INT55917

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Context Info
Confidence 0.45
First Reported 1993
Last Reported 2009
Negated 1
Speculated 2
Reported most in Body
Documents 26
Total Number 32
Disease Relevance 12.65
Pain Relevance 5.58

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

transport (Sigmar1) nuclear envelope (Sigmar1) lipid particle (Sigmar1)
endoplasmic reticulum (Sigmar1) plasma membrane (Sigmar1) nucleus (Sigmar1)
Anatomy Link Frequency
brain 4
pancreas 2
liver 1
spleen 1
Sigmar1 (Mus musculus)
Pain Link Frequency Relevance Heat
fortral 63 100.00 Very High Very High Very High
Opioid 24 99.96 Very High Very High Very High
opioid receptor 14 99.88 Very High Very High Very High
Enkephalin 2 99.82 Very High Very High Very High
antidepressant 6 98.80 Very High Very High Very High
nMDA receptor 4 98.36 Very High Very High Very High
cocaine 3 97.92 Very High Very High Very High
Potency 12 97.52 Very High Very High Very High
anticonvulsant 5 97.36 Very High Very High Very High
Central nervous system 9 97.16 Very High Very High Very High
Disease Link Frequency Relevance Heat
Apoptosis 474 99.76 Very High Very High Very High
Cancer 739 99.68 Very High Very High Very High
Neuroblastoma 11 99.68 Very High Very High Very High
Disease 185 99.58 Very High Very High Very High
Solid Tumor 6 98.80 Very High Very High Very High
Adenocarcinoma 81 98.32 Very High Very High Very High
Pancreatic Cancer 309 97.40 Very High Very High Very High
Convulsion 9 96.48 Very High Very High Very High
Drug Induced Neurotoxicity 4 95.80 Very High Very High Very High
Cognitive Disorder 59 95.64 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Originally mischaracterized as an opioid receptor, the sigma-1 receptor binds a vast number of synthetic compounds but does not bind opioid peptides; it is currently considered an orphan receptor.
sigma-1 receptor Binding (binds) of associated with opioid receptor and opioid
1) Confidence 0.45 Published 2009 Journal Science Section Abstract Doc Link 19213917 Disease Relevance 0.05 Pain Relevance 0.20
Furthermore, binding studies showed that the kinetic parameters and the inhibitory potencies of sigma receptor ligands for the binding of [3H](+)-SKF-10,047 in the mouse vas deferens were similar to those in the guinea pig brain.
sigma receptor Binding (binding) of in brain
2) Confidence 0.45 Published 1993 Journal Eur. J. Pharmacol. Section Abstract Doc Link 8449236 Disease Relevance 0 Pain Relevance 0.28
Sigma receptor binding affinity and inhibition of apomorphine-induced climbing.
Sigma receptor Binding (affinity) of associated with fortral
3) Confidence 0.44 Published 1993 Journal Eur. J. Pharmacol. Section Title Doc Link 8508904 Disease Relevance 0 Pain Relevance 0.30
The potential of Müller cells to bind sigmaR1 ligands may prove beneficial in retinal degenerative diseases such as diabetic retinopathy.


