INT6437

Context Info Confidence 0.47 First Reported 1981 Last Reported 2010 Negated 9 Speculated 4 Reported most in Abstract Documents 154 Total Number 159 Disease Relevance 26.30 Pain Relevance 90.46

cell differentiation (YY1) chromosome organization (YY1) RNA binding (YY1) plasma membrane (YY1) nucleus (YY1) intracellular (YY1)

Anatomy Link Frequency brain 9 lymphocytes 4 spinal 2 NK cell 2 body 2 YY1 (Homo sapiens)

Pain Link Frequency Relevance Heat Opioid 199 100.00 Enkephalin 170 100.00 opioid receptor 169 100.00 agonist 115 100.00 opiate 93 100.00 pregabalin 82 100.00 Delta opioid receptors 74 100.00 antagonist 73 100.00 Potency 32 100.00 tolerance 16 100.00

Disease Link Frequency Relevance Heat Alzheimer's Dementia 6 100.00 Eating Disorder 12 99.84 Neuroblastoma 13 99.68 Disease 56 99.64 Urological Neuroanatomy 16 99.44 Anxiety Disorder 18 99.36 Pain 94 99.34 Cancer 27 99.10 INFLAMMATION 10 99.00 Diabetes Mellitus 7 99.00

Sentences Mentioned In

Key:

Protein

Mutation

Event

Anatomy

Negation

Speculation

Pain term

Disease term

Compared with naloxone, nalmefene has a longer half-life, is more potent at the mu-receptor, and has a higher affinity for kappa- and delta-opioid receptors.

delta Binding (affinity) of associated with narcan and delta opioid receptors

1) Confidence 0.47 Published 1998 Journal Alcohol. Clin. Exp. Res. Section Abstract Doc Link 9802524 Disease Relevance 0.17 Pain Relevance 0.84

6-O-(2-[(18)F]fluoroethyl)-6-O-desmethyldiprenorphine ([(18)F]FDPN) is a nonselective opiate ligand that binds to postsynaptic micro, kappa and delta opiate receptors.

delta Binding (binds) of associated with opiate

2) Confidence 0.47 Published 2004 Journal Neuroimage Section Abstract Doc Link 15275909 Disease Relevance 0 Pain Relevance 0.29

Taken together, these findings suggest that modulation of receptor function as a result of physical associations between delta opiate receptors and alpha2A-adrenoceptors may account for the observed synergy between opiate and adrenergic agonists in spinal analgesia.

delta Binding (associations) of in spinal associated with agonist, opiate and analgesia

3) Confidence 0.47 Published 2004 Journal Clin. Exp. Pharmacol. Physiol. Section Abstract Doc Link 15566403 Disease Relevance 0 Pain Relevance 0.78

The putative mechanism of action of the drug is reduced excitatory neurotransmitter release caused by binding to the alpha(2)-delta protein, resulting in allosteric modulation of P/Q-type voltage-gated calcium channels.

delta Binding (binding) of associated with neurotransmitter and calcium channel

4) Confidence 0.47 Published 2005 Journal CNS Drugs Section Abstract Doc Link 15740180 Disease Relevance 0.35 Pain Relevance 0.60

This randomized controlled trial demonstrates that pregabalin, a new drug that interacts with the alpha2-delta protein subunit of the voltage-gated calcium channel, is an efficacious and safe treatment for the pain of this condition.

delta Binding (interacts) of associated with pain, pregabalin and calcium channel

5) Confidence 0.47 Published 2005 Journal J Pain Section Abstract Doc Link 15820913 Disease Relevance 1.35 Pain Relevance 1.67

When the carboxylate was replaced by a tetrazole, this group was recognized by the alpha2-delta protein.

delta Binding (recognized) of

6) Confidence 0.47 Published 2006 Journal Bioorg. Med. Chem. Lett. Section Abstract Doc Link 15946842 Disease Relevance 0 Pain Relevance 0.26

The pharmacologically defined kappa drug 3H-ethylketazocine (3H-EKC) and 3H-bremazocine bind to unique sites, but also to mu and delta receptors.

delta Binding (bind) of

7) Confidence 0.47 Published 1982 Journal Life Sci. Section Abstract Doc Link 6128654 Disease Relevance 0 Pain Relevance 0.66

These findings might allow peptides to be designed retaining a high affinity for delta opioid receptors associated with a very low cross-reactivity with mu binding sites.

delta Spec (might) Binding (affinity) of associated with delta opioid receptors

8) Confidence 0.47 Published 1987 Journal Int. J. Pept. Protein Res. Section Abstract Doc Link 3692682 Disease Relevance 0 Pain Relevance 0.21

The present study used in vitro expression systems to investigate interactions of members of the KDN series with delta-kappa heterodimers through competition binding using selective ligands and the mitogen-activated protein kinase (MAPK) assay.

