INT5539

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Context Info
Confidence 0.59
First Reported 1980
Last Reported 2010
Negated 0
Speculated 2
Reported most in Abstract
Documents 75
Total Number 93
Disease Relevance 28.91
Pain Relevance 41.84

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 (Mme) plasma membrane (Mme)
Anatomy Link Frequency
lung 9
plasma 7
brain 5
vas deferens 2
Cleavage 1
Mme (Mus musculus)
Pain Link Frequency Relevance Heat
narcan 83 100.00 Very High Very High Very High
Pain 42 100.00 Very High Very High Very High
headache 12 100.00 Very High Very High Very High
Enkephalin 180 99.90 Very High Very High Very High
Antinociceptive 88 99.84 Very High Very High Very High
Morphine 27 99.80 Very High Very High Very High
Analgesic 72 99.72 Very High Very High Very High
Endogenous opioid 20 99.60 Very High Very High Very High
intrathecal 10 99.60 Very High Very High Very High
Pain threshold 5 99.60 Very High Very High Very High
Disease Link Frequency Relevance Heat
Adult Respiratory Distress Syndrome 1584 99.92 Very High Very High Very High
Targeted Disruption 11 99.88 Very High Very High Very High
Adverse Drug Reaction 2 99.84 Very High Very High Very High
Pain 24 99.60 Very High Very High Very High
Syndrome 1 99.40 Very High Very High Very High
Hyperalgesia 12 99.30 Very High Very High Very High
Diarrhoea 22 99.08 Very High Very High Very High
Lung Injury 234 98.96 Very High Very High Very High
Osteogenic Sarcomas 4 98.72 Very High Very High Very High
Injury 254 98.56 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Enkephalinase inhibition by thiorphan and subsequent response of ethanol, normorphine and enkephalins on mouse vas deferens.
Negative_regulation (inhibition) of Enkephalinase in vas deferens associated with enkephalin
1) Confidence 0.59 Published 1986 Journal Funct. Neurol. Section Title Doc Link 3301556 Disease Relevance 0 Pain Relevance 0.27
It is suggested that increased saturation of the opioid receptors by endogenous opioid peptides following enkephalinase inhibition, might suppress the severity of the withdrawal syndrome.
Negative_regulation (inhibition) of enkephalinase associated with endogenous opioid, opioid receptor and withdrawal
2) Confidence 0.59 Published 1986 Journal Arch Int Pharmacodyn Ther Section Abstract Doc Link 3539055 Disease Relevance 0.26 Pain Relevance 0.66
SCH 32615, an enkephalinase inhibitor, enhances pregnancy-induced analgesia in mice.
Negative_regulation (inhibitor) of enkephalinase associated with analgesic and analgesia
3) Confidence 0.59 Published 1995 Journal Anesth. Analg. Section Title Doc Link 7726437 Disease Relevance 0 Pain Relevance 0.72
SCH 32615, an enkephalinase inhibitor, significantly enhanced this analgesia.


