relevance 0 Pain Relevance 0.24
The sodium channel activators veratridine and aconitine and the local anesthetic dibucaine inhibited specific [3H]BTX-B binding at both 7 degrees C and 27 degrees C. 4.
Negative_regulation (inhibited) of BTX-B Binding (binding) of associated with sodium channel and local anesthetic
8) Confidence 0.17 Published 1993 Journal Comp. Biochem. Physiol. C, Comp. Pharmacol. Toxicol. Section Abstract Doc Link 8103729 Disease Relevance 0 Pain Relevance 0.22
The dihydropyrazole insecticide RH 3421 inhibited specific [3H]BTX-B binding at 7 degrees C but had no effect on specific binding at 27 degrees C.
Negative_regulation (inhibited) of BTX-B Binding (binding) of
9) Confidence 0.17 Published 1993 Journal Comp. Biochem. Physiol. C, Comp. Pharmacol. Toxicol. Section Abstract Doc Link 8103729 Disease Relevance 0 Pain Relevance 0.21
However, in the presence of batrachotoxin, tetracaine inhibited the batrachotoxin-dependent increase in scorpion toxin binding (KD = 2.0 microM) in a dose-dependent manner, suggesting that inhibition of [3H]BTX-B binding by local anesthetics does not occur through binding at the scorpion toxin binding site.
Negative_regulation (inhibition) of BTX-B Binding (binding) of associated with local anesthetic
10) Confidence 0.08 Published 1984 Journal Mol. Pharmacol. Section Abstract Doc Link 6321944 Disease Relevance 0 Pain Relevance 0.78
This reduction in receptor affinity in the presence of local anesthetics appears to be due, at least in part, to an increased rate of ligand dissociation from the receptor-ligand complex, suggesting an indirect allosteric mechanism for the inhibition of [3H]BTX-B binding by local anesthetics.
Negative_regulation (inhibition) of BTX-B Binding (binding) of associated with local anesthetic
11) Confidence 0.08 Published 1984 Journal Mol. Pharmacol. Section Abstract Doc Link 6321944 Disease Relevance 0 Pain Relevance 0.87
The inhibition of [3H]BTX-B binding by lidocaine was reversible within 30 min when samples were diluted from 10(-3)M to 10(-4) M lidocaine.
Negative_regulation (inhibition) of BTX-B Binding (binding) of associated with lidocaine
12) Confidence 0.08 Published 1984 Journal Mol. Pharmacol. Section Abstract Doc Link 6321944 Disease Relevance 0 Pain Relevance 0.85
A plot of log KD from these binding experiments against log K0.5 for inhibition of sodium currents by local anesthetics from electrophysiological experiments yielded a regression line with a slope of 0.84 and a correlation coefficient, r, of 0.86, demonstrating that the inhibition of [3H]BTX-B binding by local anesthetics occurs within a concentration range of physiological relevance.
Negative_regulation (inhibition) of BTX-B Binding (binding) of associated with local anesthetic
13) Confidence 0.08 Published 1984 Journal Mol. Pharmacol. Section Abstract Doc Link 6321944 Disease Relevance 0 Pain Relevance 0.65
Yohimbine inhibited the specific binding of [3H]BTX-B in the vesicular preparation with an IC50 value of 2.2 X 10(-5) M.
Negative_regulation (inhibited) of BTX-B Binding (binding) of
14) Confidence 0.07 Published 1988 Journal Biochem. Pharmacol. Section Abstract Doc Link 2449217 Disease Relevance 0 Pain Relevance 0.30
We conclude that micro1-N434K and micro1-L437K residues located near the middle of the I-S6 segment of Na+ channels can reduce the LA binding affinity without BTX.
Negative_regulation (reduce) of BTX Binding (affinity) of
15) Confidence 0.06 Published 1998 Journal Mol. Pharmacol. Section Abstract Doc Link 9687581 Disease Relevance 0 Pain Relevance 0.23
Our results show that LA binding in BTX-resistant micro1 Na+ channels was reduced significantly.
Negative_regulation (reduced) of BTX Binding (binding) of
16) Confidence 0.06 Published 1998 Journal Mol. Pharmacol. Section Abstract Doc Link 9687581 Disease Relevance 0 Pain Relevance 0.28
Scatchard analysis of BTX-B binding isotherms at 25 degrees C in the presence and absence of 1 microM TTX revealed that inhibition is due to a 3-fold decrease in the affinity of BTX-B binding with no change in the number of binding sites (Bmax).
Negative_regulation (decrease) of BTX Binding (binding) of associated with tetrodotoxin
17) Confidence 0.02 Published 1986 Journal J. Neurosci. Section Abstract Doc Link 2426426 Disease Relevance 0 Pain Relevance 0.88
They are 15 times less potent in inhibiting [3H]BTX-B binding and 2.5 times less potent in inhibiting veratridine-induced depolarization than yohimbine.
Negative_regulation (inhibiting) of BTX-B Binding (binding) of
18) Confidence 0.02 Published 1988 Journal Neuropharmacology Section Abstract Doc Link 2905027 Disease Relevance 0 Pain Relevance 0.42
Both of the compounds inhibited the [3H]BTX-B binding with an IC50 of (approximately) 150 microM, which is more than four orders of magnitude higher than the concentration required for antagonism of a presynaptic alpha 2-adrenoceptor (7 nM).
Negative_regulation (inhibited) of BTX-B Binding (binding) of
19) Confidence 0.02 Published 1988 Journal Neuropharmacology Section Abstract Doc Link 2905027 Disease Relevance 0 Pain Relevance 0.51

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