delta Binding (interactions) of

9) Confidence 0.47 Published 2005 Journal Mol. Pharmacol. Section Abstract Doc Link 16006595 Disease Relevance 0 Pain Relevance 0.45

Other experiments revealed that the binding of naltrindole to delta opioid receptors could increase the binding of nor-BNI to kappa opioid receptors and vice versa, suggesting reciprocal allosteric modulation of receptors in the heterodimer.

delta Binding (binding) of associated with kappa opioid receptor and delta opioid receptors

10) Confidence 0.47 Published 2005 Journal Mol. Pharmacol. Section Abstract Doc Link 16006595 Disease Relevance 0 Pain Relevance 0.63

Evidence is also provided showing that nitrous oxide may be a partial agonist and that it may interact with the endogenous opioid system by the release of endogenous opioids, and/or by direct action at the mu, delta, sigma and kappa receptors.

delta Binding (interact) of associated with endogenous opioid and agonist

11) Confidence 0.47 Published 1986 Journal Life Sci. Section Abstract Doc Link 3020325 Disease Relevance 0 Pain Relevance 1.20

The results show that the kappa and delta receptors bind the same opioid core differently and achieve their selectivity through different mechanisms.

delta Binding (bind) of associated with opioid

12) Confidence 0.47 Published 1995 Journal J. Biol. Chem. Section Abstract Doc Link 7759527 Disease Relevance 0 Pain Relevance 0.37

Opioid antagonist naltrexone disrupts feedback interaction between mu and delta opioid receptors in splenocytes to prevent alcohol inhibition of NK cell function.

delta Binding (interaction) of in NK cell associated with antagonist, delta opioid receptors, opioid and alcohol

13) Confidence 0.47 Published 2004 Journal J. Immunol. Section Title Doc Link 15210757 Disease Relevance 0.09 Pain Relevance 0.79

Naltrexone disrupts this feedback control by reducing micro opioid receptor function, thereby up-regulating delta opioid receptor binding, which results in an enhanced NK cell cytolytic response to delta opioid receptor ligands.

delta Binding (binding) of in NK cell associated with opioid receptor

14) Confidence 0.47 Published 2004 Journal J. Immunol. Section Abstract Doc Link 15210757 Disease Relevance 0.07 Pain Relevance 0.73

Binding of the YGGFL-NH2 derivatives to the mu- and delta-opioid receptors, and to the anti-beta-endorphin monoclonal antibody (clone 3E7), indicated any change at the Leu5 had little effect on the binding when compared with modifications to the YGGF-sequence.

delta Binding (Binding) of associated with delta opioid receptors

15) Confidence 0.47 Published 1997 Journal Bioorg. Med. Chem. Section Abstract Doc Link 9354243 Disease Relevance 0 Pain Relevance 0.29

The pharmacological profile for inhibition of [3H]U69593 binding was determined in this brain region using drugs known to bind to mu, kappa and delta opioid receptors.

delta Binding (bind) of in brain associated with delta opioid receptors

16) Confidence 0.47 Published 1999 Journal Life Sci. Section Abstract Doc Link 10465345 Disease Relevance 0.16 Pain Relevance 0.55

This compound displays a binding affinity of 5.5 nM for the delta opioid receptor as well as a 470-fold delta versus mu selectivity.

delta Binding (affinity) of associated with opioid receptor

17) Confidence 0.47 Published 1999 Journal Bioorg. Med. Chem. Lett. Section Abstract Doc Link 10612597 Disease Relevance 0 Pain Relevance 0.31

Binding to delta opiod receptors was rarely, if ever, observed.

delta Binding (Binding) of

18) Confidence 0.47 Published 2000 Journal Immunopharmacology Section Abstract Doc Link 10708810 Disease Relevance 0.48 Pain Relevance 1.12

Binding of delta-opioid receptors is also decreased in the amygdaloid complex and ventral putamen of Alzheimer's disease brains.

delta Binding (Binding) of in ventral associated with delta opioid receptors and disease

19) Confidence 0.47 Published 2001 Journal Brain Res. Section Abstract Doc Link 11223000 Disease Relevance 0.61 Pain Relevance 0.72

A novel "restoration of function" mutagenesis strategy was developed to identify amino acid sequence combinations necessary to restore the ability to bind delta-selective ligands to an inactive delta/mu receptor chimera in which 10 amino acids of the third extracellular loop of the delta receptor were replaced by the corresponding amino acids from the mu receptor (delta/mu291-300).

delta Binding (bind) of

20) Confidence 0.47 Published 1997 Journal J. Biol. Chem. Section Abstract Doc Link 9083060 Disease Relevance 0 Pain Relevance 0.12

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