INT40811

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Context Info
Confidence 0.48
First Reported 1982
Last Reported 2010
Negated 1
Speculated 1
Reported most in Abstract
Documents 26
Total Number 27
Disease Relevance 2.76
Pain Relevance 18.68

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

plasma membrane (OPRL1) signal transducer activity (OPRL1)
Anatomy Link Frequency
brain 4
CHO 2
tails 1
brain stem 1
cortex 1
OPRL1 (Homo sapiens)
Pain Link Frequency Relevance Heat
Opioid 121 100.00 Very High Very High Very High
orphanin 85 100.00 Very High Very High Very High
opioid receptor 67 100.00 Very High Very High Very High
narcan 19 100.00 Very High Very High Very High
Kappa opioid receptor 16 100.00 Very High Very High Very High
tolerance 10 100.00 Very High Very High Very High
MU agonist 7 100.00 Very High Very High Very High
opiate 6 100.00 Very High Very High Very High
Buprenorphine 182 99.98 Very High Very High Very High
antagonist 29 99.74 Very High Very High Very High
Disease Link Frequency Relevance Heat
Neuroblastoma 3 97.84 Very High Very High Very High
Pain 91 94.36 High High
Hyperalgesia 4 91.88 High High
Syndrome 3 91.80 High High
Respiratory Failure 28 88.24 High High
Nociception 8 84.48 Quite High
Substance Withdrawal Syndrome 2 78.48 Quite High
Anxiety Disorder 7 76.08 Quite High
Opiate Addiction 5 75.00 Quite High
Cough 2 75.00 Quite High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
These compounds were tested for binding affinity using [3H]N/OFQ binding to human ORL1 in CHO cells, and functional activity by measuring stimulation of [35S]GTPgammaS binding in CHO cell membranes.
ORL1 Binding (binding) of
1) Confidence 0.48 Published 2003 Journal J. Pept. Res. Section Abstract Doc Link 14531842 Disease Relevance 0 Pain Relevance 0.53
Moreover, beta-FNA (1 microM) failed to inhibit specific ORL1 receptor binding.
ORL1 receptor Binding (binding) of
2) Confidence 0.48 Published 2000 Journal Eur. J. Pharmacol. Section Abstract Doc Link 10940375 Disease Relevance 0.07 Pain Relevance 0.74
Thus, it is hypothesized that ORL1 and muR interact to form the heterodimer and that ORL1/muR heterodimerization may be one molecular basis for ORL1-mediated antiopioid effects in the brain.
ORL1 Binding (interact) of in brain
3) Confidence 0.47 Published 2005 Journal J. Neurochem. Section Abstract Doc Link 15748148 Disease Relevance 0.09 Pain Relevance 0.49
Second messenger assays further indicate that formation of ORL1/muR heterodimer selectively induces cross-desensitization of muR and impairs the potency by which [D-Ala(2),N-methyl-Phe(4),Gly-ol(5)]enkephalin (DAMGO) inhibits adenylate cyclase and stimulates p42/p44 mitogen-activated protein kinase (MAPK) phosphorylation.
ORL1 Binding (formation) of associated with enkephalin and potency
4) Confidence 0.47 Published 2005 Journal J. Neurochem. Section Abstract Doc Link 15748148 Disease Relevance 0.07 Pain Relevance 0.53
Buprenorphine, a long-acting opioid with both agonist and antagonist properties, binds to mu-opioid (OP(3)), kappa-opioid (OP(2)), delta-opioid (OP(1)), and nociceptin (ORL-1) receptors.
ORL-1 Binding (binds) of associated with long acting opioid, orphanin, antagonist, agonist, opioid and buprenorphine
5) Confidence 0.47 Published 2002 Journal CNS Drug Rev Section Abstract Doc Link 12481193 Disease Relevance 0.14 Pain Relevance 1.62
Peptide and nonpeptide ligands for the nociceptin/orphanin FQ receptor ORL1: research tools and potential therapeutic agents.
ORL1 Binding (ligands) of associated with pain and orphanin
6) Confidence 0.37 Published 2003 Journal Life Sci. Section Title Doc Link 12801588 Disease Relevance 0.23 Pain Relevance 1.05
Ligands for kappa-opioid and ORL1 receptors identified from a conformationally constrained peptide combinatorial library.
ORL1 Binding (Ligands) of associated with opioid
7) Confidence 0.37 Published 1999 Journal J. Biol. Chem. Section Title Doc Link 10488086 Disease Relevance 0 Pain Relevance 0.39
The potential interactions of natively expressed mu-opioid and opioid receptor-like (ORL1) receptors were studied by exposing intact BE(2)-C cells to agonists or antagonists for 1 h.
ORL1 Binding (interactions) of in C cells associated with antagonist, agonist, opioid receptor and opioid
8) Confidence 0.37 Published 2000 Journal Eur. J. Pharmacol. Section Abstract Doc Link 10940375 Disease Relevance 0.07 Pain Relevance 0.73
Thus, it is hypothesized that ORL1 and muR interact to form the heterodimer and that ORL1/muR heterodimerization may be one molecular basis for ORL1-mediated antiopioid effects in the brain.
