INT114126

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Context Info
Confidence 0.01
First Reported 2004
Last Reported 2004
Negated 0
Speculated 0
Reported most in Title
Documents 1
Total Number 2
Disease Relevance 0.47
Pain Relevance 2.85

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plasma membrane (APLNR, OPRL1) signal transducer activity (APLNR, OPRL1) nucleus (APLNR)
APLNR (Homo sapiens)
OPRL1 (Homo sapiens)
Pain Link Frequency Relevance Heat
antagonist 6 100.00 Very High Very High Very High
opiate 4 99.70 Very High Very High Very High
opioid receptor 2 96.32 Very High Very High Very High
orphanin 6 94.72 High High
tolerance 4 93.02 High High
Morphine 6 92.82 High High
Pain 4 92.02 High High
Antinociceptive 2 90.84 High High
Thermal hyperalgesia 6 74.20 Quite High
IPN 2 67.16 Quite High
Disease Link Frequency Relevance Heat
Nociception 2 92.56 High High
Hyperalgesia 6 74.20 Quite High
Pain 4 5.00 Very Low Very Low Very Low
Inflammatory Pain 2 5.00 Very Low Very Low Very Low

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Modification of nociception and morphine tolerance by the selective opiate receptor-like orphan receptor antagonist (-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111).

(-)-cis-1-Methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111) is a novel human opiate receptor-like orphan receptor (ORL-1) antagonist that has high affinity for the clonal human ORL-1 receptor (hORL-1 K(i) = 0.33 nM), selectivity versus mu-(174-fold), delta-(6391-fold), and kappa (486-fold)-opioid receptors and is able to inhibit nociceptin signaling via hORL-1 in a whole cell gene reporter assay.

orphan receptor Binding (affinity) of ORL-1 receptor associated with nociception, pain, opioid receptor, morphine, antagonist, orphanin, tolerance and opiate
1) Confidence 0.01 Published 2004 Journal J. Pharmacol. Exp. Ther. Section Title Doc Link 14593080 Disease Relevance 0.24 Pain Relevance 1.42
Modification of nociception and morphine tolerance by the selective opiate receptor-like orphan receptor antagonist (-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111).

(-)-cis-1-Methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111) is a novel human opiate receptor-like orphan receptor (ORL-1) antagonist that has high affinity for the clonal human ORL-1 receptor (hORL-1 K(i) = 0.33 nM), selectivity versus mu-(174-fold), delta-(6391-fold), and kappa (486-fold)-opioid receptors and is able to inhibit nociceptin signaling via hORL-1 in a whole cell gene reporter assay.

orphan receptor Binding (affinity) of hORL-1 associated with nociception, pain, opioid receptor, morphine, antagonist, orphanin, tolerance and opiate
2) Confidence 0.01 Published 2004 Journal J. Pharmacol. Exp. Ther. Section Title Doc Link 14593080 Disease Relevance 0.24 Pain Relevance 1.43

General Comments

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