INT18258

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Context Info
Confidence 0.56
First Reported 1984
Last Reported 2010
Negated 0
Speculated 1
Reported most in Abstract
Documents 20
Total Number 21
Disease Relevance 1.60
Pain Relevance 8.61

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

peptidase activity (Thop1) cytoplasm (Thop1)
Anatomy Link Frequency
brain 3
tail 1
caudate-putamen 1
cleavage 1
epithelium 1
Thop1 (Rattus norvegicus)
Pain Link Frequency Relevance Heat
Enkephalin 67 100.00 Very High Very High Very High
Analgesic 18 100.00 Very High Very High Very High
narcan 10 100.00 Very High Very High Very High
Pain 2 98.52 Very High Very High Very High
Antinociceptive 3 96.84 Very High Very High Very High
tail-flick 3 96.48 Very High Very High Very High
Opioid 7 96.44 Very High Very High Very High
Eae 1 95.08 Very High Very High Very High
depression 3 94.84 High High
Neuropeptide 8 93.68 High High
Disease Link Frequency Relevance Heat
Urological Neuroanatomy 5 99.92 Very High Very High Very High
Natriuresis 3 99.44 Very High Very High Very High
Pain 2 98.52 Very High Very High Very High
Diarrhoea 2 98.12 Very High Very High Very High
Depression 3 94.84 High High
Opiate Addiction 3 89.48 High High
Schizophrenia 9 77.52 Quite High
Dementia 1 71.32 Quite High
Hypothermia 1 59.68 Quite High
Tremor 1 51.92 Quite High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
The data suggest that inhibition of the metalloendopeptidase decreases the rate of degradation of endogenous enkephalins, however the analgesic properties of the inhibitors do not seem to be related to their inhibitory potencies.
Negative_regulation (inhibition) of metalloendopeptidase associated with analgesic and enkephalin
1) Confidence 0.56 Published 1984 Journal Eur. J. Pharmacol. Section Abstract Doc Link 6383843 Disease Relevance 0 Pain Relevance 0.97
The enzyme responsible for the cleavage has an optimal substrate length of 8-13 amino acids and is inhibited by N-[1-(RS)-carboxy-2-phenylethyl]-Ala-Ala-Phe-p-aminobenzoate, a site-directed inhibitor of the metalloendopeptidase EC 3.4.24.15.
Negative_regulation (inhibitor) of metalloendopeptidase EC 3.4.24.15 in cleavage
2) Confidence 0.51 Published 1990 Journal J. Neurochem. Section Abstract Doc Link 1968961 Disease Relevance 0 Pain Relevance 0.53
Thimet oligopeptidase--a review of a thiol dependent metallo-endopeptidase also known as Pz-peptidase endopeptidase 24.15 and endo-oligopeptidase.
Negative_regulation (review) of metallo-endopeptidase
3) Confidence 0.41 Published 1993 Journal Biol. Chem. Hoppe-Seyler Section Title Doc Link 8471182 Disease Relevance 0 Pain Relevance 0.07
Intraperitoneal administration of N-[1-(R,S)-carboxy-2-phenylethyl-Phe-p-aminobenzoate, synthesized in this laboratory as a potent inhibitor of membrane-bound metalloendopeptidase (EC 3.4.24.11) caused a prolonged but weak analgesic effect on rats as measured by the tail flick test.
Negative_regulation (inhibitor) of metalloendopeptidase in tail associated with analgesic and tail-flick
4) Confidence 0.41 Published 1984 Journal Eur. J. Pharmacol. Section Abstract Doc Link 6383843 Disease Relevance 0 Pain Relevance 0.59
For this purpose, the responses induced by RB 38A, a mixed inhibitor of enkephalin catabolism, and RB 38B, a selective inhibitor of neutral endopeptidase EC 3.4.24.11, were compared with the antidepressive effect induced by imipramine.
Negative_regulation (inhibitor) of endopeptidase EC 3.4.24.11 associated with enkephalin
5) Confidence 0.41 Published 1993 Journal Biol. Psychiatry Section Abstract Doc Link 8373929 Disease Relevance 0.17 Pain Relevance 0.68
Inhibitors of an enkephalin degrading membrane-bound metalloendopeptidase: analgesic properties and effects on striatal enkephalin levels.
Negative_regulation (Inhibitors) of metalloendopeptidase associated with analgesic and enkephalin
6) Confidence 0.41 Published 1984 Journal Eur. J. Pharmacol. Section Title Doc Link 6383843 Disease Relevance 0 Pain Relevance 1.24
Substrate-related potent inhibitors of brain metalloendopeptidase.
Negative_regulation (inhibitors) of metalloendopeptidase in brain
7) Confidence 0.38 Published 1988 Journal Biochemistry Section Title Doc Link 3162384 Disease Relevance 0 Pain Relevance 0.30
Metalloendopeptidase 24.15 activity was decreased in the caudate-putamen after acute haloperidol and increased in the frontal cortex after acute apomorphine administration; however, no effect was noted after subchronic administration of either drug.
Negative_regulation (decreased) of Metalloendopeptidase in caudate-putamen associated with urological neuroanatomy
8) Confidence 0.36 Published 1996 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 8613907 Disease Relevance 0.37 Pain Relevance 0.32
Thimet oligopeptidase--a review of a thiol dependent metallo-endopeptidase also known as Pz-peptidase endopeptidase 24.15 and endo-oligopeptidase.
Negative_regulation (review) of Thimet oligopeptidase
9) Confidence 0.36 Published 1993 Journal Biol. Chem. Hoppe-Seyler Section Title Doc Link 8471182 Disease Relevance 0 Pain Relevance 0.07
The conversion of enkephalin-containing peptides into enkephalins was virtually completely inhibited by N-[1-(R,S)-carboxy-2-phenylethyl]-Ala-Ala-Phe-p-aminobenzoate, a specific active-site-directed inhibitor of endopeptidase-24.15, indicating that this enzyme was responsible for the observed interconversions.
Negative_regulation (inhibitor) of endopeptidase-24.15 associated with enkephalin
10) Confidence 0.35 Published 1987 Journal J. Neurochem. Section Abstract Doc Link 2878974 Disease Relevance 0 Pain Relevance 0.78
Thiorphan and acetorphan, two potent inhibitors of enkephalinase (EC 3.4.24.11 membrane-metalloendopeptidase) significantly reduced the castor oil-induced diarrhea in rats when administered intravenously (or orally, for acetorphan) but not when administered intracerebroventricularly.
Negative_regulation (inhibitors) of EC 3.4.24.11 membrane-metalloendopeptidase associated with diarrhoea
11) Confidence 0.32 Published 1987 Journal Eur. J. Pharmacol. Section Abstract Doc Link 3481337 Disease Relevance 0.10 Pain Relevance 0.15
The antibody raised against recombinant endooligopeptidase A specifically inhibited its own activity and reduced the thiol-activated oligopeptidase activity of rabbit brain cytosol to less than 30%.
Negative_regulation (reduced) of oligopeptidase in brain
12) Confidence 0.30 Published 2000 Journal Biochem. Biophys. Res. Commun. Section Abstract Doc Link 10694468 Disease Relevance 0 Pain Relevance 0.21
Neutral metalloendopeptidase (NEP) inhibitors delay atrial natriuretic factor (ANF) catabolism and potentiate biological responses to ANF.
Negative_regulation (inhibitors) of Neutral metalloendopeptidase associated with natriuresis
13) Confidence 0.22 Published 1993 Journal Am. J. Hypertens. Section Abstract Doc Link 8512660 Disease Relevance 0.17 Pain Relevance 0.07
We investigated the effects of thiorphan, a selective inhibitor of endopeptidase 24.11 'enkephalinase', kelatorphan ((R)-3-(N-hydroxy-carboxamido-2-benzylpropanoyl)-L-alanine), and RB 38 A ((R)-3-(N-hydroxycarboxamido-2-benzylpropanoyl)-L-phenylalanine) two almost complete inhibitors of enkephalin metabolism, on the naloxone-precipitated morphine withdrawal syndrome in rats.
Spec (investigated) Negative_regulation (inhibitor) of endopeptidase 24.11 associated with narcan, enkephalin, withdrawal and morphine
14) Confidence 0.20 Published 1989 Journal Eur. J. Pharmacol. Section Abstract Doc Link 2776828 Disease Relevance 0.35 Pain Relevance 0.49
In contrast, the formation of YGG was completely prevented by Thiorphan (IC50 value = 9 nM) and phosphoramidon, two inhibitors of "enkephalinase" (EC 3.4.24.11; membrane metallo-endopeptidase), thus identifying the latter as the YGG-forming enzyme.
Negative_regulation (inhibitors) of metallo-endopeptidase
15) Confidence 0.13 Published 1986 Journal Peptides Section Abstract Doc Link 3532054 Disease Relevance 0 Pain Relevance 0.46
The relationships between various properties of inhibitors of enkephalinase (membrane metalloendopeptidase, EC 3.4.24.11) i.e., enzyme inhibition, protection of endogenous enkephalins, antinociceptive activity and stimulation of locomotor activity was investigated by comparing the relative potencies of the two enantiomers of Thiorphan and acetorphan, its parenterally active prodrug.
Negative_regulation (inhibitors) of metalloendopeptidase associated with eae, enkephalin and antinociceptive
16) Confidence 0.04 Published 1987 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 3479550 Disease Relevance 0 Pain Relevance 0.27
In addition, our data suggest that T4 treatment to prematurely born neonates should be reconsidered in order to compensate for the maternal TH deficiency, and thus preventing THOP.


