INT20881

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Context Info
Confidence 0.43
First Reported 1990
Last Reported 2008
Negated 0
Speculated 0
Reported most in Abstract
Documents 20
Total Number 21
Disease Relevance 3.73
Pain Relevance 13.37

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 (OPRK1) signal transducer activity (OPRK1)
Anatomy Link Frequency
spinal 1
brain 1
sympathetic 1
DRG 1
prefrontal 1
OPRK1 (Homo sapiens)
Pain Link Frequency Relevance Heat
Kappa opioid receptor 96 100.00 Very High Very High Very High
agonist 70 100.00 Very High Very High Very High
antagonist 39 100.00 Very High Very High Very High
opioid receptor 20 100.00 Very High Very High Very High
cocaine 6 99.92 Very High Very High Very High
Glutamate 1 99.64 Very High Very High Very High
Delta opioid receptors 8 99.44 Very High Very High Very High
Opioid 41 99.28 Very High Very High Very High
analgesia 1 98.94 Very High Very High Very High
Buprenorphine 13 98.84 Very High Very High Very High
Disease Link Frequency Relevance Heat
Ocular Hypertension 1 99.96 Very High Very High Very High
Increased Venous Pressure Under Development 5 99.20 Very High Very High Very High
Ganglion Cysts 6 98.64 Very High Very High Very High
Death 4 98.64 Very High Very High Very High
Opiate Addiction 12 98.12 Very High Very High Very High
Schizophrenia 4 97.44 Very High Very High Very High
Manic Depressive Disorder 2 96.84 Very High Very High Very High
Overdose 1 96.16 Very High Very High Very High
Stress 2 95.48 Very High Very High Very High
Suicidal Behaviour 1 86.72 High High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
The results show that kappa-opioid selective agonists and antagonists inhibit binding of this ligand in human brain with comparable affinities and rank order as previously described for rat and guinea pig brain and the cloned kappa1-opioid receptor subtype.
Negative_regulation (inhibit) of kappa1-opioid in brain associated with antagonist, agonist, opioid receptor and opioid
1) Confidence 0.43 Published 1999 Journal Life Sci. Section Abstract Doc Link 10465345 Disease Relevance 0.15 Pain Relevance 0.55
The in vitro binding affinity (Ki) of these fluorinated ligands for the kappa opioid receptor is reduced two orders of magnitude relative to U-50488.
Negative_regulation (reduced) of kappa opioid receptor associated with kappa opioid receptor
2) Confidence 0.42 Published 1990 Journal Int J Rad Appl Instrum A Section Abstract Doc Link 2158952 Disease Relevance 0 Pain Relevance 0.38
Naltrexone did not alter rKOR mRNA levels or translational efficiency, and rKOR up-regulation was not inhibited by cycloheximide.
Negative_regulation (inhibited) of rKOR
3) Confidence 0.42 Published 2007 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 17720886 Disease Relevance 0 Pain Relevance 0.34
Tonic modulation of neurotransmitter release in the guinea-pig myenteric plexus: effect of mu and kappa opioid receptor blockade and of chronic sympathetic denervation.
Negative_regulation (blockade) of kappa opioid receptor in sympathetic associated with neurotransmitter and kappa opioid receptor
4) Confidence 0.41 Published 1995 Journal Neurosci. Lett. Section Title Doc Link 7478234 Disease Relevance 0 Pain Relevance 0.61
Redefinition of the human kappa opioid receptor gene (OPRK1) structure and association of haplotypes with opiate addiction.
Negative_regulation (Redefinition) of OPRK1 associated with addiction, kappa opioid receptor and opiate
5) Confidence 0.41 Published 2004 Journal Pharmacogenetics Section Title Doc Link 15608558 Disease Relevance 0.32 Pain Relevance 0.78
Following 4-h incubation, all three compounds induced down-regulation of the human KOR, with salvinorin A causing a lower extent of down-regulation.
Negative_regulation (down-regulation) of KOR associated with kappa opioid receptor
6) Confidence 0.41 Published 2005 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 15383632 Disease Relevance 0 Pain Relevance 0.78
Naltrexone did not alter rKOR mRNA levels or translational efficiency, and rKOR up-regulation was not inhibited by cycloheximide.
Negative_regulation (inhibited) of rKOR
7) Confidence 0.36 Published 2007 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 17720886 Disease Relevance 0 Pain Relevance 0.34
Redefinition of the human kappa opioid receptor gene (OPRK1) structure and association of haplotypes with opiate addiction.
Negative_regulation (Redefinition) of kappa opioid receptor gene associated with addiction, kappa opioid receptor and opiate
8) Confidence 0.35 Published 2004 Journal Pharmacogenetics Section Title Doc Link 15608558 Disease Relevance 0.32 Pain Relevance 0.77
Meperidine, a combined mu- and kappa-receptor agonist, also slightly increased the threshold for sweating and reduced the thresholds for vasoconstriction.
Negative_regulation (reduced) of kappa-receptor associated with agonist and increased venous pressure under development
9) Confidence 0.29 Published 1997 Journal Ann. N. Y. Acad. Sci. Section Abstract Doc Link 9100971 Disease Relevance 0.46 Pain Relevance 0.45
