INT768

Context Info Confidence 0.70 First Reported 1977 Last Reported 2010 Negated 3 Speculated 12 Reported most in Abstract Documents 179 Total Number 192 Disease Relevance 40.05 Pain Relevance 156.93

plasma membrane (Oprl1) signal transducer activity (Oprl1)

Anatomy Link Frequency brain 13 spinal 10 dorsal root ganglia 5 spinal cord 4 blood 3 Oprl1 (Rattus norvegicus)

Pain Link Frequency Relevance Heat orphanin 514 100.00 Opioid 320 100.00 Pain 289 100.00 Kappa opioid receptor 245 100.00 opiate 241 100.00 opioid receptor 239 100.00 agonist 206 100.00 Analgesic 200 100.00 narcan 158 100.00 Dynorphin 79 100.00

Disease Link Frequency Relevance Heat Stress 35 100.00 Natriuresis 27 100.00 Urological Neuroanatomy 26 100.00 INFLAMMATION 56 99.96 Dystonia 1 99.96 Diuresis 4 99.92 Nociception 46 99.90 Nervous System Injury 13 99.88 Cognitive Disorder 11 99.84 Neuroblastoma 7 99.84

Sentences Mentioned In

Key:

Protein

Mutation

Event

Anatomy

Negation

Speculation

Pain term

Disease term

Expression levels of the mRNA for the kappa-opioid receptor, as detected by reverse transcription-polymerase chain reaction followed by Southern blot analysis, were significantly increased in the cerebral cortex, striatum, and midbrain, including thalamus, hippocampus, and pons, in animals dependent on butorphanol.

Positive_regulation (increased) of kappa-opioid receptor in midbrain associated with butorphanol, kappa opioid receptor, hippocampus, thalamus, midbrain and cerebral cortex

1) Confidence 0.70 Published 2005 Journal J. Neurosci. Res. Section Abstract Doc Link 16130146 Disease Relevance 0.09 Pain Relevance 1.54

Brain opiate receptor concentrations are increased in adult spontaneously hypertensive rats.

Positive_regulation (increased) of opiate receptor in Brain associated with hypertension and opiate

2) Confidence 0.70 Published 1979 Journal Endocr Res Commun Section Title Doc Link 232441 Disease Relevance 0.27 Pain Relevance 0.18

We conclude that U-50,488H prevents the impairment of working memory following transient forebrain ischemia, an event mediated by the activation of the kappa-opioid receptor.

Positive_regulation (activation) of kappa-opioid receptor in forebrain associated with ischemia and kappa opioid receptor

3) Confidence 0.70 Published 1991 Journal Eur. J. Pharmacol. Section Abstract Doc Link 1647321 Disease Relevance 0.50 Pain Relevance 0.37

These alterations in brain synaptosomal accumulation of methadone could result from the progressive increase in the affinity of methadone for synaptosomes as these particles become enriched in the protein and lipid contents and possibly increase in opiate receptor density during the neuronal maturation and the synaptogenesis of the developing brain.

Spec (possibly) Positive_regulation (increase) of opiate receptor in brain associated with opiate and methadone

4) Confidence 0.70 Published 1984 Journal Dev Pharmacol Ther Section Abstract Doc Link 6705654 Disease Relevance 0 Pain Relevance 0.73

An increase in opiate receptor-sites is associated with enhanced cardiovascular depressant, but not respiratory depressant action of morphine.

Positive_regulation (increase) of opiate receptor in respiratory associated with narcan, opiate and morphine

5) Confidence 0.70 Published 1984 Journal Brain Res. Section Title Doc Link 6322927 Disease Relevance 0 Pain Relevance 1.15

Kyotorphin (tyrosine-arginine): further evidence for indirect opiate receptor activation.

Positive_regulation (activation) of opiate receptor associated with opiate

6) Confidence 0.70 Published 1982 Journal Life Sci. Section Title Doc Link 6283289 Disease Relevance 0 Pain Relevance 0.82

In rats, kappa-receptor activation in this brainstem nucleus significantly attenuates local mu-receptor-mediated analgesia.

Positive_regulation (activation) of kappa-receptor in brainstem nucleus associated with medulla and analgesia

7) Confidence 0.69 Published 1997 Journal Nature Section Abstract Doc Link 9311779 Disease Relevance 0.09 Pain Relevance 1.69

Activation of the kappa-receptor hyperpolarizes neurons that are activated indirectly by the mu-receptor.

Positive_regulation (Activation) of kappa-receptor in neurons

8) Confidence 0.69 Published 1997 Journal Nature Section Abstract Doc Link 9311779 Disease Relevance 0.10 Pain Relevance 1.75

Here we present in vitro electrophysiological and in vivo behavioural evidence that activation of the kappa-receptor specifically antagonizes mu-receptor-mediated analgesia.

Positive_regulation (activation) of kappa-receptor associated with analgesia

9) Confidence 0.69 Published 1997 Journal Nature Section Abstract Doc Link 9311779 Disease Relevance 0.09 Pain Relevance 1.78

Two micro-opioid receptor agonists, morphine and endomorphin-1, whose effectiveness in neuropathic pain is different, also disparately influenced nociceptin/orphanin FQ system in this pain model, inasmuch as an increase in pronociceptin/orphanin FQ and ORL1 receptor mRNAs was observed in laminae I-VI after morphine administration (5 microg i.t.) but not after endomorphin-1 treatment (5 microg i.t.).