Negative_regulation (preventing) of THOP
17) Confidence 0.03 Published 2010 Journal Cerebral Cortex (New York, NY) Section Body Doc Link PMC2871377 Disease Relevance 0.20 Pain Relevance 0.11
We conclude that the effects of exogenous and endogenous tachykinins are enhanced by removal of epithelium and by inhibition of metalloendopeptidase and cyclooxygenase, suggesting that tachykinins may be degraded by epithelial enzymes, and may release relaxant prostanoids in airways.
Negative_regulation (inhibition) of metalloendopeptidase in epithelium
18) Confidence 0.02 Published 1989 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 2464059 Disease Relevance 0 Pain Relevance 0.39
Selective inhibitors of this metalloendopeptidase could be useful in the treatment of pain with a spectrum of activity similar to that of opioids (139).
Negative_regulation (inhibitors) of metalloendopeptidase associated with pain and opioid
19) Confidence 0.01 Published 2005 Journal Evidence-based Complementary and Alternative Medicine Section Body Doc Link PMC1193547 Disease Relevance 0.24 Pain Relevance 0.58
Peptide retro-inverso modification was applied to the complete hydroxamate inhibitors of the three zinc metallopeptidases (neutral endopeptidase 24-11 (NEP, EC 3.4.24.11), aminopeptidase N (APN, EC 3.4.11.2), and a dipeptidylaminopeptidase (DAP) involved in the in vitro enkephalin degradation by brain tissues.
Negative_regulation (inhibitors) of endopeptidase 24-11 in brain associated with enkephalin
20) Confidence 0.01 Published 1988 Journal J. Med. Chem. Section Abstract Doc Link 2900898 Disease Relevance 0 Pain Relevance 0.20

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