Negative_regulation (inhibitor) of enkephalinase
4) Confidence 0.59 Published 1995 Journal Anesthesiology Section Body Doc Link 7741304 Disease Relevance 0 Pain Relevance 0
Enkephalinase inhibition: regulation of ethanol intake in genetically predisposed mice.
Negative_regulation (inhibition) of Enkephalinase
5) Confidence 0.58 Published 1987 Journal Alcohol Section Title Doc Link 2829941 Disease Relevance 0.09 Pain Relevance 0.38
The significant decrease in the NEP enzymatic activity in the lung of mice with ALI was associated with a lower level of its gene expression in the lung, suggesting that the downregulation of NEP activity was due to its decreased expression at the transcriptional level responsible for ALI/ARDS.
Negative_regulation (downregulation) of NEP in lung associated with adult respiratory distress syndrome
6) Confidence 0.58 Published 2010 Journal Respir Res Section Body Doc Link PMC3009633 Disease Relevance 1.14 Pain Relevance 0.04
Decreased amounts of NEP protein in the lung were also confirmed by Western immunoblot analysis.
Negative_regulation (Decreased) of NEP protein in lung
7) Confidence 0.58 Published 2010 Journal Respir Res Section Body Doc Link PMC3009633 Disease Relevance 1.01 Pain Relevance 0.09
This downregulation of NEP activity may contribute to the inactivation of the tachykinins degradation pathway and to uncontrolled inflammation in ALI/ARDS, and in other neurogenic respiratory diseases [9,24-26].
Negative_regulation (downregulation) of NEP in respiratory associated with inflammation, adult respiratory distress syndrome and respiratory disease
8) Confidence 0.58 Published 2010 Journal Respir Res Section Body Doc Link PMC3009633 Disease Relevance 1.17 Pain Relevance 0.05
Carfecillin was a competitive inhibitor of enkephalinase from mouse brain striata (IC50 = 207 + 57 nM, cf thiorphan 10.6 +/- 1.9 nM) but did not inhibit other known enkephalin- degrading enzymes.
Negative_regulation (inhibitor) of enkephalinase in brain associated with enkephalin
9) Confidence 0.58 Published 1989 Journal J. Enzym. Inhib. Section Abstract Doc Link 2489237 Disease Relevance 0 Pain Relevance 0.44
Compounds (26) and (16) represent the first combined inhibitors of enkephalinase and aminopeptidase MII.
Negative_regulation (inhibitors) of enkephalinase
10) Confidence 0.58 Published 1991 Journal J. Enzym. Inhib. Section Abstract Doc Link 1669442 Disease Relevance 0 Pain Relevance 0.34
The antinociceptive effect seen with (26) reflects its ranking in vitro as an inhibitor of enkephalinase (Ki = 0.14 microM) but it is possible that this effect is not totally opioid-mediated.
Negative_regulation (inhibitor) of enkephalinase associated with opioid and antinociceptive
11) Confidence 0.58 Published 1991 Journal J. Enzym. Inhib. Section Abstract Doc Link 1669442 Disease Relevance 0 Pain Relevance 0.35
In this study, a rather new compound, Thiorphan, was examined, which displays an antinociceptive activity by inhibiting enkephalinase activity.
Negative_regulation (inhibiting) of enkephalinase associated with antinociceptive
12) Confidence 0.58 Published 1983 Journal AJNR Am J Neuroradiol Section Abstract Doc Link 6224405 Disease Relevance 0.75 Pain Relevance 0.45
Oral administration of BL-2401 to mice significantly inhibited the enkephalinase activity in the striatum and also potentiated the antinociceptive effect of (D-Ala2,Met5)-enkephalin given intracisternally.
Negative_regulation (inhibited) of enkephalinase in striatum associated with enkephalin and antinociceptive
13) Confidence 0.57 Published 1997 Journal Jpn. J. Pharmacol. Section Abstract Doc Link 9469639 Disease Relevance 0.16 Pain Relevance 0.90
As for the mechanism of the action, the active metabolite of BL-2401, BL-2240 ((+/-)-3-(2-benzyl-3-mercaptopropionyl) amino-5-methylbenzoic acid), selectively inhibited enkephalinase in vitro (IC50: 5.2 nM).
Negative_regulation (inhibited) of enkephalinase
14) Confidence 0.57 Published 1997 Journal Jpn. J. Pharmacol. Section Abstract Doc Link 9469639 Disease Relevance 0.16 Pain Relevance 0.90
These findings indicate that BL-2401 is an orally active enkephalinase inhibitor and may produce antinociceptive and antidepressant-like effects in association with endogenous opioid systems.
Negative_regulation (inhibitor) of enkephalinase associated with antidepressant, endogenous opioid and antinociceptive
15) Confidence 0.57 Published 1997 Journal Jpn. J. Pharmacol. Section Abstract Doc Link 9469639 Disease Relevance 0.14 Pain Relevance 0.88
Antinociceptive and antidepressant-like profiles of BL-2401, a novel enkephalinase inhibitor, in mice and rats.
Negative_regulation (inhibitor) of enkephalinase associated with antidepressant and antinociceptive
16) Confidence 0.57 Published 1997 Journal Jpn. J. Pharmacol. Section Title Doc Link 9469639 Disease Relevance 0.15 Pain Relevance 1.10
Intracerebroventricular (icv) injection of 3 in mice leads to a high potentiation of the analgesic effect of the exogenously administered D-Ala2-Met-enkephalin, evidencing the in vivo inhibition of enkephalinase.
Negative_regulation (inhibition) of enkephalinase associated with analgesic, enkephalin and intracerebroventricular
17) Confidence 0.55 Published 1983 Journal J. Med. Chem. Section Abstract Doc Link 6298420 Disease Relevance 0 Pain Relevance 0.86
Intracerebroventricular injection in mice of these mixed inhibitors, especially kelatorphan, led to naloxone reversible analgesic responses (hot-plate test) that were slightly better than those produced by a mixture of thiorphan and bestatin, two potent inhibitors of enkephalinase and aminopeptidase, respectively.
Negative_regulation (inhibitors) of enkephalinase associated with analgesic, narcan and intracerebroventricular
18) Confidence 0.55 Published 1985 Journal J. Med. Chem. Section Abstract Doc Link 3897541 Disease Relevance 0 Pain Relevance 0.66
On the other hand, a decrease in NEP activity in plasma has been reported during septic shock, a major cause of ALI/ARDS [21].
Negative_regulation (decrease) of NEP in plasma associated with adult respiratory distress syndrome and sepsis
19) Confidence 0.51 Published 2010 Journal Respir Res Section Body Doc Link PMC3009633 Disease Relevance 0.88 Pain Relevance 0
Cleavage of the fluorescent substrate was suppressed in presence of thiorphan, a relatively specific inhibitor of NEP, which inhibits a few enzymes other than NEP.
Negative_regulation (inhibitor) of NEP in Cleavage
20) Confidence 0.51 Published 2010 Journal Respir Res Section Body Doc Link PMC3009633 Disease Relevance 0.79 Pain Relevance 0

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