Positive_regulation (increase) of ORL1 associated with pain, orphanin, neuropathic pain, agonist, opioid receptor and morphine

10) Confidence 0.69 Published 2004 Journal Pharmacol. Biochem. Behav. Section Abstract Doc Link 15159147 Disease Relevance 0.52 Pain Relevance 1.71

The present electrophysiological study of the effects of NalBzOH on the activation of ORL1 and mu-opioid receptors was performed in brain slices of the ventrolateral periaqueductal grey (PAG), a crucial site for opioid-induced supraspinal analgesia.

Positive_regulation (activation) of ORL1 in brain associated with periaqueductal grey, mu opioid receptor, opioid and analgesia

11) Confidence 0.69 Published 2001 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 11414652 Disease Relevance 0.34 Pain Relevance 1.08

Both NC and ORL1 receptor IR were upregulated 7 days after nerve injury (to 56 and 55%) and inflammation (to 53 and 48%), respectively.

Positive_regulation (upregulated) of ORL1 in nerve associated with nervous system injury, inflammation and orphanin

12) Confidence 0.69 Published 2006 Journal J. Peripher. Nerv. Syst. Section Abstract Doc Link 16930285 Disease Relevance 1.50 Pain Relevance 1.36

Activation of opioid receptor like-1 receptor in the spinal cord produces sex-specific antinociception in the rat: estrogen attenuates antinociception in the female, whereas testosterone is required for the expression of antinociception in the male.

Positive_regulation (Activation) of opioid receptor like-1 receptor in spinal cord associated with antinociception, analgesic, opioid receptor and spinal cord

13) Confidence 0.68 Published 2006 Journal J. Neurosci. Section Title Doc Link 17167094 Disease Relevance 0.32 Pain Relevance 1.32

Opiate receptor density in the medial preoptic area (MPOA) was elevated on day 12 of gestation in both primigravid and multigravid rats when compared with ovariectomized subjects.

Positive_regulation (elevated) of Opiate receptor in preoptic area associated with urological neuroanatomy and opiate

14) Confidence 0.68 Published 1992 Journal Brain Res. Section Abstract Doc Link 1324763 Disease Relevance 0.37 Pain Relevance 0.39

Having verified the agonist properties of Ro64-6198, we then assessed the potency and distribution of ORL1 receptor activation in rat brain sections.

Positive_regulation (activation) of ORL1 receptor in brain associated with agonist and potency

15) Confidence 0.68 Published 2006 Journal Neuropeptides Section Abstract Doc Link 16403422 Disease Relevance 0.12 Pain Relevance 0.74

These results indicate that stimulation of ORL1 receptor accelerates the colonic contraction and transit independently from opioid receptors.

Positive_regulation (stimulation) of ORL1 receptor associated with opioid receptor

16) Confidence 0.68 Published 1998 Journal Eur. J. Pharmacol. Section Abstract Doc Link 9726656 Disease Relevance 0 Pain Relevance 0.83

These results demonstrate that orphanin FQ can function as an inhibitory modulator regulating synaptic transmission and synaptic plasticity in the hippocampus, suggesting that activation of ORL1 receptors may play an important role in synaptic plasticity involved in learning and memory.

Positive_regulation (activation) of ORL1 in hippocampus associated with orphanin and hippocampus

17) Confidence 0.67 Published 1997 Journal Hippocampus Section Abstract Doc Link 9138672 Disease Relevance 0 Pain Relevance 0.61

Up-regulation of ORL-1 receptors in spinal tissue of allodynic rats after sciatic nerve injury.

Positive_regulation (Up-regulation) of ORL-1 in spinal associated with pain, nervous system injury and sciatic nerve

18) Confidence 0.67 Published 2002 Journal Eur. J. Pharmacol. Section Title Doc Link 12106803 Disease Relevance 0.43 Pain Relevance 0.75

These findings suggested that r/m HK-1 might play an important role in pain modulation at supraspinal level in mice and these effects were first elicited through the activation of NK(1) receptor, subsequently, whether activation of the classical opioid receptor or the ORL1 receptor depending on the dose of i.c.v. administration of r/m HK-1.

Spec (whether) Positive_regulation (activation) of ORL1 associated with pain and opioid receptor

19) Confidence 0.67 Published 2005 Journal Brain Res. Section Abstract Doc Link 16102736 Disease Relevance 0.48 Pain Relevance 0.57

We have previously shown that activation of kappa opioid receptors within the rostral ventral medulla in lightly anesthetized rats has an anti-mu opioid analgesic action in male rats.

Positive_regulation (activation) of kappa opioid in ventral associated with medulla, analgesic, kappa opioid receptor and opioid

20) Confidence 0.66 Published 2000 Journal Pain Section Abstract Doc Link 10692614 Disease Relevance 0.22 Pain Relevance 1.06

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