INT5061

Context Info Confidence 0.59 First Reported 1981 Last Reported 2011 Negated 0 Speculated 9 Reported most in Abstract Documents 306 Total Number 320 Disease Relevance 51.97 Pain Relevance 136.90

peptidase activity (Mme) plasma membrane (Mme)

Anatomy Link Frequency brain 13 plasma 7 neutrophils 6 amygdala 4 neural 3 Mme (Rattus norvegicus)

Pain Link Frequency Relevance Heat Enkephalin 575 100.00 qutenza 214 100.00 narcan 172 100.00 Morphine 146 100.00 opiate 56 100.00 withdrawal 35 100.00 Potency 33 100.00 Hippocampus 31 100.00 nociceptor 20 100.00 anesthesia 16 100.00

Disease Link Frequency Relevance Heat Reprotox - General 2 146 100.00 Stress 151 99.84 Obesity 421 99.80 Weight Gain 99 99.80 Pheochromocytoma 18 99.80 Nociception 118 99.76 Arrhythmia Under Development 2 99.76 Myocardial Infarction 44 99.66 Cough 93 99.56 Exsanguination 12 99.48

Sentences Mentioned In

Key:

Protein

Mutation

Event

Anatomy

Negation

Speculation

Pain term

Disease term

Decreased enkephalinase activity following postnatal treatment with phenobarbital.

Negative_regulation (Decreased) of enkephalinase

1) Confidence 0.59 Published 1985 Journal Neuropharmacology Section Title Doc Link 3885070 Disease Relevance 0 Pain Relevance 0.22

The treatment of the rats with phenobarbital resulted in a significant inhibition of enkephalinase A when measured in vitro, using methionine enkephalin as substrate.

Negative_regulation (inhibition) of enkephalinase associated with enkephalin

2) Confidence 0.59 Published 1985 Journal Neuropharmacology Section Abstract Doc Link 3885070 Disease Relevance 0 Pain Relevance 0.26

Chronic naloxone administration evoked progressive inhibition of enkephalinase activity that induced the morphine analgetic effect in morphine-resistant and -tolerant rats.

Negative_regulation (inhibition) of enkephalinase associated with narcan and morphine

3) Confidence 0.59 Published 1993 Journal Biull Eksp Biol Med Section Abstract Doc Link 8400186 Disease Relevance 0.21 Pain Relevance 1.87

Chronic inhibition of enkephalinase induces changes in the antinociceptive and locomotor effects of the enkephalinase inhibitor acetorphan in rats.

Negative_regulation (inhibition) of enkephalinase associated with analgesic and antinociceptive

4) Confidence 0.59 Published 1991 Journal Neuropharmacology Section Title Doc Link 1780043 Disease Relevance 0 Pain Relevance 0.35

Antinociceptive effects of ONO-9902, an enkephalinase inhibitor, after visceral stress condition in rats.

Negative_regulation (inhibitor) of enkephalinase in visceral associated with stress and antinociceptive

5) Confidence 0.59 Published 1996 Journal Can J Anaesth Section Title Doc Link 8922777 Disease Relevance 0.10 Pain Relevance 0.29

Prolonged analgesia by enkephalinase inhibition in rats with spinal cord adrenal medullary transplants.

Negative_regulation (inhibition) of enkephalinase in spinal cord associated with narcan, spinal cord and analgesia

6) Confidence 0.59 Published 1990 Journal Eur. J. Pharmacol. Section Title Doc Link 2364994 Disease Relevance 0.15 Pain Relevance 1.20

Multiple washings with buffer of the ethanol-preincubated membranous fraction of these brain structures in the control rats did not lead to a significant reduction in the activating effect of ethanol on enkephalinase A.

Negative_regulation (reduction) of enkephalinase in brain structures

7) Confidence 0.59 Published 1984 Journal Biull Eksp Biol Med Section Abstract Doc Link 6378268 Disease Relevance 0 Pain Relevance 0.22

The present experiments indicate that blocking enkephalinase activity by i.c.v. thiorphan or i.p. acetorphan results in an increased analgesic effect of electrostimulation as measured by the 50 degrees C wet tail flick test.

Negative_regulation (blocking) of enkephalinase in tail associated with analgesic and tail-flick

8) Confidence 0.59 Published 1989 Journal Life Sci. Section Abstract Doc Link 2716474 Disease Relevance 0 Pain Relevance 0.54

Inhibition of enkephalinase activity attenuates naloxone-precipitated withdrawal symptoms.