ORL1 Binding (heterodimerization) of in brain
9) Confidence 0.37 Published 2005 Journal J. Neurochem. Section Abstract Doc Link 15748148 Disease Relevance 0.09 Pain Relevance 0.54
Co-immunoprecipitation experiments demonstrate that ORL1 dimerizes with muR and that intracellular C-terminal tails of ORL1 and muR are required for the formation of ORL1/muR heterodimer.
ORL1 Binding (dimerizes) of in tails
10) Confidence 0.37 Published 2005 Journal J. Neurochem. Section Abstract Doc Link 15748148 Disease Relevance 0.08 Pain Relevance 0.53
A core-promoter region functions bi-directionally for human opioid-receptor-like gene ORL1 and its 5'-adjacent gene GAIP.
ORL1 Binding (functions) of associated with opioid
11) Confidence 0.36 Published 2000 Journal J. Mol. Biol. Section Title Doc Link 11090272 Disease Relevance 0 Pain Relevance 0.19
These compounds exhibit high affinity for the nociceptin receptor, moderate to excellent selectivity over the opioid mu receptor, and behave as full agonists.
nociceptin receptor Binding (affinity) of associated with orphanin, agonist and opioid
12) Confidence 0.36 Published 2009 Journal Bioorg. Med. Chem. Lett. Section Abstract Doc Link 19339177 Disease Relevance 0.23 Pain Relevance 0.28
Human ORL1 receptors expressed in CHO cells selectively bound [125I][Tyr14]nociceptin with a Kd of 2.1 pM and a Bmax of 2.6 pmol/mg protein.
ORL1 Binding (bound) of in CHO associated with orphanin
13) Confidence 0.36 Published 1997 Journal Eur. J. Pharmacol. Section Abstract Doc Link 9384238 Disease Relevance 0 Pain Relevance 0.71
The neuropeptide was indeed identified in brain extracts as the natural ligand of a previously cloned orphan G protein-coupled receptor, the opioid receptor-like 1 (ORL1) receptor.
ORL1 Binding (ligand) of in brain associated with neuropeptide and opioid receptor
14) Confidence 0.36 Published 2003 Journal Am J Pharmacogenomics Section Abstract Doc Link 12749729 Disease Relevance 0.27 Pain Relevance 0.34
Herein we describe the pharmacological activity of a series of N-terminally modified hexapeptides with high affinity for ORL1.
ORL1 Binding (affinity) of
15) Confidence 0.36 Published 2003 Journal J. Pept. Res. Section Abstract Doc Link 14531842 Disease Relevance 0 Pain Relevance 0.52
The design of these agents was based partially on the possibility of two aryl receptor binding sites on the opiate receptor.
opiate receptor Spec (possibility) Binding (possibility) of associated with opiate
16) Confidence 0.35 Published 1982 Journal J. Med. Chem. Section Abstract Doc Link 6121915 Disease Relevance 0 Pain Relevance 0.52
The discovery of 1 as a high-affinity ligand for the nociceptin receptor has led to the synthesis of a series of tropane (8-methyl-8-azabicyclo[3.2.1]octane) derivatives as optimized ligands.
nociceptin receptor Binding (ligand) of associated with orphanin
17) Confidence 0.35 Published 2009 Journal Bioorg. Med. Chem. Lett. Section Abstract Doc Link 19339177 Disease Relevance 0.21 Pain Relevance 0.25
The molecular mechanism(s) underlying cross-tolerance between mu and opioid receptor-like 1 (ORL1) receptor agonists were investigated using two human neuroblastoma cell lines endogenously expressing these receptors and G protein-coupled receptor kinases (GRKs).
ORL1 Binding (cross-tolerance) of associated with neuroblastoma, agonist, tolerance and opioid receptor
18) Confidence 0.35 Published 2002 Journal Neuropharmacology Section Abstract Doc Link 12423667 Disease Relevance 0.10 Pain Relevance 0.19
Buprenorphine interacts with orphanin FQ/nociceptin receptor ORL-1 in the spinal cord and the brain stem.
receptor ORL-1 Binding (interacts) of in brain stem associated with orphanin, spinal cord and buprenorphine
19) Confidence 0.32 Published 2008 Journal Clinical Interventions in Aging Section Body Doc Link PMC2682375 Disease Relevance 0.08 Pain Relevance 2.49
In order to gain further insight into the functional architecture of structurally related G protein-coupled receptors, the ORL1 (nociceptin) and opioid receptors, we have constructed chimeras of ORL1 and mu-, delta- and kappa-opioid receptors, and compared their binding and functional properties with those of the parent receptors.
ORL1 Binding (binding) of associated with orphanin, kappa opioid receptor and opioid receptor
20) Confidence 0.30 Published 1998 Journal FEBS Lett. Section Abstract Doc Link 9607332 Disease Relevance 0 Pain Relevance 0.93

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