sigmaR1 Binding (bind) of
4) Confidence 0.37 Published 2006 Journal Invest. Ophthalmol. Vis. Sci. Section Body Doc Link 17122151 Disease Relevance 0 Pain Relevance 0
Furthermore, affinities for the sigma 1 and sigma 2 binding sites are presented.
sigma 1 Binding (affinities) of
5) Confidence 0.37 Published 1997 Journal Psychopharmacology (Berl.) Section Abstract Doc Link 9084057 Disease Relevance 0.57 Pain Relevance 0.49
Therefore, on the basis of these findings, these novel sigma receptor ligands were assayed, in mice, in three tests: maximal electroshock, subcutaneous pentylenetetrazol and rotarod neurotoxicity.
sigma receptor Binding (ligands) of associated with drug induced neurotoxicity
6) Confidence 0.37 Published 1997 Journal Eur. J. Pharmacol. Section Abstract Doc Link 9369382 Disease Relevance 0.19 Pain Relevance 0.19
A series of original 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives were evaluated for their affinity at sigma1 and sigma2 receptor subtypes in competition binding experiments, using [3H](+)-pentazocine or [3H]1,3-di-o-tolyl-guanidine (DTG) in the presence of 100 nM (+)-N-allylnormetazocine (NANM) in guinea-pig brain membranes.
sigma1 Binding (affinity) of in brain associated with fortral
7) Confidence 0.37 Published 1997 Journal Eur. J. Pharmacol. Section Abstract Doc Link 9369382 Disease Relevance 0 Pain Relevance 0.10
A series of original 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives were evaluated for their affinity at sigma1 and sigma2 receptor subtypes in competition binding experiments, using [3H](+)-pentazocine or [3H]1,3-di-o-tolyl-guanidine (DTG) in the presence of 100 nM (+)-N-allylnormetazocine (NANM) in guinea-pig brain membranes.
sigma2 receptor Binding (affinity) of in brain associated with fortral
8) Confidence 0.37 Published 1997 Journal Eur. J. Pharmacol. Section Abstract Doc Link 9369382 Disease Relevance 0 Pain Relevance 0.10
Compounds 2 [3-(1-piperidinopropyl)-6-propanoylbenzothiazolin-2-one] and 3 [3-(1-piperidinopropyl)-6-propanoylbenzoxazolin-2-one] still showed rather high affinities for sigma1 binding sites with Ki values of 2.3 and 8.5 nM, respectively.
sigma1 Binding (affinities) of
9) Confidence 0.37 Published 1997 Journal Eur. J. Pharmacol. Section Abstract Doc Link 9369382 Disease Relevance 0.06 Pain Relevance 0.18
With respect to sigma 1 affinity the N-benzyl derivative 2a, the N-cyclohexylmethyl derivative 2d, and the N-p-fluorobenzyl derivative 2i represent the most potent compounds of this series binding with K i values of 0.32, 0.29, and 0.62 nM, respectively.
sigma 1 Binding (binding) of
10) Confidence 0.36 Published 2008 Journal J. Med. Chem. Section Abstract Doc Link 18816044 Disease Relevance 0 Pain Relevance 0.11
In our present study, both the specific ligand of the Sigma-2 receptor (SV119) and the chemotherapies showed moderate apoptosis in all pancreas cancer cells in vitro.
Sigma-2 receptor Binding (ligand) of in pancreas associated with pancreatic cancer and apoptosis
11) Confidence 0.36 Published 2009 Journal J Transl Med Section Body Doc Link PMC2669042 Disease Relevance 1.57 Pain Relevance 0
To demonstrate the specificity of SW120 for Sigma-2 receptor binding, 10?
Sigma-2 receptor Binding (binding) of
12) Confidence 0.36 Published 2009 Journal J Transl Med Section Body Doc Link PMC2669042 Disease Relevance 0.31 Pain Relevance 0.10
Originally mischaracterized as an opioid receptor, the sigma-1 receptor binds a vast number of synthetic compounds but does not bind opioid peptides; it is currently considered an orphan receptor.
sigma-1 receptor Neg (not) Binding (bind) of associated with opioid receptor and opioid
13) Confidence 0.34 Published 2009 Journal Science Section Abstract Doc Link 19213917 Disease Relevance 0.06 Pain Relevance 0.22
Sigma-2 receptor ligand induces caspase-3/7 dependent cancer cell apoptosis
Sigma-2 receptor Binding (ligand) of associated with cancer and apoptosis
14) Confidence 0.34 Published 2007 Journal Mol Cancer Section Body Doc Link PMC1939854 Disease Relevance 0.86 Pain Relevance 0.06
Pharmacologic studies suggest that the sigma 2 ligand binding site is well conserved between rodents and primates, and we have demonstrated that sigma 2 receptor-specific ligands induce apoptosis in both mouse and human pancreas adenocarcinoma cell lines equally.
sigma 2 receptor-specific Binding (ligands) of in pancreas associated with adenocarcinoma and apoptosis
15) Confidence 0.34 Published 2007 Journal Mol Cancer Section Body Doc Link PMC1939854 Disease Relevance 0.82 Pain Relevance 0.03
Antitumor effect of sigma-2 receptor ligand in vivo
sigma-2 receptor Binding (ligand) of
16) Confidence 0.34 Published 2007 Journal Mol Cancer Section Body Doc Link PMC1939854 Disease Relevance 0.34 Pain Relevance 0
In vivo treatment with a sigma-2 receptor ligand causes tumor apoptosis with minimal effects on normal tissues
sigma-2 receptor Binding (ligand) of associated with cancer and apoptosis
17) Confidence 0.34 Published 2007 Journal Mol Cancer Section Body Doc Link PMC1939854 Disease Relevance 1.38 Pain Relevance 0.08
Single cell suspensions were incubated for 1 hour with KO5-138 (a fluorescent labeled sigma-2 receptor ligand, Figure 1) at 50 nM or 100 nM of ligand, left unstained.
sigma-2 receptor Binding (ligand) of
18) Confidence 0.29 Published 2007 Journal Mol Cancer Section Body Doc Link PMC1939854 Disease Relevance 0.26 Pain Relevance 0
Cells from spleen and pancreas exhibited higher binding capacity for sigma-2 receptor ligands at the highest dose tested (100 nM) and the spleen appeared to contain two populations of cells with regard to sigma-2 receptor ligand binding; however, even compared to the high KO5-138-binding population of splenocytes, approximately 10-fold more KO5-138 bound per cell to the syngeneic Panc-02 tumors grown in vivo (Figure 2B).
sigma-2 receptor Spec (appeared) Binding (binding) of in spleen associated with cancer
19) Confidence 0.28 Published 2007 Journal Mol Cancer Section Body Doc Link PMC1939854 Disease Relevance 0.86 Pain Relevance 0
The sigma-2 receptor and its undiscovered endogenous ligand(s) is poorly understood.
sigma-2 receptor Binding (ligand) of
20) Confidence 0.28 Published 2009 Journal J Transl Med Section Body Doc Link PMC2669042 Disease Relevance 1.40 Pain Relevance 0.03

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