Negative_regulation (Inhibition) of enkephalinase associated with narcan and withdrawal

9) Confidence 0.59 Published 1987 Journal Gen. Pharmacol. Section Title Doc Link 3549428 Disease Relevance 0.43 Pain Relevance 0.99

Injection of small dose naloxone inhibited enkephalinase activity in brain structures and decreased morphine antibodies titres to these in control morphine-sensitive rats and therefore suppressed morphine tolerance.

Negative_regulation (inhibited) of enkephalinase in brain structures associated with tolerance, narcan and morphine

10) Confidence 0.59 Published 2000 Journal Patol Fiziol Eksp Ter Section Abstract Doc Link 10741178 Disease Relevance 0.09 Pain Relevance 1.47

Assessment of the abuse potential of acetorphan, an enkephalinase inhibitor.

Negative_regulation (inhibitor) of enkephalinase

11) Confidence 0.59 Published 1989 Journal Drug Alcohol Depend Section Title Doc Link 2702924 Disease Relevance 0.17 Pain Relevance 0.43

Thus, decrease in NEP mRNA levels preceded the changes in protein level, enzyme activity and plasma creatinine levels.

Negative_regulation (decrease) of NEP mRNA in plasma

12) Confidence 0.59 Published 1999 Journal Mol. Cell. Biochem. Section Abstract Doc Link 10485324 Disease Relevance 0.50 Pain Relevance 0.25

The different analogs varied considerably in the degree of enhancement of morphine analgesia and inhibition of enkephalinase.

Negative_regulation (inhibition) of enkephalinase associated with analgesia and morphine

13) Confidence 0.59 Published 1982 Journal Life Sci. Section Abstract Doc Link 6124860 Disease Relevance 0 Pain Relevance 1.30

The effects of nineteen AHPA* derivatives were examined on morphine analgesia by tail-flick test in rats and on enkephalinase inhibition which was based on the formation of tyrosyl-glycyl-glycine from met-enkephalin.

Negative_regulation (inhibition) of enkephalinase in tail associated with tail-flick, enkephalin, analgesia and morphine

14) Confidence 0.59 Published 1982 Journal Life Sci. Section Abstract Doc Link 6124860 Disease Relevance 0 Pain Relevance 1.06

These results are consistent with the hypothesis that high-threshold thermal and mechanical stimuli will evoke the release of an opioid in the spinal space, the metabolism of which is significantly influenced by enkephalinase inhibition.

Negative_regulation (inhibition) of enkephalinase in spinal associated with opioid

15) Confidence 0.58 Published 1990 Journal Brain Res. Section Abstract Doc Link 2357551 Disease Relevance 0.23 Pain Relevance 0.38

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 enkephalinase associated with diarrhoea

16) Confidence 0.58 Published 1987 Journal Eur. J. Pharmacol. Section Abstract Doc Link 3481337 Disease Relevance 0.10 Pain Relevance 0.07

In contrast to loperamide, a peripherally acting opiate receptor agonist, the enkephalinase inhibitors did not significantly reduce gastrointestinal transit as measured in the charcoal meal test.

Negative_regulation (inhibitors) of enkephalinase associated with agonist and opiate

17) Confidence 0.58 Published 1987 Journal Eur. J. Pharmacol. Section Abstract Doc Link 3481337 Disease Relevance 0.08 Pain Relevance 0.32

Action of enkephalinase (EC 3.4.24.11) inhibition on the pre- and post-prandial electromyographic patterns of colon in rats.

Negative_regulation (inhibition) of enkephalinase in colon associated with narcan

18) Confidence 0.58 Published 1993 Journal Neuropeptides Section Title Doc Link 8392143 Disease Relevance 0.15 Pain Relevance 0.46

Surprisingly kelatorphan, which inhibits not only enkephalinase but also aminopeptidase and dipeptidylaminopeptidase activities, was less potent than thiorphan or phosphoramidon to enhance SPLI overflow.

Negative_regulation (inhibits) of enkephalinase

19) Confidence 0.58 Published 1987 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 2445957 Disease Relevance 0 Pain Relevance 0.51

OBJECTIVE AND METHOD: The authors compared the effects of acetorphan, an enkephalinase inhibitor, with those of clonidine for the treatment of the opioid withdrawal syndrome.

Negative_regulation (inhibitor) of enkephalinase associated with withdrawal, opioid and clonidine

20) Confidence 0.58 Published 1991 Journal Am J Psychiatry Section Abstract Doc Link 2018165 Disease Relevance 0.26 Pain Relevance 0.72

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