Overall, our data do not provide strong evidence for impaired prodynorphin or kappa opioid receptor mRNA levels in the dorsolateral prefrontal or cingulate cortices of schizophrenic, bipolar disorder, or major depressed subjects.
Negative_regulation (impaired) of kappa opioid receptor mRNA in prefrontal associated with manic depressive disorder, kappa opioid receptor and schizophrenia
10) Confidence 0.13 Published 2001 Journal Brain Res. Bull. Section Abstract Doc Link 11576758 Disease Relevance 0.79 Pain Relevance 0.27
A slightly reduced kappa-receptor affinity is observed with the propionamide (S,S)-13 (K(i) = 0.67 nM).
Negative_regulation (reduced) of kappa-receptor
11) Confidence 0.13 Published 2001 Journal J. Med. Chem. Section Abstract Doc Link 11495592 Disease Relevance 0 Pain Relevance 0.22
Most of the analogues showed sub-nanomolar potency for the kappa opioid receptor and were highly selective relative to the mu and delta opioid receptors. (-)-3-(3,4-Dihydroisoquinolin-2(1H)-yl)-N-{(1R,4S,5S,7R)-5-(3-hydroxyphenyl)-4-methyl-2-[2-(2-methylphenyl)ethyl]-2-azabicyclo[3.3.1]non-7-yl}propanamide (5n, MTHQ) is at least as potent and selective as nor-BNI as a kappa opioid receptor antagonist in the [35S]GTP-gamma-S in vitro functional test.
Negative_regulation (antagonist) of kappa opioid receptor associated with antagonist, kappa opioid receptor, delta opioid receptors and potency
12) Confidence 0.11 Published 2006 Journal J. Med. Chem. Section Abstract Doc Link 16509593 Disease Relevance 0 Pain Relevance 0.47
RATIONALE: Previous research has shown that kappa-opioid receptor agonists decrease intravenous cocaine self-administration.
Negative_regulation (decrease) of kappa-opioid receptor associated with agonist, kappa opioid receptor and cocaine
13) Confidence 0.11 Published 1999 Journal Psychopharmacology (Berl.) Section Abstract Doc Link 10435406 Disease Relevance 0 Pain Relevance 0.34
In addition to the potent agonist action of etorphine at mu-, delta- and kappa-inhibitory opioid receptors in vivo and on DRG neurons in culture, this opioid has also been shown to be a potent antagonist of excitatory mu-, delta- and kappa-receptor functions in naive and chronic morphine-treated DRG neurons.
Negative_regulation (antagonist) of kappa-receptor in DRG associated with dorsal root ganglion, antagonist, agonist, opioid receptor, opioid, morphine and immobilon
14) Confidence 0.07 Published 1996 Journal Brain Res. Section Abstract Doc Link 9001733 Disease Relevance 0.62 Pain Relevance 1.99
This is consistent with recent findings that mutation of a single serine to alanine is sufficient to block internalization and desensitization of the KOR, since this mutation removes a residue that is required for G protein receptor kinase (GRK2) phosphorylation [23].
Negative_regulation (desensitization) of KOR associated with kappa opioid receptor
15) Confidence 0.07 Published 2005 Journal BMC Biol Section Body Doc Link PMC551613 Disease Relevance 0 Pain Relevance 0.14
Buprenorphine has partial mu-opioid receptor agonist activity and is a kappa-opioid receptor antagonist; hence, it can substitute for other micro-opioid receptor agonists, yet is less apt to produce overdose reactions or dysphoria.
Negative_regulation (antagonist) of kappa-opioid receptor associated with antagonist, kappa opioid receptor, agonist, opioid receptor, overdose and buprenorphine
16) Confidence 0.07 Published 2006 Journal CNS Drugs Section Abstract Doc Link 16953647 Disease Relevance 0.42 Pain Relevance 1.61
The same dose of spiradoline resulted in a similar 47% loss of KOR from the cell surface (not shown).
Negative_regulation (loss) of KOR associated with kappa opioid receptor
17) Confidence 0.06 Published 2005 Journal BMC Biol Section Body Doc Link PMC551613 Disease Relevance 0 Pain Relevance 0.30
Kappa-opioid receptor agonists have been shown to reduce intraocular pressure in rabbits and monkeys.
Negative_regulation (reduce) of Kappa-opioid receptor associated with agonist, kappa opioid receptor and ocular hypertension
18) Confidence 0.06 Published 2001 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 11504788 Disease Relevance 0.26 Pain Relevance 0.24
It also, however, possesses kappa receptor antagonist activity making it useful not only as an analgesic, but also in opioid abuse deterrence, detoxification, and maintenance therapies.
Negative_regulation (possesses) of kappa receptor associated with analgesic, antagonist, narcan and opioid
19) Confidence 0.01 Published 2008 Journal Pain Physician Section Abstract Doc Link 18354714 Disease Relevance 0.10 Pain Relevance 1.12
Additive OL losses were evident when NorBNI was paired with toxic levels of glutamate, suggesting that kappa-receptor blockade alone is sufficient to induce OL death.
Negative_regulation (blockade) of kappa-receptor associated with glutamate and death
20) Confidence 0.01 Published 2001 Journal Glia Section Abstract Doc Link 11460271 Disease Relevance 0.29 Pain Relevance 0.70

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